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Acetaminophen-d4 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase .
Sub1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sub1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
SUB1 Human Pre-designed siRNA Set A contains three designed siRNAs for SUB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Sub1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sub1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Ac-{Cpg}-Thr-Ala-{Ala(CO)}-Asp-{Cpg}-NH2 (compound 40) is a potent Plasmodium subtilisin-like protease 1 (SUB1) inhibitor. SUB1-IN-1 shows IC50 values of 12 nM and 10 nM against P. vivax and P. falciparumSUB1 (Pv- and PfSUB1), respectively .
Zidovudine-d4 is deuterated labeled Zidovudine (HY-17413). Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
4-Aminobenzoic acid-d4 is the deuterium labeled 4-Aminobenzoic acid. 4-Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi.
N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine . N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection [4] .
Demethoxycurcumin-d4 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin (Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties .
IMPDH-IN-2 (compound 2) is an inhibitor of inosine monophosphate dehydrogenase (IMPDH) with IC50 for IMPDH I and IMPDH II >Values are 0.15 and 0.17 μM, respectively. IMPDH-IN-2 has antitumor activity .
D-Glucose-d4 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Isoniazid-d4 is the deuterium labeled Isoniazid. Isoniazid (INH) is a proagent and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity [4].
Tiagabine-d4(NO050328-d4) is deuterium labeled Tiagabine. Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively .
Sulfameter-d4(Sulfametoxydiazine-d4) is the deuterium labeled Sulfameter (HY-B0213) . Sulfameter (Sulfametoxydiazine) is an orally active long-acting sulfonamide antibiotic. Sulfameter is active against both Gram-positive and Gram-negative bacteria. Sulfameter can be used for the research of diseases such as respiratory and urinary tract infections .
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Enclomiphene-d4((E)-Clomiphene-d4) hydrochloride?is a deuterium labeled Enclomiphene hydrochloride (HY-118861B). Enclomiphen hydrochloride?is a potent and orally active?estrogen receptor?antagonist with antioestrogenic property .
Enclomiphene-d4((E)-Clomiphene-d4) is a deuterium labeled Enclomiphene. Enclomiphen?is a potent and orally active?estrogen receptor?antagonist with antioestrogenic property .
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Phosphorylethanolamine-d4 (Monoaminoethyl phosphate-d4; NSC 254167-d4) is a deuterium labeled Phosphorylethanolamine (HY-N5034). Phosphorylethanolamine is an endogenous metabolite.
Telbivudine-d4 is deuterium labeled Telbivudine. Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication .
Binimetinib-d4(MEK162-d4) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
Cyclosporin A-d4 is the deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 ad
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Deracoxib-d4 (SC 046-d4; SC 59046--d4) is deuterium labeled Deracoxib (HY-17509). Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas.
Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
Erlotinib-d4(CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Valproic acid-d4 (sodium) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Vatalanib-d4(PTK787-d4;ZK-222584-d4;CGP-79787-d4) is the deuterium labeled Vatalanib (HY-10203). Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis[4].
Dihydromyricetin-d4(Ampelopsin-d4) is deuterium labeled Dihydromyricetin. Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination . Acyclovir prevents bacterial infections during induction therapy for acute leukaemia [4].
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
Bronopol-d4 is deuterium labeled Bronopol. Bronopol is an antibacterial agent with low toxicity (to mammals) and high activity (especially against Gram-negative bacteria). Bronopol oxidizes protein thiols, inhibits enzymatic activity, and exhibits antibacterial activity. Bronopol is also a formaldehyde releaser .
Sulfamethazine-d4(Sulfadimidine-d4) is a deuterium labeled Sulfamethazine (Sulfadimidine). Sulfamethazine is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections) .
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells .
Butylparaben-d4 is the deuterium labeled Butylparaben. Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
2-Phenylethanol-d4 is the deuterium labeled 2-Phenylethanol . 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans . It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Cladribine-d4(2-Chloro-2′-deoxyadenosine-d4) is deuterium labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis .
Hydroxytyrosol-d4 (DOPET-d4) is the deuterium labeled Hydroxytyrosol (HY-N0570). Hydroxytyrosol is a phenol found in the olive oil. Hydroxytyrosol can alleviate oxidative stress and improve mitochondrial function, thereby exerting neuroprotective effects. Hydroxytyrosol can induce cancer cells apoptosis via inducing ROS production. Hydroxytyrosol shows antibacterial and antiviral effect. Hydroxytyrosol can be used for the researches of cancer, infection, inflammation, immunology, metabolic, neurological and cardiovascular disease, such as colon cancer, diabetes, Alzheimer's Disease and atherosclerosis [4] .
D-Alanine-d4 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
(-)-(S)-Cibenzoline-d4(Escibenzoline-d4) is deuterium labeled (-)-(S)-Cibenzoline. (-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent .
Fosribnicotinamide-d4 (β-Nicotinamide mononucleotide-d4) is the deuterium labeled Fosribnicotinamide. Fosribnicotinamide is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD+ intermediate. The pharmacological activities of Fosribnicotinamide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity .
Thymidine-d4 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication .
Miltefosine-d4(HePC-d4) is deuterium labeled Miltefosine. Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity [4]. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT) .
Levamlodipine-d4 is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina .
Dropropizine-d4((±)-Dropropizine-d4) is deuterium labeled Dropropizine. Dropropizine ((±)-Dropropizine) belongs to the phenylpiperazine group of organic compounds. Dropropizine is a peripheral antitussive agent that acts by inhibiting cough reflex through its action on the peripheral receptors and their afferent conductors .
Carbamazepine-d4(CBZ-d4) is the deuterium labeled Carbamazepine (HY-B0246) . Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na +, Ca 2+, and K + channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.
Difethialone-d4(Baraki-d4; LM 2219-d4) is the deuterium labeled Difethialone (HY-113958). Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Adefovir-d4 is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses .
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Leriglitazone-d4(MIN-102-d4;Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
Rifampicin-d4 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Rebamipide-d4 is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner .
Exemestane-d4 (FCE 24304-d4) is deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Salbutamol-d4(Albuterol-d4;AH-3365-d4) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is a short-acting beta-2 adrenergic receptor agonist with oral activity. Salbutamol promotes tumorigenesis of gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol is used to study bronchospasms caused by asthma and chronic obstructive pulmonary disease (COPD) .
Sulfabrom-d4 (N 3517-d4) is is the deuterium labeled Sulfabrom (HY-U00131). Sulfabrom is a long-acting Sulfonamide that is used for the treatment of coccidiosis and various bacterial infections in the poultry, swine and cattle .
Aspirin-d4 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis [4] .
Estrone-d4 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Nicotinamide-d4 is the deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
4-Methylumbelliferone- 13C4 (Hymecromone- 13C4) is the 13C-labeled 4-Methylumbelliferone (HY-N0187). 4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects.
Corticosterone-d4 is the deuterium labeled Corticosterone. Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
Estradiol-d4 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
D-Glucose-d-44 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Etoricoxib-d4(MK-0663-d4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Vitamin K1-d4 is the deuterium labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism .
Fosamprenavir-d4 is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .
Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Lapatinib-d4(GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
D-Sorbitol-d4 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
Baloxavir-d4 (Baloxavir acid-d4;S-033447-d4) is the deuterium-labeled Baloxavir (HY-109025A). Baloxavir-d4(Baloxavir-d4 acid), derived from the proagent Baloxavir-d4 marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir-d4 inhibits viral RNA transcription and replication and has potently antiviral activity .
Serotonin-d4(5-Hydroxytryptamine-d4) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473) . Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Cibenzoline-d4(Cifenline-d4) is deuterium labeled Cibenzoline. Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a KATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC50 of 22.2 μM. Cibenzoline inhibits IKr and IKs currents with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia [4].
Procainamide-d4 hydrochloride is deuterated labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Entinostat-d4 is the deuterium labeled Entinostat . Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively .
Lornoxicam-d4 is the deuterium labeled Lornoxicam. Lornoxicam (Chlortenoxicam), a COX-1 and COX-2 inhibitor, is a new nonsteroidal anti-inflammatory agent (NSAID).
Penciclovir-d4 is the deuterium labeled Penciclovir. Penciclovir is reported to be potent against HSV types 1 and 2 with IC50 of 0.04-1.8 μg/mL and 0.06-4.4 μg/mL, respectively .
Lifitegrast-d4 (SAR 1118-d4) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Cysteamine-d4 (hydrochloride) is the deuterium labeled Cysteamine hydrochloride. Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
Isavuconazole-d4(BAL-4815-d4) is a deuterium labeled Isavuconazole (BAL-4815). Isavuconazole is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi .
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
Pantoprazole-d4(BY1023-d4) is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Lomitapide-d4(AEGR-733-d4) is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Palmitoylethanolamide-d4 is the deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.
Talazoparib-d4(BMN-673-d4) is deuterium labeled Talazoparib. Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity .
N4-Acetylsulfamerazine-d4(Acetylsulfamerazine-d4;Sulfamelazine-d4) is the deuterium labeled N4-Acetylsulfamerazine (HY-W031230). N4-Acetylsulfamerazine is a sulfonamides derivative .
Glimepiride-d4-1 is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
Darolutamide-d4(ODM-201-d4) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay .
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Caspofungin-d4 (acetate) is the deuterium labeled Caspofungin diacetate . Caspofungin (MK-0991) diacetate is a potent antifungal agent. Caspofungin diacetate inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan .
Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
(-)-Epigallocatechin Gallate-d4(EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma [4].
Dapivirine-d4(TMC120-d4) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities .
Revefenacin-d4(TD-4208-d4) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Secnidazole-d4 is the deuterium labeled Secnidazole . Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Serotonin-d4 is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
Caspofungin-d4(MK-0991-d4;L-743872-d4) is a deuterium labeled Caspofungin (HY-17006A). Caspofungin is a potent antifungal agent. Caspofungin inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan .
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
Irbesartan-d4(SR-47436-d4) is the deuterium labeled Irbesartan Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
Volinanserin-d4 (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity .
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
3-Nitrobenzoic acid-d4(m-Carboxynitrobenzene-d4; m-Nitrobenzenecarboxylic acid-d4; m-Nitrobenzoic acid-d4) is the deuterium labeled 3-Nitrobenzoic acid (HY-Y1313). 3-Nitrobenzoic acid is an antioxidant and antibacterial agent that can kill bacteria and fungi. 3-Nitrobenzoic acid can be degraded or reduced by certain bacteria (such as Pseudomonas) and fungi (such as white rot fungi) into aldehydes and alcohols.
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
Carvedilol metabolite 4-Hydroxyphenyl Carvedilol-d4 is deuterated labeled Carvedilol metabolite 4-Hydroxyphenyl Carvedilol (HY-12767). 4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol.
Acetaminophen-d7 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
Acetaminophen-d3 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
Acetaminophen-d5 is deuterated-labeled Acetaminophen (HY-66005). Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
NAD+-d4 is the deuterium-labeled NAD+ (HY-B0445). NAD+-d4 is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
Pimelic acid-d4 is the deuterium labeled Pimelic acid . Pimelic acid is the organic compound and its derivatives are involved in the biosynthesis of the amino acid called lysine.
Imatinib-d4(STI571-d4) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM) .
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .
Thiamine-d4 (hydrochloride) is deuterium labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
Pioglitazone-d4 hydrochloride (U 72107A-d4; AD 4833-d4) is the deuterium labeled Pioglitazone hydrochloride (HY-14601). Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
Valproic acid-d4 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
Etoposide-d4(VP-16-d4;VP-16-213-d4) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Clopidogrel carboxylic acid-d4 is a deuterated derivative of Clopidogrel carboxylic acid, which is an inactive metabolite of the antiplatelet agent Clopidogrel (HY-15283) in plasma. Clopidogrel carboxylic acid-d4 can be used to further explore the metabolic characteristics of Clopidogrel .
Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Octisalate-d4 (Octyl salicylate-d4; 2-Ethylhexyl salicylate-d4) is the deuterium labeled Octisalate (HY-B0929). Octisalate (Octyl salicylate) is an organic compound with high lipophilicity, which is used in sunscreens and cosmetics that absorbs UVB rays .
Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder .
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
Propylparaben-d4 is the deuterium labeled Propylparaben . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats [4].
4-Methylanisole-d4 is the deuterium labeled 4-Methylanisole . 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil .
4-Vinylphenol-d4 is deuterated labeled 4-Vinylphenol (HY-W005288). 4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
(-)-Epigallocatechin Gallate-d3/d4(EGCG-d3/d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma [4].
Higenamine-d4-1(Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [4] .
L-5-Hydroxytryptophan-d4(L-5-HTP-d4;Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [4] .
Retinyl acetate-d4 is the deuterium labeled Retinyl acetate . Retinyl acetate is a synthetic acetate ester form derived from retinol and has potential antineoplastic and chemo preventive activities .
Ticagrelor-d4(AZD6140-d4) is deuterium labeled Ticagrelor. Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
Losartan-d4 carboxylic acid (E-3174-d4) is the deuterium labeled Losartan Carboxylic Acid (HY-12765). Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
Loratadine-d4-1(Loratidine-d4-1) is deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators .
Folic acid-d4 is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
Glimepiride-d4-2(GliAmperide-d4-2) is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
4-(Trifluoromethyl)aniline-d4(4-Aminobenzotrifluoride-d4) is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively .
L-Asparagine- 13C4 monohydrate is the 13C-labeled L-Asparagine monohydrate (HY-W017443). L-Asparagine monohydrate is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine monohydrate can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia [4] .
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Dinoprost-d4 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
N-(3-Indolylacetyl)-L-alanine-d4(Indoleacetylalanine-d4) is the deuterium labeled N-(3-Indolylacetyl)-L-alanine (HY-W141858). N-(3-Indolylacetyl)-L-alanine is an indoleacetylamino acid. N-(3-Indolylacetyl)-L-alanine appears to increase callus growth and reduces the ability of growths to differentiate into shoots of Phalaenopsis orchids .
p-Anisic acid-d4 is the deuterium labeled p-Anisic acid . p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties .
Folitixorin-d4(5,10-Methylenetetrafolate-d4; ANX-510 (free acid)-d4) is the deuterium labeled Folitixorin (HY-14769). Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research .
β-Alanine-d4 is the deuterium labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
Olaparib-d4-1(AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [4].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ～30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
Alpha-Naphthoflavone (Standard) is the analytical standard of Alpha-Naphthoflavone. This product is intended for research and analytical applications. Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis [4].
Toxoflavin- 13C4 is the 13C-labeled Toxoflavin. Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity . Antibiotic properties.
5-Azacytidine- 15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy[4].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
Cyclosporin A- 13C2,d4 (Cyclosporine A- 13C2,d4; Ciclosporin A- 13C2,d4) is a 13C labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
AChE/Aβ-IN-3 (compound AM5) is a dual inhibitor of AChE and Amyloid-β aggregation with IC50<.sub> values of 1.29 and 4.93 μM, respectively. AChE/Aβ-IN-3 has antioxidant properties that scavenge ROS and restore their normal levels. AChE/Aβ-IN-3 can be used in the study of neurological diseases, such as Alzheimer's disease .
Nitroxoline-d4 is the deuterium labeled Nitroxoline. Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe 2+ and Zn 2+ ions from the biofilm matrix .
Valproic acid-d4-1 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
3-Indoleacetic acid-d4 (Indole-3-acetic acid-d4;3-IAA-d4) is the deuterium labeled 3-Indoleacetic acid (HY-18569) . 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Lipoic acid-d4 ((R)-(+)-α-Lipoic acid-d4) is deuterium labeled Lipoic acid. Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid .
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD) .
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
Acotiamide-d4 (Z-338 (free base)-d4) is deuterium labeled Acotiamide. Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
4-Aminohippuric acid-d4 (p-Aminohippuric acid-d4) is the deuterium labeled 4-Aminohippuric acid (HY-B1306). 4-Aminohippuric acid (p-Aminohippuric acid) is a coordination ligand for metal ions (such as Cu 2+, Fe 3+, Hg 2+) and a functionalization reagent for nanomaterials. 4-Aminohippuric acid can coordinate with metal ions or modify the surface of materials such as carbon nanotubes and gold nanoparticles through amino and carboxyl groups. 4-Aminohippuric acid can form stable complexes with metal ions or participate in the synthesis of nanomaterials as a reducing agent/stabilizer, enriching metal ions or giving nanoparticles peroxidase-mimicking activity. 4-Aminohippuric acid can be used to construct highly sensitive electrochemical sensors or colorimetric sensors to detect and quantitatively analyze heavy metal ions such as copper, iron, and mercury in environmental water samples and biological samples. 4-Aminohippuric acid may also be a biomarker for attention-deficit/hyperactivity disorder (ADHD) [4].
4-Oxofenretinide-d4(4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
Sutezolid- 13C4 (PNU-100480- 13C4) is 13C labeled Sutezolid. Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis .
Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla) .
FSI-TN42 (N42) is a selective, orally active and irreversible ALDH1A1 inhibitor with an IC50 of 23 nM. FSI-TN42 shows 800-fold more potent against ALDH1A1 than ALDH1A2 (IC50 of 18 μM). FSI-TN42 suppresses weight gain in a diet induced mouse model of obesity .
Ezetimibe phenoxy glucuronide-d4 is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity . Ezetimibe is a potent cholesterol absorption inhibitor .
Mono-(2-ethylhexyl) phthalate-d4 is a deuterium labeled Mono-(2-ethylhexyl) phthalate (HY-W018392). Mono-(2-ethylhexyl) phthalate (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP). Mono-(2-ethylhexyl) phthalate can promote fatty acid synthesis in hepatocytes by regulating the expression of relevant genes and proteins, contributing to non-alcoholic fatty liver disease (NAFLD) .
Leukotriene B4-d4 is the deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs .
Colfosceril miristate-d4(DMPC-d4) is deuterium labeled Colfosceril miristate. Colfosceril miristate is a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Tamsulosin-d4 ((R)-(-)-YM12617 (free base)-d4) is deuterium labeled Tamsulosin. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
Drospirenone-d4 is the deuterium labeled Drospirenone. Drospirenone (Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone .
Sulfatroxazole-d4(Isosulfafurazole-d4) is the deuterium labeled Sulfatroxazole (HY-105829) . Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50 of 0.26 μM) .
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Sulfacetamide-d4(Sulphacetamide-d4) is the deuterium labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
Ethambutol-d4 dihydrochloride is deuterated labeled Ethambutol dihydrochloride (HY-B0535A). Ethambutol dihydrochloride is an antimycobacterial compound that prevents cell wall formation by inhibiting arabinosyltransferase activity.
Sulfadimethoxine-d4 is a deuterium labeled Sulfadimethoxine (Sulphadimethoxine). Sulfadimethoxine is a sulfonamide antibiotic used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections .
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
Salcaprozate-d4 (sodium) is a deuterated labeled Salcaprozate (sodium) . Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation .
Tetrahydrozoline-d4 (hydrochloride) is the deuterium labeled Tetrahydrozoline hydrochloride. Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion .
Chlorpheniramine-d4(Chlorphenamine-d4) is deuterium labeled Chlorpheniramine. Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research .
Indomethacin-d4(Indometacin-d4) is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells . Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes .
Dicyclomine-d4 is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Sulfachloropyridazine-d4 is the deuterium labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria .
Sulfisomidin-d4(Sulfaisodimidine-d4) is deuterium labeled Sulfisomidin. Sulfisomidin (Sulfaisodimidine) is an orally active short-acting sulfonamide antibacterial. Sulfisomidin can be used for the research of lower urinary tract infections .
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
Nefopam-d4 (hydrochloride) is deuterium labeled Nefopam (hydrochloride). Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo .
Histamine-d4(Ergamine-d4) is deuterium labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
Ethambutol-d4 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Dibenzylamine-d4(Bisbenzylamine-d4) is the deuterium labeled Dibenzylamine (HY-Y1067). Dibenzylamine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Hydrocortisone-d4 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Sulfadoxine-d4 is the deuterium labeled Sulfadoxine. Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
(±)-Lisofylline-d4((±)-Lisophylline-d4) is deuterium labeled (±)-Lisofylline. (±)-Lisofylline ((±)-Lisophylline) is the racemate of Lisofylline. Lisofylline inhibits the generation of phosphatidic acid and free fatty acids. Lisofylline also blocks the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline can be used for Type 1 diabetes research .
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
Desmethylcitalopram-d4 hydrochloride is deuterated labeled Desmethylcitalopram hydrochloride (HY-113739). Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6, -2C19 with IC50s of 39.5 and 53.5 μM .
Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Cabozantinib-d4 (S-malate) (XL184-d4 (S-malate); BMS-907351-d4 (S-malate)) is the deuterium labeled Cabozantinib (S-malate) (HY-12044). Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
D-Glucose- 13C2-4 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with Kis of 64 nM, 0.03 nM and 0.7 nM in rat, human and ferret, respectively .
ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research .
Neochilenin (3-O-Methylquercetin 4 '-O-glucoside) is a glycoside of 3-O-methylquercetin, which can be isolated from the sub-family Cereoideae (Cactaceae). .
Everolimus- 13C2,d4 (RAD001- 13C2,d4) is 13C labeled Everolimus. Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities .
Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties [4] .
Sacubitrilat- 13C4 (Desethyl Sacubitril- 13C4) is 13C labeled Sacubitrilat. Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
Hypoxanthine- 15N4 is the 15N labeled Hypoxanthine . Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia .
Pyridoxine- 13C4 (hydrochloride) is the 13C-labeled Pyridoxine (hydrochloride). Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
4'-Fluoroacetophenone-d4(1-(4-Fluorophenyl)ethan-1-one-d4) is deuterium labeled 4'-Fluoroacetophenone. 4'-Fluoroacetophenone (1-(4-Fluorophenyl)ethan-1-one) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Lenalidomide-d4(CC-5013-d4) is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Lesinurad-d4(RDEA594-d4) is deuterium labeled Lesinurad. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 μM, respectively.
Ketoprofen-d4 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively .
Homosalate-d4 is the deuterium labeled Homosalate. Homosalate is an organic compound used in some sunscreens, it is used as a chemical UV filter, protecting the skin from sun damage.
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
Evocalcet-d4(KHK7580-d4) is deuterium labeled Evocalcet. Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism .
Carboplatin-d4 is the deuterium labeled Carboplatin. Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
Oxcarbazepine-d4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Anti-cancer and anticonvulsant effects .
Diisopropyl phthalate-d4(DiPP-d4) is the deuterium labeled Diisopropyl Phthalate (HY-W011926). Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM .
Ertapenem-d4(MK-0826-d4) is deuterium labeled Ertapenem. Ertapenem (MK-0826) is a broad spectrum and long acting β-lactam antibiotic. Ertapenem has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract .
Etodolac-d4(AY-24236-d4) is deuterium labeled Etodolac. Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM)
Terconazole-d4 is the deuterium labeled Terconazole. Terconazole is a broad-spectrum antifungal medication for the treatment of vaginal yeast infection.
4-Hydroxytolbutamide-d9 is the deuterium labeled 4-Hydroxytolbutamide. 4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic .
Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Darifenacin-d4 is the deuterium labeled Darifenacin . Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) .
Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant .
Granisetron-d4 (BRL 43694-d4) is deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
Equilin-d4 is the deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism .
Ropinirole-d4 (SKF 101468-d4) hydrochloride is the deuterium labeled Ropinirole hydrochloride. Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Kiof 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Sulfabenzamide-d4 is the deuterium labeled Sulfabenzamide (HY-B0960). Sulfabenzamide (N-Sulfanilylbenzamide) is an antimicrobial agent and usually consumed in combination with Sulfathiazole and Sulfacetamide. Sulfabenzamide is effective against Gram-positive and negative bacterial strains .
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
Azaperone-d4 is the deuterium labeled Azaperone. Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic agent with antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM .
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Acalabrutinib-d4(ACP-196-d4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
Posaconazole-d4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity .
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Risedronic acid-d4(Risedronate-d4) is the deuterium labeled Risedronic acid (HY-B0148). Risedronic acid (Risedronate) is a bisphosphonate and potent antiresorptive agent. Risedronic acid induces Apoptosis. Risedronic acid inhibits the transfer of farnesyl pyrophosphate groups to parasite proteins. Risedronic acid inhibits osteoclast-mediated bone resorption and alters bone metabolism. Risedronic acid inhibits blood-stage Plasmodium falciparum (IC50 of 20.3 μM) [4].
Azilsartan-d4 is the deuterium labeled Azilsartan . Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research [4] .
Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Paroxetine-d4(BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches [4] .
Lansoprazole-d4(AG-1749-d4) is a deuterium labeled Lansoprazole. Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid .
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities [4].
Mirogabalin-d4(DS5565-d4) is a deuterated compound of Mirogabalin (HY-12650), a ligand that selectively targets the voltage-sensitive calcium channel complex α2δ-1 .
Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
Mequinol-d4 is the deuterium labeled Mequinol[1]. Mequinol (4-Methoxyphenol) is one of bioactive components in Mercurialis. Mequinol is used for skin depigmentation[2].
Efinaconazole-d4 is the deuterium labeled Efinaconazole. Efinaconazole (KP-103) is a triazole antifungal agent and againsts T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 μg/mL and 0.00098 μg/mL, respectively . Efinaconazole has a potent in vitro activity against fungal pathogens including dermatophytes, Candida and Malassezia species .
Gusacitinib-d4(ASN-002-d4) is the deuterium labeled Gusacitinib (HY-103018). Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5 .
Cinacalcet-d4(AMG-073-d4) hydrochlorideis deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment .
Vanzacaftor-d4(VX-121-d4) is the deuterium labeled Vanzacaftor (HY-145603). Vanzacaftor is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases .
Acipimox-d4 is the deuterium labeled Acipimox. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Hydroxymetronidazole-d4 is the deuterium labeled Hydroxymetronidazole. Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle .
(R)-Lansoprazole-d4 is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Rabeprazole-d4 potassium is deuterated labeled Rabeprazole potassium. Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an b>IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux .
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
Sarpogrelate-d4(MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis [4].
Famotidine-d4(MK-208-d4) is deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion .
Famciclovir-d4 is the deuterium labeled Famciclovir. Famciclovir (BRL 42810) is a guanine analogue antiviral agent used for the treatment of various herpesvirus infections .
Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
Latanoprost-d4 is the deuterium labeled Latanoprost. Latanoprost (PHXA41) is a prostaglandin F2α analogue and an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).
Sitagliptin-d4(MK-0431-d4) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
Sacubitril-d4 is the deuterium labeled Sacubitril. Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer [4] .
2-Mercaptoethanesulfonate-d4 sodium (Mesnum-d4 sodium) is the deuterium labeled Sodium 2-mercaptoethanesulfonate (HY-13679). Mesna (Sodium 2-mercaptoethanesulfonate) is an antioxidant which has cytoprotective effects. Mesna is widely used as a systemic protective agent against chemotherapy toxicity. Mesna is also used to reduce hemorrhagic cystitis induced by cyclophosphamide .
Raltegravir-d4 (potassium) (MK 0518-d4 (potassium)) is deuterium labeled Raltegravir (potassium). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CLpro activity [4].
Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
Remdesivir-d4(GS-5734-d4) is deuterium labeled Remdesivir (HY-104077). Remdesivir (GS-5734) is a nucleoside analogue with effective antiviral activity. Remdesivir can inhibit the synthesis of viral DNA or RNA. Remdesivir can be used for the research of infection, such as SARS-CoV and MHV infection .
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K .
Sitagliptin-d4 (hydrochloride) is the deuterium labeled Sitagliptin . Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Losartan-d4 is the deuterium labeled Losartan. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure .
2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide . 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics .
Quinapril-d4(CI-906-d4) is deuterium labeled Quinapril. Quinapril is a potent, orally active, non-peptide and nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE). Quinapril specifically interrupts the conversion of angiotensin I to angiotensin II in both plasma and tissue. Quinapril is enzymatically hydrolyzed to a pharmacologically active diacid form quinaprilat. Quinapril is efficacious in hypertensive models .
Rabeprazole-d4 is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux .
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors [4] .
Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Ponesimod-d4(ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation [4].
Flecainide-d4 (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential .
Glycochenodeoxycholic acid-d4 is the deuterium labeled Glycochenodeoxycholic acid. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) induces hepatocyte apoptosis .
Prasugrel-d4 is the deuterium labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Cilnidipine-d4(FRC-8653-d4) is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca 2+-channel blocker on L and N-type Ca 2+ channel [4]. Antihypertensive effects .
Delamanid-d4 is the deuterium labeled Delamanid. Delamanid, a newer?mycobacterial cell wall synthesis ?inhibitor, inhibits the synthesisi of mucolic acids .
Prothioconazole-d4(JAU-6476-d4) is the deuterium labeled Prothioconazole (HY-116568). Prothioconazole is a triazolinthione fungicide. Prothioconazole is a CYP51 inhibitor .
Glasdegib-d4(PF-04449913-d4) is deuterium labeled Glasdegib. Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
Candesartan-d4(CV-11974-d4) is the deuterium labeled Candesartan (HY-B0205). Candesartan (CV 11974) is an orally active angiotensin II AT1-Receptor blocker and PPAR-γ agonist. Candesartan has potent and long-lasting antihypertensive effects. Candesartan can be used for the research of hypertension, chronic heart failure (CHF) and Traumatic brain injury (TBI).
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
Tecovirimat-d4(ST-246-d4) is a deuterium-labelled Tecovirimat (HY-14805). Tecovirimat is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat could be used in the study for orthopoxvirus-induced diseases [4] .
Eliglustat-d4 is the deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM .
Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levocetirizine-d4((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
Erdosteine-d4 is a deuterium labeled Erdosteine (HY-B0289). Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects .
Momelotinib-d4(CYT387-d4) dihydrochloride hydrate is a deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50s of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3 .
Diclazuril-d4 is deuterium labeled Diclazuril. Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. Diclazuril can be used for the research of certain infectious and parasitic diseases, including coccidiosis, acute toxoplasmosis, equine protozoal pyoencephalitis (EPM) et.al .
(R)-Pantetheine-d4(Pantetheine-d4) is the deuterium labeled (R)-Pantetheine (HY-126050). (R)-Pantetheine is the biosynthetic precursor to CoA. (R)-Pantetheine and its corresponding disulfide pantethine, play a key role in metabolism as a building block of coenzyme A (CoA). (R)-Pantetheine has high toxicity .
Meclofenamic acid-d4 is the deuterium labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker .
Ezetimibe-d4 (SCH 58235-d4) is the deuterium labeled Ezetimibe (HY-17376). Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Butenafine-d4 (KP363-d4) is the deuterium labeled Butenafine (HY-114518). Butenafine (KP363) is a potent and broad spectrum benzylamine antifungal agent . Butenafine inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation, leading to a deficiency of the fungal cell membranes. Butenafine is effective against dermatophytes infections, such as ?tinea pedis, ?tinea cruris, tinea versicolor .
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
Dapagliflozin-d4(BMS-512148-d4) is deuterium labeled Dapagliflozin. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
Elacestrant-d4(RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Methylprednisolone-d4 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels .
Dasatinib-d4(BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Rabeprazole-d4 (sodium) is the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
Olmesartan-d4(RNH-6270-d4) is the deuterium labeled Olmesartan (HY-17004). Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma [4].
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
Pazufloxacin-d4 is deuterium labeled Pazufloxacin (HY-B0724B). Pazufloxacin is an orally active fluoroquinolone antimicrobial agent. Pazufloxacin inhibits DNA gyrase with IC50 values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). Pazufloxacin exhibits broad-spectrum antimicrobial activity, with MIC90 values ranging from 0.025 to 100 μg/mL against Gram-positive and Gram-negative bacteria, non-fermenting bacteria, Legionella spp., and anaerobic bacteria. Pazufloxacin is indicated for research on systemic infections, lung infections, urinary tract infections, and Legionella pneumonia [4] .
Glycoursodeoxycholic acid-d4(Ursodeoxycholylglycine-d4) is the deuterium labeled Glycoursodeoxycholic acid. Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid .
Lumateperone-d4(ITI-007-d4) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .
Fluconazole-d4 is the deuterium labeled Fluconazole. Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL .
Nemonoxacin-d4 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
Piroxicam-d4 is the deuterium labeled Piroxicam. Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
Didesethyl chloroquine-d4 is the deuterium labeled Didesethyl chloroquine. Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial agent Chloroquine. Didesethyl chloroquine is a potent myocardial depressant .
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Estragole-d4 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity [4] [10] .
Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
Empagliflozin-d4 is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2 .
Ciprofloxacin-d4(Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity [4].
Bimatoprost-d4 is the deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface .
Flurbiprofen-d4 is deuterated labeled Flurbiprofen (HY-10582). Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma [4] .
Urea-d4 is the deuterium labeled Urea . Urea is a powerful protein denaturant via both direct and indirect mechanisms . A potent emollient and keratolytic agent . Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function [4]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic .
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .
Glutathione oxidized- 13C4, 15N2 is the 13C and 15N labeled Glutathione oxidized (HY-D0844). Glutathione oxidized is produced by the oxidation of glutathione. Detoxification of reactive oxygen species is accompanied by production of glutathione oxidized. Glutathione oxidized can be used for the research of sickle cells and erythrocytes .
Inosinic acid- 15N4 dilithium (5'-IMP-15N4 (dilithium); IMP-15N4 (dilithium); Inosine 5'-(dihydrogen phosphate)-15N4 (dilithium)) is 15N-labeled Inosinic acid (HY-108213). Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant, or as the dietary supplement to improve the yield and meat quality of pigs .
Ceftolozane- 15N2,d4 (CXA-101- 15N2,d4) TFA is the 15N- and deuterium-labeled Ceftolozane TFA (HY-106257A). Ceftolozane TFA is a cephalosporin antibiotic that can be used to inhibit Gram-negative bacterial infections. Ceftolozane TFA can be used to synthesize new antibiotic that are more potent and safer .
Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
Clindamycin (hydrochloride monohydrate) (Standard) is the analytical standard of Clindamycin (hydrochloride monohydrate). This product is intended for research and analytical applications. Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla) .
N6-Methyladenosine- 13C4 (6-Methyladenosine- 13C4; N-Methyladenosine- 13C4) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
Rivaroxaban-d4 (BAY 59-7939-d4) is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM) .
N-Acetylsulfanilamide-d4(4-Acetamidobenzenesulfonamide-d4) is a deuterium labeled N-Acetylsulfanilamide (HY-W069721). N-Acetylsulfanilamide is a compound with potential anti-infective activity .
Sulfamethoxazole-d4 (Ro 4-2130-d4) is a deuterium labeled Sulfamethoxazole (HY-B0322). Sulfamethoxazole (Ro 4-2130) is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
Diethyl succinate-d4 is the deuterium labeled Diethyl succinate . Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring .
Eslicarbazepine-d4 (BIA 2-194-d4) is deuterium labeled Eslicarbazepine. Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
Dihydrouracil-d4 is the deuterium labeled Dihydrouracil . Dihydrouracil (HY-W012926), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient .
Fenofibric acid-d4 (FNF acid-d4) is deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
cis-Atovaquone-d4 is deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Nonanoic acid-d4 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
Minodronic acid-d4 is deuterium labeled Minodronic acid. Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain .
Suberic acid-d4 is the deuterium labeled Suberic acid . Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency .
Taurine-d4 is the deuterium labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
Hydroxychloroquine-d4 (sulfate) is the deuterium labeled Hydroxychloroquine sulfate. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro .
Isobutylparaben-d4 is the deuterium labeled Isobutylparaben. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics .
Tenoxicam-d4(Ro-12-0068-d4) is the deuterium labeled Tenoxicam (HY-B0440). Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
Lansoprazole sulfone-d4(AG-1813-d4) is the deuterium labeled Lansoprazole sulfone. Lansoprazole sulfone-d4 is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone-d4 can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone-d4 has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease .
Moxifloxacin-d4 hydrochloride (BAY 12-8039-d4) is the hydrochloride salt form of deuterium labeled Moxifloxacin (Moxifloxacin). Moxifloxacin is an orally active antimicrobial, that can be used in the research of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Climbazole-d4 is the deuterium labeled Climbazole. Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450 .
Benzyl salicylate-d4 (NSC 6647-d4) is the deuterium labeled Benzyl salicylate (HY-B1556). Benzyl salicylate (NSC 6647)?is a salicylic acid benzyl ester. It can be used as a fragrance additive or UV light absorber .
Taurocholic acid-d4 (sodium) is the deuterium labeled Taurocholic acid. Taurocholic acid (N-Choloyltaurine) is a bile acid involved in the emulsification of fats.
Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
SAH-d4 is the deuterium labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine . SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 μM .
Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects .
21-Desacetyldeflazacort-d4(21-desDFZ-d4) is the deuterium labeled 21-Desacetyldeflazacort (HY-100085). 21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
Cefadroxil-d4 (hydrate) is the deuterium labeled Cefadroxil hydrate (HY-B1190A). Cefadroxil hydrate is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil hydrate inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil hydrate is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil hydrate has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain [4] .
4-Methylanisole-d7 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
4-Hydroxynonenal-d3 is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria .
Succinic-2,2,3,3-d4 acid is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
Glycohyocholic acid-d4 is the deuterium labeled Glycohyocholic acid (HY-122141). Glycohyocholic acid (GHCA) is a primary conjugated bile acid formed by the conjugation of Cholic acid (HY-N0324) and Glycine (HY-Y0966). Glycohyocholic acid can be used in the study of hepatitis C-related cirrhosis and diabetes mellitus [4].
Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
Tolcapone-d4 (Ro 40-7592-d4) is the deuterium labeled Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4].
Nifedipine-d4 is the deuterium labeled Nifedipine. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
DSG Crosslinker-d4 is the deuterium labeled DSG Crosslinker. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Acarbose-d4 (BAY g 5421-d4) is deuterium labeled Acarbose. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate . Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products . A systemic acquired resistance (SAR) signal in tobacco . A topical nonsteroidal anti-inflammatory agent (NSAID). Methyl salicylate lactoside is a COX inhibitor .
1-Undecanol-d4 (Undecyl alcohol-d4) is the deuterium labeled 1-Undecanol (HY-W004292). 1-Undecanol (Undecyl alcohol) is the main product generated from the degradation of 2-tridecanone by Pseudomonas bacteria isolated from the soil. 1-Undecanol can enhance the attraction of Grapholita molesta to sex pheromone traps .
5-Methoxytryptamine-d4 (O-Methylserotonin-d4) is the deuterium labeled 5-Methoxytryptamine (HY-W015169). 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .
Vortioxetine-d4 (Lu AA 21004-d4) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
Sitafloxacin-d4(DU6859a-d4) is deuterium labeled Sitafloxacin. Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection .
Taurochenodeoxycholic acid-d4 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
Veratrole-d4 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
Ramatroban-d4 is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
Arachidic acid-d4 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Adipic acid-d4 (Hexanedioic acid-d4) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Docosanoic acid-d4 (Behenic acid-4) is deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Sorafenib-d4 (Bay 43-9006-d4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
Lansoprazole sulfide-d4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacterium tuberculosis) agent with IC50 values of 0.59 μM intracellularly and 0.46 μM in broth .
4',7-Dimethoxyisoflavone-d6 (Dimethoxydaidzein-d6) is the deuterium labeled 4',7-Dimethoxyisoflavone (HY-N2145). 4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity .
Tryptophol-d4(Indole-3-ethanol-d4) is the deuterium labeled Tryptophol (HY-W010155). Tryptophol is an aromatic alcohol and secondary metabolite produced by microorganisms. Tryptophol induces apoptosis and cleavage of caspase-8. Tryptophol inhibits Cunninghamella blakesleeana biofilm. Tryptophol has anti-phage infection, biofilm formation regulation, anti-inflammatory, hemolytic, sleep induction, temperature change, seizure susceptibility and immune regulation activities. Tryptophol is used in the research of African trypanosomiasis, sleep disorders, epilepsy [4] .
Clofibric acid-d4 is the deuterium labeled Clofibric acid (HY-B1415). Clofibric acid also is an herbicideClofibric acid (Chlorofibrinic acid) is an orally active PPARα agonist. Clofibric acid inhibits the fimbriation of Escherichia coli. Clofibric acid increases SOD activity. Clofibric acid lowers blood lipids and prevents experimental pyelonephritis. Clofibric acid has anticancer activity against ovarian cancer. Clofibric acid is also a herbicide. Clofibric acid is used in ovarian cancer, liver cancer, obesity, and urinary tract infection research [4] .
Alendronate-d4 (sodium) (Alendronic acid-d4 (monosodium salt)) is deuterium labeled Alendronate sodium. Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis .
Asoxime-d4 (dichloride) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system .
N4-Acetylsulfamethoxazole-d4 is the deuterium labeled N4-Acetylsulfamethoxazole. N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of?Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections .
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease [4] .
4-Methylanisole-d3 is the deuterium labeled 4-Methylanisole . 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil .
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis .
Deruxtecan-d4 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
DPPC-d4 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in m
4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Antipyrine in the brain .
13,14-Dihydro-15-keto prostaglandin D2-d4(DK-PGD2-d4) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
Serotonin- 13C,D4(5-Hydroxytryptamine-13C,D4) is a 13C- and deuterated labeled Serotonin (HY-B1473A). Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
DSPC-d4(1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid . 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
4-Phenylbutyric acid-d11 is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid . 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research [4].
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50 s of 24 and 25 μM, respectively. 8-CPT-Cyclic AMP sodium is a very high affinity for Epac and is a potent Epac activator .
Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
Inosinic acid- 13C10, 15N4 dilithium (5'-IMP-13C10,15N4 (dilithium); IMP-13C10,15N4 (dilithium); Inosine 5'-(dihydrogen phosphate)-13C10,15N4 (dilithium)) is 13C- and 15N-labeled Inosinic acid (HY-108213). Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant, or as the dietary supplement to improve the yield and meat quality of pigs .
1,2-Dihydropyridazine-3,6-dione-3,4,5,6- 13C4 (1,2-Dihydro-3,6-pyridazine- 13C4-dione) is 13C labeled Maleic hydrazide. Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins .
Hypoxanthine- 13C5, 15N4 is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Donepezil-d4(E2020-d4 (free base)) is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Dimethyl adipate-d4 (Hexanedioic acid dimethyl ester-d4) is the deuterium labeled Dimethyl adipate (HY-W015301). Dimethyl adipate is an aliphatic dicarboxylate compound. Dimethyl adipate is mainly used as a plasticizer and an intermediate in organic synthesis.
3-Amino-2-oxazolidinone-d4(AOZ-d4) is a deuterium labeled 3-Amino-2-oxazolidinone (HY-W012982). 3-Amino-2-oxazolidinone (AOZ) is the metabolite of Furazolidone (HY-B1336). 3-Amino-2-oxazolidinone is always be detected as a indicator of furazolidone residues in vivo. 3-Amino-2-oxazolidinone is orally active .
Pitavastatin-d4-1(NK-104-d4-1) sodium is the deuterium labeled Pitavastatin sodium (HY-B0144B). Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects [4].
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Anti-cancer and anticonvulsant effects .
Melatonin-d4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties . Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation [4].
(S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX) .
Vilanterol-d4 (trifenatate) is deuterium labeled Vilanterol (trifenatate).Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research.
Folinic acid-d4-1(Leucovorin-d4-1) calcium hydrate is deuterated labeled Folinic acid (HY-17556). Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (HY-14519) as a rescue agent to decrease Methotrexate-induced toxicity.
Mono(3-carboxypropyl) phthalate-d4(MCPP-d4) is a deuterium labeled Mono(3-carboxypropyl) phthalate (HY-133673). Mono(3-carboxypropyl) phthalate (MCPP) is a metabolite of Di-n-octyl phthalate. Di-n-octyl phthalate (DnOP) is a plasticizer used in polyvinyl chloride plastics, cellulose esters, and polystyrene resins .
Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
1,4-Dibromobenzene-d4 is a deuterium labeled 1,4-Dibromobenzene. 1,4-Dibromobenzene is used as a fumigant and as a chemical intermediate for pharmaceuticals. Inhalation exposure gives rise to dizziness and chokingwhereas contact with skin or eye produces inflammation and burning in humans .
Methyl paraben-d4 is the deuterium labeled Methyl Paraben . Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity .
4-Hydroxypropranolol-d7 is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .
Pimozide-d4-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5 [4].
Indole-3-acetyl glutamate-d4(IAGlu-d4) is deuterium labeled Indole-3-acetyl glutamate. Indole-3-acetyl glutamate (IAGlu) is a derivative of the plant hormone indole-3-acetic acid (IAA). As a conjugated form of IAA, Indole-3-acetyl glutamate involves in the transport, storage, and homeostatic regulation of IAA within the plant. Indole-3-acetyl glutamate can be used for research into the effects of plant hormones on the growth and development of plants .
Triclocarban-d4 is the deuterium labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
Latanoprost ethyl amide-d4(Lat-NEt-d4) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .
Bendamustine-d4 is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
Paliperidone palmitate-d4 (9-Hydroxyrisperidone palmitate-d4) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .
4-Methylanisole-d7-1 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
4-Methylpentanoic acid-d12 is the deuterium labeled 4-Methylpentanoic acid. 4-Methylpentanoic acid (Isocaproic Acid) is a Short chain fatty acid (SCFA) .
Prostaglandin D2-d4 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals . Prostaglandin D2 is one of the most potent endogenous sleep promoting substances . PGD2 plays a protective role by suppressing inflammation .
Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Delamanid-d4-1 is deuterated labeled Delamanid.Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids .
Sacubitril-d4 hemicalcium salt is the deuterium labeled Sacubitril hemicalcium salt (HY-15407A). Sacubitril hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM [4].
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
(R)-Carvedilol-d4 is deuterium labeled (R)-Carvedilol (HY-B0006C). (R)-Carvedilol ((R)-BM 14190) is the orally active R-isomer of Carvedilol (HY-B0006). (R)-Carvedilol has α-receptor blocking activity but no β-receptor blocking activity. (R)-Carvedilol inhibits spontaneous Ca 2+ waves. (R)-Carvedilol inhibits stress-induced ventricular tachycardia and delays the development of UV-induced skin tumors and reduces their malignancy [4].
Creosol-d4(2-Methoxy-4-methylphenol-d4) is the deuterium labeled Creosol (HY-W040971). Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable .
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Dimethyl phthalate (Ring-d4) is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins .
Desloratadine-d4 hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Prostaglandin D1-d4(PGD1-d4) is deuterium labeled Prostaglandin D1. Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
4-Methyl-1-pentanol-d7 (Isohexanol-d7) is the deuterium labeled 4-Methyl-1-pentanol (HY-W007511). 4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome [4] .
1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate .
IPR-803 is a potent inhibitor of the uPAR·uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity .
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
Riboflavin- 13C4, 15N2is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Raspberry ketone-d5 (Frambione-d5; 4-(4-Hydroxyphenyl)-2-butanone-d5) is the deuterium labeled Raspberry ketone (HY-N1426). Raspberry ketone is a major aromatic compound of red raspberry, widely used as a fragrance in cosmetics and as a flavoring agent in foodstuff; also shows PPAR-α agonistic activity.
Geranylgeraniol is an orally acitve vitamin K2sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [4].
Antibacterial agent 268 (Compound 10e) is an antibacterial agent with antimycobacterial properties. Antibacterial agent 268 shows high anti-bacterial properties at sub-micromolar values (MIC=0.44-0.07 μM) .
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
DL-Arginine- 15N4,d7 hydrochloride is deuterium and 15N labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Dimethyl phthalate- 13C6,d4 (DMP- 13C6,d4) is the deuterium labeled and 13C-labeled Dimethyl phthalate (HY-N7106). Dimethyl phthalate (DMP) can be used as a plasticizer to impart flexibility to rigid polyvinyl chloride (PVC) resin. Additionally, Dimethyl phthalate is an oral active endocrine disruptor that can cause ovarian dysfunction in mice. Dimethyl phthalate can also induce oxidative stress and apoptosis in cells, thereby affecting blood and red blood cell function in rats .
Inosine-5'-diphosphate- 15N4 dilithium (IDP- 15N4 dilithium) is 15N labeled Inosine-5'-diphosphate dilithium. Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research [4].
p-Toluic acid-d4 is the deuterium labeled p-Toluic acid . p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Taurochenodeoxycholic acid-d4-1 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) sodium is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
4-Acetamidobutanoic acid-d3 is the deuterated analog of 4-Acetamidobutanoic acid (HY-101411). 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities .
Lignoceric acid-d4-2 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research .
Docosanoic acid-d4-1 (Behenic acid-d4-1) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Moxifloxacin-d4 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Pyridoxine- 13C4 (Pyridoxol- 13C4) is 13C labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
3-Methoxytyramine-d4 (hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride. 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1) .
Deruxtecan-d4-1 is the deuterium labeled Adenosine Deruxtecan (HY-13631E) . Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
L-Alanine-d4 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N-Nitrosonornicotine-d4((2S)-N'-Nitrosonornicotine-d4) is deuterium labeled N-Nitrosonornicotine. N-Nitrosonornicotine is a tobacco-specific nitrosamine that has carcinogenic and mutagenic activity, and it can induce micronuclei in C3A cells. N-Nitrosonornicotine can form DNA adducts .
Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
Docosanoic acid-d4-2 (Behenic acid-d4-2) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
DL-Lysine-4,4,5,5-d4 (dihydrochloride) is the deuterium labeled DL-Lysine. DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins .
L-Glutamine-d4 (L-Glutamic acid 5-amide-d4) is the deuterium labeled L-Glutamine (HY-N0390). L-Glutamine is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
p-Cresol sulfate-d4 (potassium) is deuterium labeled p-Cresyl sulfate (potassium). p-Cresyl sulfate potassium is a uremic toxin that binds to a prototype protein. p-Cresyl sulfate potassium activates the JNK and p38 MAPK signaling pathways. p-Cresyl sulfate potassium has pro-inflammatory activity .
Dimethyl adipate-d4-1 (Hexanedioic acid dimethyl ester-d4-1) is the deuterium labeled Dimethyl adipate (HY-W015301). Dimethyl adipate is an aliphatic dicarboxylate compound. Dimethyl adipate is mainly used as a plasticizer and an intermediate in organic synthesis.
Adipic acid-d4-1 (Hexanedioic acid-d4-1) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
3-Methyl-2-quinoxalinecarboxylic acid-d4 is the deuterium labeled 3-Methyl-2-quinoxalinecarboxylic acid. 3-Methyl-2-quinoxalinecarboxylic acid (MQCA), an important N-oxide reductive metabolite of Quinocetone or Olaquindox, potently inhibits the growth of Chang liver cells through S phase arrest of the cell cycle .
3-O-Methyltolcapone-d4 (Ro 40-7591 d4) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4] .
Monomethyl phthalate-d4 (2-(Methoxycarbonyl)benzoic acid-d4) is the deuterium labeled Monomethyl phthalate. Monomethyl phthalate is a phthalate metabolite. Monomethyl phthalate acts as a urinary biomarker of phthalates exposure and can be used as a standard for the determination of thyroid cancer and benign nodule .
Monooctyl phthalate-d4 (Mono-n-octyl phthalate-d4) is a deuterium labeled Monooctyl phthalate (HY-133671). Monooctyl phthalate (Mono-n-octyl phthalate) exhibits antimycobacterial activity with a MIC of 20 μg/mL .
SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase . SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism .
Anticancer agent 67 (Compound 13g) is an anti-cancer agent. Anticancer agent 67 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 67 is a ciprofloxacin analog .
Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog .
Clindamycin-d3 (hydrochloride) is the deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
Clindamycin (Standard) is the analytical standard of Clindamycin. This product is intended for research and analytical applications. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 μM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
(R)-3-Hydroxybutanoic acid- 13C4 sodium is a 13C labeled (R)-3-Hydroxybutanoic acid (HY-W051723). (R)-3-Hydroxybutanoic acid is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones .
Riboflavin-5-Phosphate- 13C4, 15N2-1 is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
L-Arginine- 15N4,d7 (hydrochloride) is the deuterium and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
4-[[(4-Fluorophenyl)imino]methyl]phenol-d4(4-{(E)-[(4-Fluorophenyl)imino]methyl}phenol-d4) is the deuterium labeled 4-[[(4-Fluorophenyl)imino]methyl]phenol (HY-W014178).
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38 . TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro .
Bexarotene- 13C4 (LGD1069- 13C4) is the 13C-labeled Bexarotene (HY-14171). Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
Resolvin E1-d4-1 is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production .
Ethylenediaminetetraacetic acid- 13C4 (EDTA- 13C4) is the 13C-labeled Ethylenediaminetetraacetic acid (HY-Y0682). Ethylenediaminetetraacetic acid (EDTA) is a kind of metal chelating agent (binds to bivalent and trivalent metal cations, including calcium). Ethylenediaminetetraacetic acid has antibacterial, anti-inflammatory, antioxidant, anti-hypercalcemia and anticoagulant activities. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can alleviate the liver fibrosis. Ethylenediaminetetraacetic acid can be used for coronary artery disease and neural system disease research [4] .
Coproporphyrin III- 15N4 (Zincphyrin- 15N4) is the 15N-labeled Coproporphyrin III (HY-101398). Coproporphyrin III (Zincphyrin) is a naturally occurring porphyrin derivative that is mainly found in urine .
Timonacic-d4 (1,3-Thiazolidine-4-carboxylicacid-d4) is deuterium labeled Timonacic. Timonacic (1,3-Thiazolidine-4-carboxylic acid) is a thiol antioxidant. Timonacic has anti-aging and anti-hepatotoxic effects, and it can be used to study acute illnesses and liver diseases, by inducing reversal, it is also used in research on certain cancer cases .
Mono(7-carboxy-2-methyloctyl) phthalate-d4(MCNP-d4) is the deuterium labeled Mono(7-carboxy-2-methyloctyl) phthalate (HY-133679). Mono(7-carboxy-2-methyloctyl) phthalate (MCNP) is a metabolite of Di-decyl phthalate (DDP) .
3-Hydroxybutyric acid-d4 (sodium) is the deuterium labeled 3-Hydroxybutyric acid. 3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids .
Sacubitril-13C4 (AHU-377-13C4) is a 13C-labeled version of Sacubitril (HY-15407). Sacubitril is an orally active inhibitor of neprilysin NEP (IC50=5 nM). Sacubitril is used in research on heart failure, hypertension and COVID-19 [4] .
2-Ketoglutaric acid-d4 (Alpha-Ketoglutaric acid-d4) is the deuterium labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid Sodium is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM) .
8-Isoprostaglandin E2-d4(iPE2-III-d4) is deuterium labeled 8-Isoprostaglandin E2. 8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway .
Arachidonic acid- 13C4 (Immunocytophyt- 13C4) is 13C labeled Arachidonic acid. Arachidonic acid (Immunocytophyt) is a polyunsaturated omega-6 fatty acid and a major constituent of biomembranes. Arachidonic acid also acts as the substrate for various lipid mediators, such as prostaglandins (PGs). Arachidonic acid improves cognitive response and cardiovascular function .
Estradiol valerianate-d4 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
Mono(5-carboxy-2-ethylpentyl) phthalate-d4(MECPP-d4) is a deuterium labeled Mono(5-carboxy-2-ethylpentyl) phthalate (HY-133675). Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking .
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells [4] .
N-Heptyl 4-hydroxybenzoate-d4 is the deuterium labeled N-Heptyl 4-hydroxybenzoate (HY-W150903) . N-Heptyl 4-hydroxybenzoate (p-Oxybenzoesaureheptylester) is an antimicrobial agent that inhibits S. aureus with MIC of 12.5 μg/mL. N-Heptyl 4-hydroxybenzoate also against plant pathogenic fungi, such as Alternaria brassicicola, F. solani, C. dematium and C. acutatum .
Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4(MEHHP-d4) is a deuterium labeled Mono(2-ethyl-5-hydroxyhexyl) phthalate (HY-133677). Mono(2-ethyl-5-hydroxyhexyl) phthalate (MEHHP) is an oxidative metabolite of Di(2-ethylhexyl) phthalate (DEHP). Mono(2-ethyl-5-hydroxyhexyl) phthalate may protective sperm DNA damage. Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking .
Monobenzyl phthalate-d4 is the deuterium labeled Monobenzyl phthalate. Monobenzyl phthalate (2-((Benzyloxy)carbonyl)benzoic acid) is the urinary metabolite exposuring to phthalates, such as, diethylhexyl phthalate (DEHP) .
NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor .
Clindamycin- 13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
9-Oxooctadecanedioic acid is an α,ω-dicarboxylic fatty acid monomer found in the cork suberin of Quercus suber. It contributes to the formation of the hydrophobic barrier structure in plant cell walls and may play an important role in functions such as water resistance and protection against microbial penetration .
4-(4-Fluorobenzylamino)-1-methylpiperidine-d2(N-[(4-Fluorophenyl)methyl]-1-methyl-4-piperidinamine-d2) is the deuterium labeled 4-(4-Fluorobenzylamino)-1-methylpiperidine.
NLRP3/aim2-in-2 (compound 8) is a new potent inhibitor with different species-specific effects on NLRP3 and AIM2 inflammasome dependent cell death. Its < b > IC < sub > 50 < / sub > < / b > value is 0.2392 μ M。
1-Methylpiperidin-4-ol-d4(N-Methyl-4-piperidinol-d4) is the deuterium labeled 1-Methylpiperidin-4-ol (HY-W018626). 1-Methylpiperidin-4-ol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Butyric acid-13C4 sodium (Butanoic acid-13C4 sodium) is a stable isotope labeled compound with the activity of promoting cell proliferation and regulating gene expression. Butyric acid-13C4 sodium can be used in metabolic research and compound development to help scientists gain a deeper understanding of the role of short-chain fatty acids in organisms. Butyric acid-13C4 sodium also plays an important role in nutrition and intestinal health research, especially in the regulation of probiotic function and intestinal microbiota.
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
4,4'-Sulfonyldiphenol-d8 (Bisphenol S (4,4'-Sulfonyldiphenol)-d8) is the deuterium labeled 4,4'-Sulfonyldiphenol (HY-W011927).4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
(S)-2-Aminohexanedioic acid-d4 is the deuterium labeled (S)-2-Aminohexanedioic acid. (S)-2-Aminohexanedioic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Docosanoic acid- 13C4 (Behenic acid- 13C4) is the 13C-labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in vivo .
Pseudane IX-d4(2-Nonylquinolin-4(1H)-one-d4) is deuterium labeled Pseudane IX. Pseudane IX, a compound isolated from the leaves of Ruta angustifolia, has strong anti-HCV activity with an IC50 value of 1.4 μg/mL. Pseudane IX reduces HCV RNA replication and viral protein synthesis levels .
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
L-Arginine- 15N4 (hydrochloride) is the 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis .
(Rac)-Moxifloxacin-d4 ((Rac)-BAY 12-8039-d4 (free base)) is deuterium labeled (Rac)-Moxifloxacin. (Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Octanoic acid- 13C4 is the 13C labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
rac cis-Moxifloxacin-d4 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin Hydrochloride (BAY 12-8039) is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Succinic acid- 13C4 is the 13C labeled Succinic acid . Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries .
Methyl arachidonate- 13C4 (Arachidonic acid methyl ester- 13C4) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
DL-Arginine- 13C6, 15N4,d7 hydrochloride is 13C and 15N-labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
Allantoin- 13C2, 15N4 is the 13C and 15N labeled Allantoin . Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth .
DL-Arginine- 13C6, 15N4 hydrochloride is 13C and 15N-labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
DL-α-Tocopherol acetate- 13C4,d6 is the deuterium and 13C labeled DL-α-Tocopherol acetate . DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition .
Bisphenol F- 13C12 is the 13C labeled Bisphenol F (HY-W014901). Bisphenol F is an orally active endocrine disruptor. Bisphenol F promotes ROS generation, upregulates p-AKT/p-GSK3β, and induces Apoptosis. Bisphenol F interferes with glucose metabolism, affects neurodevelopment and reproductive function. Bisphenol F reduces social novelty preference in mouse offspring. Bisphenol F can be used in bone, blood, and fat-related studies. Bisphenol F is used as a substitute for Bisphenol A (HY-18260) [4] .
Bisphenol F- 13C6 is the 13C labeled Bisphenol F (HY-W014901). Bisphenol F is an orally active endocrine disruptor. Bisphenol F promotes ROS generation, upregulates p-AKT/p-GSK3β, and induces Apoptosis. Bisphenol F interferes with glucose metabolism, affects neurodevelopment and reproductive function. Bisphenol F reduces social novelty preference in mouse offspring. Bisphenol F can be used in bone, blood, and fat-related studies. Bisphenol F is used as a substitute for Bisphenol A (HY-18260) [4] .
L-Arginine- 13C6, 15N4,d7 (hydrochloride) is the deuterium, 13C-, and 15-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
13-cis-4-Oxoretinoic acid-d6 (4-Keto 13-cis-retinoic acid-d6; 4-Oxoisotretinoin-d6; Ro 22-6595-d6) is the deuterium labeled 13-cis-4-Oxoretinoic acid (HY-107494). 13-cis-4-Oxoretinoic acid (4-Keto 13-cis-retinoic acid) is a metabolite of vitamin A in human plasma .
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
4-Hydroxy-1-(pyridin-3-yl)butan-1-one-d4(4-Hydroxy-1-(3-pyridyl)-1-butanone-d4) is the deuterium labeled 4-Hydroxy-1-(pyridin-3-yl)butan-1-one (HY-W270498).
Lactic acid-d4 (DL-Lactic acid-d4) sodium (60% in water) is the deuterium labeled Lactic acid sodium (60% in water) (HY-B2227B) . Lactic acid (DL-Lactic acid) sodium (60% w/w in water) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium (60% w/w in water) is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium (60% w/w in water) is an oncometabolite and has immune protective role of lactate in anti-tumor immunity . Lactic acid sodium (60% w/w in water) also has antimicrobial activity, which can be used as a food preservative .
Oxaloacetic acid- 13C4 is the 13C-labeled Oxaloacetic acid. Oxaloacetic acid (2-Oxosuccinic acid) is a metabolic intermediate involved in several ways, such as citric acid cycle, gluconeogenesis, the urea cycle, the glyoxylate cycle, amino acid synthesis, and fatty acid synthesis .
Isoallolithocholic acid-d4 (3β-Hydroxy-5α-cholanic acid-d4) is deuterium labeled Isoallolithocholic acid. Isoallolithocholic acid (3β-Hydroxy-5α-cholanic acid), a derivative of Lithocholic acid (HY-10219), is a T cell regulator. Isoallolithocholic acid enhances regulatory T cells (Tregs) differentiation .
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
NH2-C2-NH-Boc-d4 is the deuterium labeled NH2-C2-NH-Boc . NH2-C2-NH-Boc (PROTAC Linker 22) is a alkyl chain-based PROTAC linker can be used in the synthesis of PROTACs .
4-Trifluoromethylsalicylic acid- 13C6 is the 13C labeled 4-Trifluoromethylsalicylic acid . 4-Trifluoromethylsalicylic acid is a platelet aggregation inhibitor .
S 8849-1-d4 (free base) (Tianeptine metabolite MC5-d4) is deuterium labeled S 8849-1 (free base). S 8849-1 (free base) (Tianeptine metabolite MC5) is a Tianeptine (HY-90003) metabolite that is found in plasma. The mean elimination half-lives of S 8849-1 (free base) is 7.53 h in rats. S 8849-1 (free base) is promising for research of antidepressants .
Succinyladenosine- 13C4 (N6-Succinyl adenosine- 13C4) is the 13C-labeled Succinyladenosine (HY-113284). Succinyladenosine, the metabolic product of dephosphorylation of intracellular adenylosuccinic acid (S-AMP) by cytosolic 5-nucleotidase, is a biochemical marker of adenylosuccinase (ASL) deficiency .
17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid .
2-Nonyl-3-hydroxy-4-quinolone-d4(C9-PQS-d4) is deuterium labeled 2-Nonyl-3-hydroxy-4-quinolone. 2-nonyl-3-hydroxy-4-Quinolone (C9-PQS) is a quinolone compound produced by P. aeruginosa and other related bacterias. 2-nonyl-3-hydroxy-4-Quinolone is a quorum sensing (QS) signal molecule that controls the expression of many virulence genes as a function of cell population density .
2,5-Deoxyfructosazine- 13C4 (NSC 270912- 13C4) is the 13C-labeled 2,5-Deoxyfructosazine (HY-135078). 2,5-Deoxyfructosazine is a pyrazine derivative that can be found in cured tobacco and is used as a flavoring agent in the food and tobacco industry. Pyrazines, including 2,5-deoxyfructosazine, can be produced either by pyrolytic decomposition of natural compounds or by the reaction of sugars with alcoholic ammonia. 2,5-Deoxyfructosazine is also formed by the breakdown of D-glucosamine at neutral pH. Like glucosamine, 2,5-deoxyfructosazine has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC50=~1.25 mM).
Sacubitril- 13C4 (hemicalcium salt) is a 13C-labeled and deuterium labeled Sacubitril hemicalcium salt. Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696 .
N-(2-Iodophenyl)-4-methylbenzenesulfonamide-d4(N-Tosyl-2-iodoaniline-d4) is the deuterium labeled N-(2-Iodophenyl)-4-methylbenzenesulfonamide (HY-W024801).
4-Hydroxyestrone- 13C6 is a 13C-labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone (4-OHE1), an estrone metabolite, has strong neuroprotective effect against oxidative neurotoxicity. 4-Hydroxyestrone increases cytoplasmic translocation of p53 resulting from SIRT1-mediated deacetylation of p53. 4-Hydroxyestrone has little estrogenic activity .
Dihydrouracil- 13C4, 15N2 is the 13C and 15N labeled Dihydrouracil . Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient .
5-Fluorouracil- 13C4, 15N2 is the 13C and 15N labeled 5-Fluorouracil . 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer . 5-Fluorouracil also inhibits HIV [4].
L-Arginine- 13C6, 15N4 (hydrochloride) is the 13C- and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
MtTMPK-IN-8 (compound 27) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor. MtTMPK-IN-8 has sub-micromolar activity against mycobacteria (MICs = 0.78~9.4 μM) without significant cytotoxicity. MtTMPK-IN-8 can be used for researching tuberculosis .
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 μM. BK50164 binds to CD99 with a KD value of 1.5 μM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase .
Talaporfin- 13C4, 15N (ME2906 (free acid)- 13C4, 15N) is the 13C- and 15N-labeled Talaporfin (HY-16477A). Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
Geranylgeraniol (Standard) is the analytical standard of Geranylgeraniol. This product is intended for research and analytical applications. Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [3][4].
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitory activity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
4-(2-(5-Ethylpyridin-2-yl)ethoxy)benzaldehyde-d4(4-[2-(5-ethyl-pyridin-2-yl)-ethoxy]-benzaldehyde-d4) is the deuterium labeled 4-(2-(5-Ethylpyridin-2-yl)ethoxy)benzaldehyde (HY-W329684).
Indinavir- 13C4, 15N (MK-639 (free base)- 13C4, 15N) is 13C and 15N labeled Indinavir. Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL pro inhibitor [4].
4-Nonylphenol-d5 is the deuterium labeled 4-Nonylphenol. 4-Nonylphenol, a major degradation product of Nonylphenol ethoxylates (NPEOs), is a persistent organic pollutant with endocrine-disrupting properties and exerts estrogenic activity .
Pyruvic acid- 13C,d4 is the deuterium and 13C labeled Pyruvic acid . Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats .
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Histamine-α,α,β,β-d4 (dihydrochloride) is the deuterium labeled Histamine. Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
Pyridinium bisretinoid A2E-d4 TFA is the deuterium-labeled Pyridinium bisretinoid A2E (HY-134928). Pyridinium bisretinoid A2E (A2E)is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E mediates autophagy and the production of reactive oxygen species [4].
Azetidine-2-carboxylic acid-d4 (D,L-Azetidine-2-carboxylic acid-d4) is the deuterium labeled Azetidine-2-carboxylic acid (HY-75308). Azetidine-2-carboxylic acid is a non proteinogenic amino acid homologue of proline. Found in common beets. Azetidine-2-carboxylic acid can be misincorporated into proteins in place of proline in many species, including humans. Toxic and teratogenic agent .
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
4-Hydroxy-5-methylfuran-3(2H)-one-d3 is deuterated labeled 4-Hydroxy-5-methylfuran-3(2H)-one (HY-W012927). 4-Hydroxy-5-methylfuran-3(2H)-one (Chicory furaneol) can be used to assay oxidoreductase activity. 4-Hydroxy-5-methylfuran-3(2H)-one is a kind of biological materials or organic compounds that are widely used in life science research .
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [4].
Geranylgeraniol-d5 is the deuterium labeled Geranylgeraniol (HY-W011474). Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [4].
Antibacterial agent 182 (compound 8c) is an antibacterial agent that shows antibacterial activity against various Gram-positive bacteria, particularly against Vancomycin-resistant Enterococcus faecalis (MIC ≤0.125 μg/mL). Antibacterial agent 182 inhibits biofilm formation of Staphylococcus aureus and Pseudomonas aeruginosa at sub-MIC doses .
JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. JNK-1-IN-5 suppresses TGF-β-induced epithelial-mesenchymal transition. JNK-1-IN-5 is promising for research of anti-pulmonary fibrosis agent targeting JNK1 .
4,4'-Sulfonyldiphenol- 13C12 (Bisphenol S- 13C12) is 13C labeled 4,4'-Sulfonyldiphenol. 4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Calcitonin- 13C6, 15N4 (salmon) (Salmon calcitonin- 13C6, 15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .
MtTMPK-IN-7 (compound 26) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 47 μM. MtTMPK-IN-7 has sub-micromolar activity against mycobacteria (MICs = 2.3~4.7 μM) without significant cytotoxicity. MtTMPK-IN-7 can be used for researching tuberculosis .
MtTMPK-IN-9 (compound 28) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 48 μM. MtTMPK-IN-9 has sub-micromolar activity against mycobacteria (MICs = 6.25~9.4 μM) without significant cytotoxicity. MtTMPK-IN-9 can be used for researching tuberculosis .
Bisphenol AF- 13C12 is an isotopic label of Bisphenol AF. Bisphenol AF is used in polycarbonate plastic and epoxy resin manufacturing. Bisphenol AF can significantly increase intracellular ROS levels .
3-Hydroxybutyric acid- 13C4 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids .
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .
L-Hydroxyproline-d4 is deuterium labeled L-Hydroxyproline. L-Hydroxyproline, one of the hydroxyproline (Hyp) isomers, is a useful chiral building block in the production of many pharmaceuticals .
11-Beta-hydroxyandrostenedione-d4 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor .
L-Alanine- 13C3, 15N,d4 is the deuterium, 13C-, and 15-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
NNC 05-2090 is aGABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50sub>: 10.6 μM). NNC 05-2090 also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity .
KHK-IN-1 hydrochloride (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 hydrochloride inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 hydrochloride has potential for the study of diabetes and obesity .
4-Amino-TEMPO-d17(4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl-d17) is the deuterium labeled 4-Amino-TEMPO (HY-W002004). 4-Amino-TEMPO (4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl) is a stable nitroxide radical and N-nucleophile based on TEMPO. 4-Amino-TEMPO has superoxide dismutase-mimetic activity, can protect cells from oxidative damage, and has radioprotective effects. 4-Amino-TEMPO is widely used in fields such as biomedicine, materials science, and industrial production. 4-Amino-TEMPO can be used as a spin label to detect free radicals, an oxidation catalyst in industrial production, and an antioxidant stabilizer for polymers, among others .
L-Alanine- 15N,d4 is the deuterium and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer .
Pelargonidin chloride is an anthocyanidin and also is a scavenger of nitric oxide radical and has antioxidant activities. Pelargonidin inhibits cell viability and induces cell cycle arrest at sub-G1 phase. Pelargonidin chloride increases the mRNA and protein expression of HO-1, NQO1, Nrf2. Pelargonidin chloride improves Aβ-induced memory and learning impairment .
Cantharidic acid is a selective inhibitor for protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cell cycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
Stewart-Grubbs catalyst is an effective catalyst for the cross-metathesis of olefins with a large number of allylic substituents. In addition, ChemBeads are chemically coated glass beads that improve flowability and chemical homogeneity, making them ideal for automated solid dispensing and high-throughput experiments. Notably, the manufacture of ChemBeads does not require additional chemicals or surfactants, allowing for precise dispensing of sub-milligram amounts of catalyst.
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
Tubulin polymerization-IN-65 is a tubulin polymerisation inhibitor with a broad spectrum cytotoxic. Tubulin polymerization-IN-65 induces G2 + M cell cycle arrest .
Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4,allo-LCA-d4) is deuterium labeled Allolithocholic acid. Allolithocholic acid is a steroid acid could found in normal serum and feces. Allolithocholic acid facilitates excretion, absorption, and transport of fats and sterols in the intestine and liver .
1,2-Cyclohexylenedinitrilotetraacetic acid (Standard) is the analytical standard of 1,2-Cyclohexylenedinitrilotetraacetic acid (HY-W102714). This product is intended for research and analytical applications. 1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate .
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels .
Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
Diethyl succinate- 13C4 is the 13C labeled Diethyl succinate . Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring .
4,5,6,7-Tetrabromoisobenzofuran-1,3-dione- 13C6 (Tetrabromophthalic anhydride- 13C6) is the 13C-labeled 4,5,6,7-Tetrabromoisobenzofuran-1,3-dione (HY-W010833).
Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC .
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [4].
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
4-Acetyl-N-methylaniline-13C,d3 (1-(4-(Methylamino)phenyl)ethanone-13C,d3) is a 13C and deuterated isotope of 4-Acetyl-N-methylaniline. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL .
DNMT-IN-5 is a stable and efficient DNA methyltransferase (DNMT) inhibitor with high stability and high activity with an IC50 of 0.78 nM. DNMT-IN-5 exhibits sub-micromolar DNMT3A inhibitory activity, upregulates the expression of DNMT-targeted genes, impairs cell proliferation, and triggers a critical cell cycle arrest. DNMT-IN-5 can be used for the study of p53-depleted colorectal cancer .
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction .
Pretomanid (Standard) is the analytical standard of Pretomanid. This product is intended for research and analytical applications. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Procyanidin A3 (Cinnamtannin A3; Cinnamtannin II) is a sub class of Proanthocyanidins (HY-N0794). Proanthocyanidin are a class of polyphenolic that are widely distributed in higher plants, consisted of an electrophilic flavanyl unit. Proanthocyanidin can be used as antioxidant and anti-cancer agent. Proanthocyanidin also exhibit anti-inflammatory, cardioprotective, antibacterial and antifungal properties, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy .
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
Fibrinopeptide B, human-(Val- 13C5, 15N, Arg- 13C6, 154) TFA is the 13C- and 15N-labeled Fibrinopeptide B, human (HY-P1493). Fibrinopeptide B, human is a 14-aa peptide, released from the amino-terminus of β-chains of fibrinogen by thrombin .
4-(Bromomethyl)-2,2-dimethyl-1,3-dioxolane-d5 (5-bromomethyl-2,2-dimethyl-1,3-dioxolane-d5) is the deuterium labeled 4-(Bromomethyl)-2,2-dimethyl-1,3-dioxolane (HY-W018073).
(1R,2S,7R)-Sitafloxacin-d4 hydrochloride is deuterium labeled (1R,2S,7R)-Sitafloxacin hydrochloride (HY-B0395D). (R)-Sitafloxacin (DU-6857), a stereoisomer of Sitafloxacin (DU-6859a), is also an inhibitor of topoisomerases, with an IC50 of 0.18 μg/mL of DNA gyrase .
9α,11β-Prostaglandin F2α-d4 is a deuterated labeled 9α,11β-Prostaglandin F2α . 9α,11β-Prostaglandin F2α is an endogenous metabolite present in Urine that can be used for the research of Asthma .
β-Carotene- 13C10 (Provitamin A- 13C10) is the 13C-labeled β-Carotene (HY-N0411). β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities [4] .
Felbamate-d5 is the deuterium labeled Felbamate . Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .
DHEA-d5 (Prasterone-d5; Dehydroisoandrosterone-d5; Dehydroepiandrosterone-d5) is the deuterium labeled DHEA (HY-14650). DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
Selegiline-d5 (Deprenyl-d5) is deuterium labeled Selegiline. Selegiline (Deprenyl) is a potent, selective and irreversible inhibitor of MAO-B, with an IC50 of 51 nM. Selegiline exhibits 450-flod selectivity for MAO-B over MAO-A (IC50=23 μM). Selegiline can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .
Nirvanol-d5 (Ethylphenylhydantoin-d5) is deuterium labeled Nirvanol (HY-W012481) . Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
Selegiline-d5 (hydrochloride) (Deprenyl-d5 (hydrochloride)) is deuterium labeled Selegiline (hydrochloride). Selegiline (Deprenyl) hydrochloride is a potent, selective and irreversible inhibitor of MAO-B, with an IC50 of 51 nM. Selegiline hydrochloride exhibits 450-flod selectivity for MAO-B over MAO-A (IC50=23 μM). Selegiline hydrochloride can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .
Oxypurinol- 13C, 15N2 is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
Zidovudine-d3 is the deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Stepronin-d5 (Prostenoglycine-d5; TTPG-d5; Tiase-d5) is the deuterium labeled Stepronin (HY-A0234). Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands .
Daunorubicin- 13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor [4] .
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride . Tolterodine hydrochloride is a potent muscarinic receptor antagonist .
CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
Tetradecyltrimethylammonium-d29 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide) . Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure .
Tetradecyltrimethylammonium-d38 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide) . Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure .
Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
TDHL-d10 (Tergurid-d10; Terguride-d10; trans-Dihydrolisuride-d10) is the deuterium labeled TDHL (HY-12714). TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.
Picropodophyllin-d3 (AXL1717-d3; Picropodophyllotoxin-d3; PPP-d3) is the deuterium labeled Picropodophyllin (HY-15494). Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist .
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
Carazolol-d7 is the deuterium labeled Carazolol (HY-107327). Carazolol is a highly potent antagonist of β1/β2 adrenoceptor. Carazolol is also a potent, selective β3-adrenoceptor agonist. Carazolol can be used in the research of hypertension .
N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine . N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
Nitisinone-d3 (NTBC-d3) is deuterium labeled Nitisinone. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase(4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism [4].
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
Moricizine-d8 Hydrochloride is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period .
Demethoxycurcumin-d7 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin(Curcumin II), a major active curcuminoid, possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
Travoprost-d7 (Fluprostenol isopropyl ester-d7) is deuterium labeled Travoprost. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction [4].
4-[[(4-Fluorophenyl)imino]methyl]phenol- 13C6 (4-{(E)-[(4-Fluorophenyl)imino]methyl}phenol- 13C6) is the 13C-labeled 4-[[(4-Fluorophenyl)imino]methyl]phenol (HY-W014178).
13,14-Dihydro-15-keto Prostaglandin F2α-d4 (13,14-Dihydro-15-keto-PGF2α-d4) is a deuterated labeled 13,14-Dihydro-15-keto Prostaglandin F2α (HY-113208). 13,14-Dihydro-15-keto Prostaglandin F2α-d4 is an endogenous metabolite present in Blood that can be used for the research of Pregnancy .
D-Glucose- 13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
Zoledronic acid-d5 is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects .
Tacrolimus-d3 (FK506-d3) is deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Alpha-Estradiol-d2 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia .
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
D-Glucose-d22 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
Squalene-d6 (Super Squalene-d6) is a deuterium labeled Squalene. Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity .
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
(Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
Tapinarof-d5 (WBI-1001-d5) is deuterium labeled Tapinarof. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice .
D-Glucose-d77 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Tiagabine-d6 (NO050328-d6) is deuterium labeled Tiagabine. Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
D-Glucose-d is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Indocyanine green-d7 (Foxgreen-d7) is the deuterium labeled Indocyanine green (HY-D0711). Indocyanine green is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography .
Normetanephrine-d3 (hydrochloride) is the deuterium labeled Normetanephrine hydrochloride. Normetanephrine ((±)-Normetanephrine) hydrochloride is the O-methylated metabolite of norepinephrine (NE) .
Clomipramine-d6 (hydrochloride) is the deuterium labeled Clomipramine hydrochloride. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD) .
Vitamin D2-d6 is the deuterium labeled Vitamin D2. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D .
Sudan IV-d6 (Solvent Red 24-d6) is the deuterium labeled Sudan IV(HY-D0932). Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections [4].
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
1-Cyclohexanol-d11 is the deuterium labeled 1-Cyclohexanol (HY-Y1217). 1-Cyclohexanol (Hydroxycyclohexane) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Tucatinib-d6 (Irbinitinib-d6) is deuterium labeled Tucatinib. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM .
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
1-Cyclohexanol-d12 is the deuterium labeled 1-Cyclohexanol (HY-Y1217). 1-Cyclohexanol (Hydroxycyclohexane) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Umbelliferone-d5 (7-Hydroxycoumarin-d5) is the deuterium labeled Umbelliferone (HY-N0573 ). Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in chronic alcohol-fed rats .
Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
Aprepitant- 13C2,d2 (Major) (MK-0869- 13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
Venetoclax-d6 (ABT-199-d6) is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
5-Aminosalicylic acid-d7 (5-ASA-d7; Mesalamie-d7; Mesalazie-d7) is deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN) .
Nevirapine-d5 (BI-RG 587-d5) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM .
Cetrimonium-d9 (bromide) is the deuterium labeled Cetrimonium bromide . Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR . Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Urethane-d5 is the deuterium labeled Urethane. Urethane (Ethyl carbamate), the ethyl ester of carbamic acid, is a byproduct of fermentation found in various food products. Urethane has the ability to suppress bacterial, protozoal, sea urchin egg, and plant tissue growth in vitro .
Amisulpride-d5 is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis[4].Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
Triapine-d3 (3-AP-d3) is deuterium labeled Triapine. Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Cetrimonium-d33 bromide is the deuterium labeled Cetrimonium bromide . Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Valproic acid-d7 (sodium) is the deuterium labeled Valproic acid (sodium salt). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Cyclosporin A-d12 (Cyclosporine A-d12) is deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
Cefpodoxime proxetil-d7 (U-76-d7,252-d7; CS-807-d7) is the deuterium labeled Cefpodoxime Proxetil (HY-N7101). Cefpodoxime Proxetil is an orally active broad spectrum third-generation cephalosporin with potent antibacterial activity against both Gram-positive and Gram-negative bacteria including staphylococci, streptococci, Haemophilus influenzae, Neisseria gonorrhoeae, Escherichia coli, Klebsiella pnuemoniae, Citrobacter spp, and Proteus spp. Cefpodoxime Proxetil binds to penicillin binding proteins (PBPs), which inhibits peptidoglycan synthesis, finally results in interfering bacterial cell wall biosynthesis. Cefpodoxime Proxetil can be used against skin structure infections, acute otitis media, pharyngitis, tonsillitis, upper respiratory tract infection, urinary tract infections and sexually transmitted diseases [4] .
Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan . Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .
Elvitegravir-d6 (GS-9137-d6) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively .
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively [4]. Vemurafenib induces cell autophagy .
Erlotinib-d6 hydrochloride a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM . Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [4].
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
N,N-Dimethylglycine-d3 (Dimethylglycine-d3) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) hydrochloride, a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine hydrochloride is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine hydrochloride has antidepressant-like and surfactant effects .
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
Pipamperone-d10 (Floropipamide-d10) dihydrochloride is a deuterated Pipamperone dihydrochloride (HY-100703A). Pipamperone dihydrochloride (Floropipamide dihydrochloride) is a butyrophenone derivative and high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0). Pipamperone dihydrochloride is also a low-affinity antagonist of D2 receptor (pKi=6.7). Pipamperone dihydrochloride affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone dihydrochloride is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease [4].
Deracoxib-d3 (SC 046-d3; SC 59046-d3) is the deuterium labeled Deracoxib (HY-17509). Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas.
Guaifenesin-d3 is the deuterium labeled Guaifenesin. Guaifenesin (Guaiacol glyceryl ether), a constituent of guaiac resin from the wood of Guajacum officinale Linné, is an expectorant. Guaifenesin can alleviate cough discomfortby increasing sputum volume and decreasing its viscosity, thereby promoting effective cough .
Erlotinib-d8 (CP-358774-d8) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells [4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
Vitamin D2-d3 (Ergocalciferol-d3) is the deuterium labeled vitamin D2 (HY-76542), where the C-6 and C-19 protons are replaced by deuterium. Vitamin D2 can be produced by plants and mushrooms in the presence of sunlight .
Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Miglustat-d9 is the deuterium labeled Miglustat. Miglustat (N-Butyldeoxynojirimycin) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1) .
Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Nevirapine-d8 (BI-RG 587-d8) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM .
Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90 . Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression .
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
Benznidazole-d7 (Benznidazol-d7; Ro 07-1051-d7; Ro 71051-d7) is the deuterium labeled Benznidazole (HY-B1548). Benznidazole (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease .
Dimethoxycurcumin-d6 is the deuterium labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin is a derivative of Curcumin that has anti-inflammatory and antioxidant activities .
N,N-Dimethylglycine-d6 (Dimethylglycine-d6) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) hydrochloride, a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine hydrochloride is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine hydrochloride has antidepressant-like and surfactant effects [4].
Cortodoxone-d2 is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone) .
Delafloxacin-d5 is deuterium labeled Delafloxacin. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia .
Cortodoxone-d7 (11-Deoxycortisol-d7) is a deuterium labeled Cortodoxone (HY-77839). Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates T cell proliferation and activation .
Acoltremon-d3 (WS-12-d3) is the deuterium labeled Acoltremon (HY-108449). Acoltremon is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .
Binimetinib-d3 (MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM .
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Miglustat-d9 hydrochloride is the deuterium labeled Miglustat hydrochloride. Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1) .
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
Fulvestrant-d5 (ICI 182780-d5) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
5-Aminosalicylic Acid-d3 (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
Cromolyn-d5 (Cromoglycate-d5) is the deuterium labeled Cromolyn (HY-B1619). Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
N6-Threonylcarbamoyladenosine- 13C4, 15N (N6-(N-Threonylcarbonyl)adenosine- 13C4, 15N) is the 13C- and 15N-labeled N6-Threonylcarbamoyladenosine (HY-18398). N6 - Threonylcarbamoyladenosine is a common nucleosides, which can decorate and become tRNA .
Nortriptyline-d3 (hydrochloride) is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression .
Ligustrazine-d12 (Chuanxiongzine-d12) is deuterium labeled Ligustrazine. Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats [4].
Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production .
Diacerein-d6 is the deuterium labeled Diacerein . Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases .
Thiamphenicol-d3 is a deuterium labeled Thiamphenicol. Thiamphenicol, a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative, Gram-positive aerobic and anaerobic bacteria) .
Physcion-d3 (Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects .
Guanidine-d5 (hydrochloride) is the deuterium labeled Guanidine hydrochloride . Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins .
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
Antipyrine-d3 is the deuterium labeled Antipyrine. Antipyrine (Phenazone) is an antipyretic and analgesic. Antipyrine can be used as a probe agent for oxidative agent metabolism. Antipyrine has been widely used in assessment of hepatic oxidative capacity .
Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research [4] .
Acepromazine-d6 (maleate) (Acetopromazine-d6 (maleate)) is deuterium labeled Acepromazine (maleate). Acepromazine (Acetopromazine) maleate is a phenothiazine tranquilizer and is alpha-adrenoceptor antagonist [2.
Metamizole-d3 sodium is the deuterium labeled Metamizole sodium. Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole sodium is a cyclooxygenase-3 (COX-3) inhibitor .
Domperidone- 13C6 (R33812- 13C6) is 13C labeled Domperidone. Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation?cephalosporin antibiotic. Cephalexin kills?gram-positive?and some?gram-negative bacteria?by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of?pneumonia,?strep throat, and bacterial endocarditis, et al .
D-erythro-Sphingosine-13C2,d2 is a deuterated labeled D-erythro-Sphingosine . D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator [4] .
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
Halobetasol propionate-d5 (BMY-30056-d5) is deuterium labeled Halobetasol propionate (HY-B0878). Halobetasol propionate (BMY-30056) is a synthetic glucocorticoid corticosteroid. Halobetasol propionate exhibits anti-inflammatory, antipruritic, and vasoconstrictive properties. Halobetasol propionate can be used for the study of psoriasis .
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
Epiandrosterone-d5 (3β-Androsterone-d5; trans-Androsterone-d5; iso-Androsterone-d5) is the deuterium labeled Epiandrosterone (HY-I0352). Epiandrosterone is a steroid hormone. Epiandrosterone activates BKCa. Epiandrosterone inhibits glucose transport and insulin release. Epiandrosterone has weak androgenic activity [4].
2-Phenylethanol-d9 is the deuterium labeled 2-Phenylethanol . 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans . It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
2-Phenylethanol-d5 is the deuterium labeled 2-Phenylethanol . 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans . It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) [4] .
Hydroxytyrosol-d5 (DOPET-d5) is the deuterium labeled Hydroxytyrosol (HY-N0570). Hydroxytyrosol is a phenol found in the olive oil. Hydroxytyrosol can alleviate oxidative stress and improve mitochondrial function, thereby exerting neuroprotective effects. Hydroxytyrosol can induce cancer cells apoptosis via inducing ROS production. Hydroxytyrosol shows antibacterial and antiviral effect. Hydroxytyrosol can be used for the researches of cancer, infection, inflammation, immunology, metabolic, neurological and cardiovascular disease, such as colon cancer, diabetes, Alzheimer's Disease and atherosclerosis [4] .
Riboflavin phosphate-d3 sodium (Riboflavine phosphate-d3 sodium; Riboflavin 5'-phosphate-d3 sodium; Riboflavine 5'-phosphate-d3 sodium) is the deuterium labeled Riboflavin phosphate sodium (HY-B0964). Riboflavin phosphate sodium (FMN-Na) is a derivative of Riboflavin (vitamin B2) which is an essential nutrient for animals. Riboflavin phosphate sodium can be used for the research of progressive keratoconus, corneal ectasia and irregular astigmatism . Riboflavine phosphate sodium is a very effective NAD+-recycling agent .
Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research .
Acetylcysteine-d3 is the deuterium labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities. In addition, Acetylcysteine is the most stable form of cysteine during drug delivery and can be used in disulfidptosis studies [4] .
HTR2A antagonist 1 (Compound 15f) is a HTR2A antagonist, with an IC50 of 42.79 nM. HTR2A antagonist 1 induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells via the activation of p53/p21/caspase 3 signaling. HTR2A antagonist 1 has good liver microsomal stability. HTR2A antagonist 1 can be used for the research of colorectal cancer .
CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
L-Tryptophan- 15N2,d8 is the deuterium and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
2,2-Dimethyl-1,3-dioxolane-4-methanol- 13C3 ((2,2-Dimethyl-[1,3] dioxane-4-yl)-methanol- 13C3) is the 13C-labeled 2,2-Dimethyl-1,3-dioxolane-4-methanol (HY-Y1372).
(R)-Pyrrolidine-2-carboxylic acid-d3 is the deuterium labeled (R)-pyrrolidine-2-carboxylic acid. (R)-pyrrolidine-2-carboxylic acid is an endogenous metabolite.
Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively [4].
Lamotrigine- 13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
Citicoline-d9 (Cytidine diphosphate-choline-d9) sodium is the deuterium labeled Citicoline sodium (HY-B0739A). Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study [4].
Cefditoren Pivoxil-d3 (Cefditoren pivoxyl-d3) is deuterium labeled Cefditoren Pivoxil. Cefditoren Pivoxil (ME 1207) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren Pivoxil has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren Pivoxil can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections .
D-Alanine-d7 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Propylthiouracil-d5 is the deuterium labeled Propylthiouracil. Propylthiouracil (6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor.
Cabazitaxel-d6 is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity .
Cabazitaxel-d9 is deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .
Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
D-Alanine-d3 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Glurate-d5 (4-Acetylbutyric acid-d5; 5-Oxohexanoic acid-d5; NSC-5281-d5) is the deuterium labeled Glurate (HY-W001957). Glurate (4-Acetylbutyric acid) is an acylating agent. Glurate can be used in the development of antiviral compounds, especially those targeting retroviruses such as herpes virus and HIV. Glurate can be used in the synthesis of acyclic nucleoside derivatives and 5-hydroxyhexanoic acid .
D-Alanine-d is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR .
Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses .
N-Acetyl-5-hydroxytryptamine-d3 is the deuterium labeled N-Acetyl-5-hydroxytryptamine. N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor .
Raloxifene-d10-1 is the deuterium labeled Raloxifene . Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) is the deuterated product of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research .
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
Benzoin-d10 (DL-Benzoin-d10) is the deuterium labeled Benzoin (HY-B1550). Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
5α-Cholestan-3β-ol-d7 (Dihydrocholesterol-d7; 5α-Cholestanol-d7; NSC 18188-d7) is the deuterium labeled 5α-Cholestan-3β-ol (HY-107819). 5α-Cholestan-3β-ol is a derivitized steroid compound.
Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Cefotaxime-d3 is the deuterium labeled Cefotaxime (HY-A0088A). Cefotaxime is the β-lactamase stable cephalosporin and the third-generation cephalosporin antibiotic. Cefotaxime possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria [4] .
L-Tryptophan-d8 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
Hexadecane-d34 (n-Hexadecane-d34) is the deuterium labeled Hexadecane (HY-W099580). Hexadecane (n-Hexadecane) is a saturated hydrocarbon of alkanes or paraffins and can be used as an organic solvent. Hexadecane is a component of petroleum, belongs to hydrophobic substrates, and is a model substance for studying bacterial degradation of hydrophobic compounds .
Rifampicin-d8 (Rifampin-d8) is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Tricaprilin-d50 (Trioctanoin-d50) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
Florfenicol-d3 ((-)-Florfenicol-d3)?is the deuterium labeled Florfenicol. Florfenicol, a commonly used veterinary antibiotic, is currently indicated for bovine respiratory disease, and also used in aquaculture for the control of enteric septicemia in catfish. Florfenicol can induce early embryonic death in eggs, with an LC50 of 1.07 μg/g.
Oxaprozin-d5 is deuterium labeled Oxaprozin. Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
Pyrazinamide-d3 is deuterium labeled Pyrazinamide. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis .
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .
Aspirin-d3 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis [4] .
Salbutamol-d3 (Albuterol-d3) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease .
D-Mannitol-d8 is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Tricaprilin-d15 (Trioctanoin-d15) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
Esomeprazole-d3 potassium is deuterated labeled Esomeprazole (HY-17021). Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
L-Tryptophan-d3 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
Dexamethasone-d5 is the deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses .
Bisdemethoxycurcumin-d8 (Curcumin III-d8) is the deuterium labeled Bisdemethoxycurcumin (HY-N0007A). Bisdemethoxycucurmin (Curcumin III) is a curcuminoid compound and an inhibitor of P-glycoprotein and ferroptosis. Bisdemethoxycucurmin exhibits multiple activities such as anti-oxidation, anti-inflammation and anti-tumor.
Bisdemethoxycucurmin can be used for the research of tumors and inflammatory diseases [4] .
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine . Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .
Esomeprazole-d3 is deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
Estrone-d2 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human?DNA topoisomerase I?and?topoisomerase II?inhibitor with?IC50s of 0.8 μM and 2.67 μM, respectively.
Rifampicin-d3 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities .
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
D-Mannitol-d2 is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Piperin-d10 is deuterium labeled Piperine. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL [4].
Omadacycline-d9 (PTK 0796-d9; Amadacycline-d9) is the deuterium labeled Omadacycline (HY-14865) that can be used as the internal standard for the analysis of Omadacycline .
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
Glycochenodeoxycholic acid-d7 (sodium) is the deuterium labeled Glycochenodeoxycholic acid (sodium salt). Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) induces hepatocyte apoptosis .
Altrenogest-d5 is the deuterium labeled Altrenogest. Altrenogest (Allyltrenbolone) is a progestogen structurally related to veterinary steroid trenbolone.
Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
Stearoylethanolamide-d3 (Ceamid-d3) is deuterium labeled Stearoylethanolamide. Stearoylethanolamide is an endocannabinoid-like compound with pro-apoptotic activity .
Atomoxetine-d7 (Tomoxetine-d7) is deuterium labeled Atomoxetine. Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na + channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research .
(-)-Ketoconazole-d3 is deuterium labeled (-)-Ketoconazole. (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Sucralose-d6 is deuterium labeled Sucralose. Sucralose?(E955; Trichlorosucrose) is a?non-nutritive?artificial?sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Spermine-d20 (NSC 268508-d20) is deuterium labeled Spermine. Spermine (NSC 268508) functions directly as a free radical scabenger to protect DNA from free radical attack. Spermine has antiviral effects .
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
Oxaprozin-d10 (Oxaprozinum-d10; Wy21743-d10) is the deuterium labeled Oxaprozin (HY-B0808). Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity [4]. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
Tofacitinib-d3 (Tasocitinib-d3) is deuterium labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
Rifabutin-d7 is the deuterium labeled Rifabutin. Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.
Nicotinamide-d3 (Niacinamide-d3) is deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity [4].
Salbutamol-d9 (Albuterol-d9) acetate is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease .
Thymidine-d3 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication .
(±)-Penbutolol-d9 (hydrochloride) is a deuterium labeled (±)-Penbutolol hydrochloride. (+)-Penbutolol hydrochloride is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM .
Cefotaxime-d3 (sodium) is the deuterium labeled Cefotaxime (sodium salt). Cefotaxime sodium salt, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria [4] .
L-Tryptophan-d5 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
Rifampicin-d11 (Rifampin-d11; Rifamycin AMP-d11) is the deuterium labeled Rifampicin (HY-B0272) . Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities. Rifampicin shows anti-orthopoxvirus activity .
Mecillinam-d12 is deuterium labeled Mecillinam. Mecillinam (Amdinocillin), the β-lactam antibiotic, has a broad spectrum of activity against gram-negative organisms .
Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Salbutamol-d9 (Albuterol-d9) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease .
Guanosine-d13 (DL-Guanosine-d13) is a deuterium of Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .
Mitoxantrone-d8 (hydrochloride) (Mitozantrone-d8 (hydrochloride)) is deuterium labeled Mitoxantrone (dihydrochloride). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity [4]. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
Meldonium-d3 is the deuterated form of Meldonium. Meldonium is a cardiovascular protective agent that competitively inhibits BBOX1 and OCTN2. The IC50 value of Mildronate against human recombinant BBOX is 34-62 μM, and the EC50 value against human OCTN2 is 21 μM. Meldonium is a fatty acid oxidation inhibitor .
Cisapride-d6 (R51619-d6) is deuterium labeled Cisapride. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity [4] .
Nateglinide-d5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (?Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling .
Ritonavir-d8 is deuterated labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM.
Atomoxetine-d5 (Tomoxetine-d5) is deuterium labeled Atomoxetine. Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na + channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research .
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone . DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling .
Thymidine-d14 (DThyd-d14; NSC 21548-d14) is deuterium labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM .
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Formamide-d3 is the deuterium labeled Formamide (HY-Y0842). Formamide is an effective DNA denaturant that significantly reduces the stability of DNA in buffer solutions. Formamide can also be used as a decalcifying agent for rat cardiac cells. Additionally, formamide is widely used as a solvent or chemical raw material for ion compounds, resins, and plasticizers. [4]
D-Mannitol-d is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
Imidaprilate-d5 is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
Esomeprazole-d3 (sodium) is the deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
Pizotyline-d3 is deuterated labeled Pizotifen (HY-B0115). Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
Theophylline- 13C2,d6 (1,3-Dimethylxanthine- 13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research [4] .
D-Glucose-d12-12 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
D-Glucose-d1-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Estradiol-d3 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
D-Glucose-d-33 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Methyl acetylacetate-d3 (Acetoacetate methyl ester-d3) is a deuterium labeled Methyl acetylacetate (HY-Y1298). Methyl acetylacetate is an endogenous metabolite .
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
Liothyronine-d3 is deuterated labeled Liothyronine (HY-A0070A). Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively .
Vincristine-d3 (sulfate)is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM .
Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
Vincristine-d6 (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
D-Glucose-d2-1 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidinesynthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs .
Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [4] .
Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
Doxifluridine-d2 is the deuterium labeled Doxifluridine . Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
Estradiol-d2 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
Vincristine-d3-ester (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM .
D-Glucose-d2-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
D-Glucose-d-11 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
Verapamil-d3 ((±)-Verapamil-d3) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
Adenosine-d13 (Adenine riboside-d13; D-Adenosine-d13) is deuterium labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
Duloxetine-d3 (hydrochloride) is a deuterium labeled Duloxetine hydrochloride. Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
Entecavir-d2 is the deuterium labeled Entecavir. Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
D-Sorbitol-d8 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement .
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
(±)-Leucine-d10 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08% .
Neohesperidin Dihydrochalcone-d3 (Neohesperidin DC-d3; NHDC-d3) is the deuterium labeled Neohesperidin dihydrochalcone (HY-N0154). Neohesperidin dihydrochalcone is a synthetic glycoside chalcone, is added to various foods and beverages as a low caloric artificial sweetener.
L-Carnitine-d9 (chloride)e is the deuterium labeled L-Carnitine chloride. L-Carnitine chloride, a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine chloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine chloride is an antioxidant. L-Carnitine chloride can ameliorate metabolic imbalances in many inborn errors of metabolism .
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Azeliragon-d9 (TTP488-d9) is the deuterium labeled Azeliragon (HY-50682). Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression with mild Alzheimer’s disease (AD) . Azeliragon also can cross the blood-brain barrier (BBB) .
Amantadine-d15 is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent .
L-Serine-d3 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Pantoprazole-d8 (BY1023-d8) sodium is a deuterium labeled Pantoprazole (HY-17507). Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Iopamidol-d3 (B-15000-d3; SQ-13396-d3) is the deuterium labeled Iopamidol (HY-B0684). Iopamidol is a nonionic, X-Ray iodinated contrast agent (CA) for a wide variety of diagnostic applications. Iopamidol contains amide and hydroxyl functionalities that can be exploited for the generation of the chemical exchange saturation transfer (CEST) contrast .
Dalbavancin-d6 is the deuterium labeled Dalbavancin . Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively .
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy [4] .
Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
Mifepristone-d3 is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
Levosulpiride-d3 is the deuterium labeled Levosulpiride. Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class .
Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Tulathromycin A-d7 (Tulathromycin-d7) is deuterium labeled Tulathromycin A. Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 μM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects [4].
Molindone-d8 is the deuterium labeled Molindone. Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses .
Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
Etoricoxib-d3 is the deuterium labeled Etoricoxib . Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood [4].
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect .
Mirtazapine-d3 is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors .
Febuxostat-d3 (TEI 6720-d3) is deuterium labeled Febuxostat. Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout .
Amantadine-d6 is the deuterium labeled Amantadine . Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research [4] .
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Fluralaner-d3 (A1443-d3) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
(±)-Leucine-d7 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08% .
Lifitegrast-d6 (SAR 1118-d6) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Levodropropizine-d8 is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
Docosahexaenoic acid-d5 is the deuterium labeled Docosahexaenoic Acid. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
Dioxybenzone-d3 is deuterium labeled Dioxybenzone. Dioxybenzone (Benzophenone-8; UV-24) is an organic compound used to block UVB and short-wave UVA (ultraviolet) radiation. Dioxybenzone has orally activity. Dioxybenzone exhibits estrogenic disrupting effect. Dioxybenzone up-regulates inflammatory cytokines. Dioxybenzone can be used for cancer, reproductive system disease and inflammatory disease study [4].
Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
Cyclopropylcarboxylic acid-d5 (Carboxycyclopropane-d5) is a deuterium labeled Cyclopropylcarboxylic acid (HY-Y0001). Cyclopropylcarboxylic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Irbesartan-d7 is deuterated labeled Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM .
Fluralaner-d2 (A1443-d2) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Secnidazole-d3 (RP-14539-d3; PM-185184-d3) is the deuterium labeled Secnidazole (HY-B1118). Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Pantoprazole-d8 (BY1023-d8) is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
N-Benzylaniline-d2 (N-Phenylbenzylamine-d2) is the deuterium labeled N-Benzylaniline (HY-W016321). N-Benzylaniline is an N-alkyl-ated derivative of aniline .
Metopimazine-d6 (EXP999-d6; RP9965-d6) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks [4].
Molnupiravir-d7 is the deuterium labeled Molnupiravir. Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza .
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively .
Octacosane-d58 is the deuterium labeled Octacosane . Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l [4].
Fexofenadine-d10 (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years) .
Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .
Pocapavir-d3 (SCH-48973-d3; V-073-d3) is the deuterium labeled Pocapavir (HY-104074) . Pocapavir (SCH-48973) is an orally active capsid inhibitor. Pocapavir prevents virion uncoating upon entry into the cell. Pocapavir has antiviral activity against polioviruses. Pocapavir also inhibits enterovirus infections .
D-Sorbitol-d2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Pergolide-d7 (mesylate) is the deuterium labeled Pergolide mesylate. Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research .
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research .
Revefenacin-d9 (TD-4208-d9) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Revefenacin-d3 (TD-4208-d3) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Ondansetron-d6 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride . Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy [4] .
Chlorambucil-d8 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease [4].
Olaparib-d5 (AZD2281-d5) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [4].
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay [4] . Boceprevir inhibits SARS-CoV-2 3CLpro activity .
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
Fexofenadine-d3 is the deuterium labeled Fexofenadine . Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research [4].
Adenosine-d9 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio .
Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively .
Phenylglyoxylic acid-d5 (Benzoylformic acid-d5) sodium is the deuterium labeled Phenylglyoxylic acid sodium (HY-W010255A). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human. Phenylglyoxylic acid can be used as drug intermediate for synthesis of antineoplastic compounds .
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo [4].
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
Fluralaner-d5 (A1443-d5) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels .
Mavacamten-d7 (MYK461-d7) is deuterium labeled Mavacamten. Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Naftopidil-d7 (KT-611-d7 ) is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Elobixibat-d5 is the deuterium labeled Elobixibat (HY-15790). Elobixibat (A 3309; AZD 7806) is orally active, bile acid transporter (IBAT) inhibitor with IC50 values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to treat metabolic syndrome. Elobixibat can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly [4].
Dacomitinib-d10 dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
Cephalexin-d5 (monohydrate) is the deuterium labeled Cephalexin monohydrate. Cephalexin monohydrate is a potent, orally active and the first-generation?cephalosporin antibiotic. Cephalexin monohydrate kills?gram-positive?and some?gram-negative bacteria?by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of?pneumonia,?strep throat, and bacterial endocarditis, et al .
Tivozanib-d6 (AV-951-d6) is deuterium labeled Tivozanib. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors .
Brequinar-d3 (DUP785-d3) is deuterium labeled Brequinar. Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity .
Midostaurin-d5 (PKC412-d5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM .
Actinine-d9 chloride is the deuterium labeled Actinine chloride. Actinine chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat .
6-Mercaptopurine-d2 is the deuterium labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent .
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
Verapamil-d6 ((±)-Verapamil-d6) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
Cyclamic acid-d11 (Sodium cyclamate-d11) sodiumis deuterium labeled Cyclamic acid (sodium). Cyclamic acid sodium (Sodium cyclamate) is a commonly used sweetener. Cyclamic acid sodium is toxic to osteoblasts and can inhibit cell proliferation, induce apoptosis and reduce cell mineralization. Cyclamic acid sodium causes focal necrosis of bladder organs in rats in vitro, which can promote bladder cancer, but some studies have shown that low doses of Cyclamic acid sodium have no carcinogenic effect. In addition, Cyclamic acid sodium has no effect on insulin and glucagon secretion induced by arginine [4] .
Undecanoic acid-d2 (Undecanoate-d2) is the deuterium labeled Undecanoic acid (HY-W004282). Undecanoic acid is a monocarboxylic acid with antifungal property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Aldox-d6 (Lexamine M-13-d6; MAPD-d6) is the deuterium labeled Myristamidopropyl dimethylamine (HY-W099582). Myristamidopropyl dimethylamine (MAPD) is an antimicrobial agent (including against bacteria and fungi) and an insecticide, exhibiting inhibitory activity against Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Fusarium solani, and Acanthamoeba polyphaga. Myristamidopropyl dimethylamine can be used in research on microbial-induced keratitis .
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive . Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Lubiprostone-d7 (RU-0211-d7) is the deuterium labeled Lubiprostone. Lubiprostone (SPI-0211) increases intestinal fluid secretion through generation of CIC-2/CFTR and activation of cAMP signaling pathway. Lubiprostone inhibits myeloperoxidase (MPO) activity, downregulates Indomethacin (HY-14397)-induced iNOS and TNFα expression. Lubiprostone can be used for chronic constipation research .
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
Duloxetine-d7 hydrochloride ((S)-Duloxetine-d7 hydrochloride) is the deuterium labeled Duloxetine hydrochloride (HY-B0161A). Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
N-Desmethyl clomipramine-d7 (Desmethylclomipramine-d7) is deuterium labeled N-Desmethyl clomipramine. Desmethylclomipramine (Norclomipramine) is a metabolite of Clomipramine (HY-B0457A) and can be used for neurological research .
Cefetamet-d3 (Ro 15-8074-d3; Deacetoxycefotaxime-d3) is the deuterium labeled Cefetamet (HY-A0111). Cefetamet (Ro 15-8074) is a cephalosporin antibiotic and the active metabolite of Cefetamet pivoxil (HY-B1894A). Cefetamet binds to bacterial penicillin-binding protein (PBP) (IC50 for PBP3 in Escherichia coli W3110 is 2.5 μg/mL). Cefetamet has significant activity against Gram-negative bacteria such as Enterobacteriaceae, Neisseria species, and Haemophilus influenzae, as well as Gram-positive bacteria such as Streptococcus. Cefetamet kills and lyses Treponema pallidum. Cefetamet can be used in the research of respiratory tract, urinary tract, ear, nose and throat infections, and syphilis [4] .
Oleanolic acid-d3 is the deuterium labeled Oleanolic Acid . Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities .
Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Resiquimod-d5 is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α .
Citronellol-d6 is deuterated labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis [4] .
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy [4] .
Levodropropizine-d5 ((S)-(-)-Dropropizine-d5) is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
Fusidic acid-d6 is the deuterium labeled Fusidic acid. Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome .
Beraprost-d3 (TRK-100-d3) is deuterium labeled (Rac)-Beraprost. (Rac)-Beraprost ((Rac)-ML 1229) is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
L-Serine-d2 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively .
Irbesartan-d7 hydrochloride is deuterated labeled Irbesartan hydrochloride (HY-B0202A). Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Pregnanediol-d5 is the deuterium labeled Pregnanediol. Pregnanediol is the major metabolite of progesterone and can be excreted via urine. Pregnanediol offers an indirect way to measure progesterone levels in vivo .
Rucaparib-d8 (AG014699-d8 ) is deuterium labeled Rucaparib. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research [4].
Danegaptide-d5 (GAP-134-d5) is deuterium labeled Danegaptide. Danegaptide (GAP-134) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect .
Belumosudil-d7 (KD025-d7) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
Febuxostat-d5 (TEI 6720-d5) is deuterium labeled Febuxostat. Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout .
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
Cibenzoline-d5 (Cifenline-d5) is deuterium labeled Cibenzoline. Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a KATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC50 of 22.2 μM. Cibenzoline inhibits IKr and IKs currents with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia [4].
S-(+)-Ketoprofen-d3 ((S)-Ketoprofen-d3) is deuterium labeled S-(+)-Ketoprofen. S-(+)-Ketoprofen is a potent inhibitor of both COX-1 and COX-2 with IC50s of 1.9 and 27 nM, respectively.
Sparfloxacin-d5 is deuterium labeled Sparfloxacin (HY-B0308). Sparfloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity .
Methylmalonic acid-d3 is the deuterium labeled Methylmalonic acid. Methylmalonic acid (Methylmalonate) is an indicator of Vitamin B-12 deficiency in cancer .
Olaparib-d8 (AZD2281-d8) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [4].
Lamotrigine-d3 is the deuterium labeled Lamotrigine . Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors .Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Verapamil-d6 (CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride . Pyridoxine hydrochloride (Pyridoxol;Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol;Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway .
Brincidofovir-d6 (CMX001-d6) is the deuterium labeled Brincidofovir (HY-14532). Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. [4].
Verapamil-d7 is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
Pyridoxine-d2 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Safinamide-d5 (FCE 26743-d5) is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Undecanoic acid-d3 (Undecanoate-d3) is the deuterium labeled Undecanoic acid (HY-W004282). Undecanoic acid is a monocarboxylic acid with antifungal property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Albendazole sulfoxide-d7 is the deuterium labeled Albendazole sulfoxide. Albendazole sulfoxide (Ricobendazole), the main active metabolite of Albendazole, exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes .
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor .
Undecanoic acid-d21 (Undecanoate-d21) is the deuterium labeled Undecanoic acid (HY-W004282). Undecanoic acid is a monocarboxylic acid with antifungal property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Aficamten-d3 (CK-274-d3) is deuterium labeled Aficamten. Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM) .
Dorzolamide-d3 hydrochloride is deuterated labeled Dorzolamide hydrochloride (HY-B0109A). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
L-Serine-d7 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
N-Desmethyl clomipramine-d6 (Desmethylclomipramine-d6) is deuterium labeled N-Desmethyl clomipramine. Desmethylclomipramine (Norclomipramine) is a metabolite of Clomipramine (HY-B0457A) and can be used for neurological research .
Pyridoxine-d3 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
Orlistat-d3 is a deuterated labeled Orlistat . Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity .?Anti-atherosclerotic?effect .
Diatrizoic acid-d6 (Diatrizoate-d6; Amidotrizoic acid-d6) is the deuterium labeled Diatrizoic acid (HY-B0926). Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium .
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
L-Carnitine-d9 is the deuterium labeled L-Carnitine. L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism .
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Mavacamten-d5 (MYK461-d5; SAR439152-d5) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma .
Baloxavir-d5 is deuterium labeled Baloxavir. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity .
Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
Quizartinib-d8 (AC220-d8) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
Ribavirin- 15N, d2 is 15N and deuterated labeled Ribavirin (HY-B0434). Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.
Tildacerfont-d8 (SPR001-d8) is a deuterium labeled Tildacerfont (HY-113603). Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia .
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
2'-Deoxycytidine-5'-monophosphoric acid- 15N3,d12 dilithium is deuterium and 15N labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator [4].
Ibudilast-d7-1 is the deuterium labeled Ibudilast . Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia .
Crystal Violet-d6 is the deuterium labeled Crystal Violet (HY-B0324A). Crystal Violet, also known as Gentian violet, methyl violet 10B, is a triphenyl-methane, an alkaline dye that binds to DNA in the nucleus of a cell, staining it a deep purple. It is often used for Gram staining to classify bacteria, or for cell or histological staining .
Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway [4].
Hexacosanoic acid methyl ester-d3 (C26:0 methyl ester-d3) is deuterium labeled Methyl hexacosanoate. Methyl hexacosanoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
C6 Ceramide- 13C2,d2 (C6-Cer- 13C2,d2) is the deuterium labeled and 13C-labeled C6 Ceramide (HY-19542). C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects [4] .
N-(1-(Adamantan-1-yl)ethyl)hydroxylamine-d4(N-(1-((3r,5r,7r)-Adamantan-1-yl)ethyl)hydroxylamine-d4) is the deuterium labeled N-(1-(adamantan-1-yl)ethyl)hydroxylamine (HY-75864).
MNI-caged kainate is a photoprotected neuroactive amino acid with the activity to generate large inward currents. MNI-caged kainate can be released at the resting membrane potential of Purkinje cells and generate significant inward currents. The release of MNI-caged kainate results in approximately 40% of the current being generated through AMPA receptor activation. MNI-caged kainate is used to study fast synaptic receptor mechanisms. The photorelease time of MNI-caged kainate is in the sub-microsecond range, making it suitable for investigating the mechanisms of fast synaptic transmission .
Zoledronic acid- 15N2, 13C2 (CGP 42446- 15N2, 13C2) is the 13C- and 15N-labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects .
Cladribine- 13C5, 15N2 (2-Chloro-2′-deoxyadenosine- 13C5, 15N2) is 13C and 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis .
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
(S)-Malic acid-d3 is the deuterium labeled (S)-Malic acid. (S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a dicarboxylic acid in naturally occurring form, contributes to the pleasantly sour taste of fruits and is used as a food additive .
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia .
Cisapride- 13C,d3 (R 51619- 13C,d3) is the deuteriumand 13C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity [4].
Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
Omeprazole metabolite Omeprazole sulfone-d3 is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Deoxycholic acid-d6 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
Betulinic acid-d3 (Lupatic acid-d3) is a deuterium labeled Betulinic acid (HY-10529). Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties [4].
Ethyl linoleate-d2 (Linoleic Acid ethyl ester-d2; Mandenol-d2) is the deuterium labeled Ethyl linoleate (HY-W013812). Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Malic acid-d3 is the deuterium labeled Malic acid. Malic acid (Hydroxybutanedioic acid) is a dicarboxylic acid that is naturally found in fruits such as apples and pears. It plays a role in many sour or tart foods .
Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
Labetalol hydrochloride-d6 (AH-5158 hydrochloride-d6) is deuterium labeled Labetalol hydrochloride (HY-B1108). Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy [4].
Vinorelbine-d3 (ditartrate) is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
Butylphthalide-d3 is the deuterium labeled Butylphthalide. Butylphthalide(3-n-Butylphthalide), an anti-cerebral-ischemia agent, is first isolated from the seeds of celery and showes efficacy in animal models of stroke.
Herniarin-d3 is the deuterium labeled Herniarin (HY-N1366). Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
Rivastigmine-d3 hydrochloride is deuterated labeled Rivastigmine (HY-17368). Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
Prostaglandin E1-d9 is deuterium labeled Prostaglandin E1.Prostaglandin E1 is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inh
Thiamine-d3 (hydrochloride) is the deuterium labeled Thiamine hydrochloride. Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
Ethyl linoleate-d11 (Linoleic Acid ethyl ester-d11) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Alvimopan-d7 (ADL 8-2698-d7) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
2'-Hydroxyacetophenone-d7 (o-Hydroxyacetophenone-d7; o-Acetylphenol-d7) is the deuterium labeled 2'-Hydroxyacetophenone (HY-Y1426). 2'-Hydroxyacetophenone is found in alcoholic beverages. 2'-Hydroxyacetophenone is present in tomato, cassia, fried beef, rum, whiskey, cocoa, coffee and black tea. 2'-Hydroxyacetophenone is a flavouring ingredient. Building block in chemical synthesis.
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research [4] .
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity .
Prostaglandin E2-d9 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
Phenylacetylglutamine-d5 (NSC 203800-d5) is the deuterium labeled Phenylacetylglutamine (HY-W050026). Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation .
Ethylparaben-d5 (Ethyl parahydroxybenzoate-d5) is deuterium labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Cabotegravir-d3 (sodium) is the deuterium labeled Cabotegravir sodium. Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltr
Enrofloxacin-d5 is the deuterium labeled Enrofloxacin. Enrofloxacin (BAY Vp 2674) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Valproic acid-d15 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity .
PF-06380101-d8 (Aur0101-d8) is a deuterium labeled PF-06380101 (HY-12522). PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue .
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease .
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor . Antianginal agent.
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice [4].
Dimebutic acid-d6 (NSC-16045-d6; NSC-741804-d6) is the deuterium labeled Dimebutic acid (HY-W015881). Dimebutic acid is a fatty acid derivative. Dimebutic acid is an orally active short-chain fatty acid. Dimebutic acid stimulates fetal globin production and alters the balance of Bcl family proteins. Dimebutic acid prolongs red blood cell survival. Dimebutic acid exhibits toxicity in rats. Dimebutic acid is used in the study of β-thalassemia and sickle cell disease .
Topotecan-d5 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87 .
Tamsulosin-d5 (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .
N-Acetylglycine-d2 (Aceturic acid-d2) is the deuterated labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity .
Chloroxylenol-d6 is the deuterium labeled Chloroxylenol. Chloroxylenol is a broad spectrum antimicrobial chemical compound used to control bacteria, algae, fungi and virus.
Adenine-d is the deuterium labeled Adenine. Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis .
Taurocholic acid-d8 (sodium) is deuterium labeled Taurocholic acid (sodium). Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect .
Butylphthalide-d9 (3-n-Butylphthalide-d9) is deuterium labeled Butylphthalide. Butylphthalide (3-n-Butylphthalide) is an active molecule against cerebral ischemia. It was originally isolated from celery species and has been shown to be effective in stroke animal models .
Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Digitoxigenin-21,23,23-d3 (Cerberigenin-d3; Echujetin-d3) is the deuterium labeled Digitoxigenin (HY-B2151). Digitoxigenin is a steroid derivative commonly found in various plants, especially the foxglove plant (Digitalis purpurea). Digitoxigenin has unique chemical properties that make it an important precursor for the synthesis of cardiac glycosides, a group of drugs used to improve heart failure and certain types of arrhythmias. It works by inhibiting the sodium potassium ATPase pump, thereby increasing the force and efficiency of cardiac contractions.
Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs . Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs) .
Dexamethasone acetate-d5 (Dexamethasone 21-acetate-d5; Hexadecadrol acetate-d5) is the deuterium labeled Dexamethasone acetate (HY-14648A). Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively [4].
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
N-Acetylglycine-d5 (Aceturic acid-d5) is the deuterium labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
Enrofloxacin-d5 (hydrochloride) is deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Thiabendazole-d6 is a deuterated labeled Thiabendazole (HY-B0263). Thiabendazole is an orally available benzimidazole fungicide with repellent and anticancer activities. Thiabendazole can result in developmental malformations. Thiabendazole can be used for modeling [4] .
3-Methylanisole-d3 is the deuterium labeled 3-Methylanisole (HY-115127) .3-Methylanisole is an intermediate in drug synthesis, which has antiseptic, antibacterial and protein stabilizing effects .
Ulipristal-d3 (CDB-3236-d3) is deuterium labeled Ulipristal. Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system .
Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
Lomefloxacin-d5 (hydrochloride) is the deuterium labeled Lomefloxacin hydrochloride. Lomefloxacin (SC47111A) hydrochloride is a broad-spectrum quinolone antibiotic, with antimicrobial activity. Lomefloxacin hydrochloride is used for the research of respiratory tract infections, genitourinary infections, gastrointestinal infections, ENT infections, etc. .
Vildagliptin-d6 (LAF237-d6 ) is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
Riboflavin-d3 is the deuterium labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases [4] .
N-Desmethylolanzapine-d8 hydrochloride (N-Demethylolanzapine-d8 hydrochloride) is the deuterium labeled N-Desmethylolanzapine (HY-W009247). N-Desmethylolanzapine is an antipsychotic drug. The formation of N-Desmethylolanzapine correlates with the level and activity of human liver flavin-containing monooxygenase (FMO3). N-Desmethylolanzapine can be used in the study of antipsychotic drugs .
Riboflavin-d8 (Vitamin B2-d8 ) is deuterium labeled Riboflavin. Riboflavin, an orally active and easily absorbed micronutrient, is a precursor of flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD), which serve as coenzymes for numerous enzymatic reactions and perform key metabolic functions by mediating the transfer of electrons in biological oxidation-reduction reaction .
N-Desmethyl Clomipramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine
Thiamphenicol-d3-1 (Thiophenicol-d3-1; Dextrosulphenidol-d3-1) is the deuterium-labeled Thiamphenicol (HY-B0479) . Thiamphenicol (Thiophenicol)，a methyl-sulfonyl derivative of Chloramphenicol，is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit，leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative，Gram-positive aerobic and anaerobic bacteria) .
Propylparaben-d7 (Propyl parahydroxybenzoate-d7) is the deuterium labeled Propylparaben (HY-N2026) . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats [4].
Sofosbuvir-d6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Taurine- 15N (2-Aminoethanesulfonic acid- 15N) is 15N labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
Cytidine-5'-triphosphate- 15N3,d14 (Cytidine triphosphate- 15N3,d14 dilithium; 5'-CTP- 15N3,d14) dilithium is deuterium and 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
Thymidine- 13C10, 15N2 is the 13C and 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Deoxycytidine triphosphate- 15N3,d14 (dCTP- 15N3,d14 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3,d14) dilithium is deuterium and 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
(±)-1,2-Propanediol-d2 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
(±)-1,2-Propanediol-d8 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) methylbenzenesulfonate is the deuterium labeled S-Adenosyl-L-methionine methylbenzenesulfonate . S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research [4].
Menaquinone-7-d7 is the deuterium labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors . Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS) .
Naloxegol- 13C,d2 (NKTR-118- 13C,d2) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
6-Aminocaproic acid-d10 hydrochloride (EACA-d10 hydrochloride; Epsilon-Amino-n-caproic Acid-d10 hydrochloride; 6-Aminohexanoic acid-d10 hydrochloride) is the deuterium labeled 6-Aminocaproic acid hydrochloride (HY-B0236A). 6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
Hydrocinnamic acid-d9 is the deuterium labeled Hydrocinnamic acid . Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activitie s.
Naloxegol- 13C,d3 (NKTR-118- 13C,d3) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
Hydrocinnamic acid-d5 is the deuterium labeled Hydrocinnamic acid . Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities .
(±)-1,2-Propanediol-d6 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
L-Tryptophan- 13C11, 15N2 is the 13C- and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
5'-Guanylic acid- 15N5,d12 (5'-GMP- 15N5,d12 dilithium; 5'-guanosine monophosphate- 15N5,d12) dilithium is deuterium and 15N labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Kevetrin (hydrochloride)- 13C2, 15N3 is the 13C-labeled and 15N-labeled Kevetrin (hydrochloride). Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
Guanosine- 13C10, 15N5 is the 13C and 15N labeled Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Cytidine 5′-monophosphate- 15N3,d12 (5'-Cytidylic acid- 15N3,d12 dilithium; 5'-CMP- 15N3,d12) dilithium is deuterium and 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects .
Coenzyme Q10-d9 is the deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Diethyltoluamide-d7 is the deuterium labeled Diethyltoluamide . Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects .
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
(22R)-Budesonide-d6 (Dexbudesonide-d6) is deuterium labeled (22R)-Budesonide. (22R)-Budesonide ((22R)-BUD) is the (22R)-enantiomer of Budesonide (HY-13580). (22R)-Budesonide is a non-halogenated glucocorticoid with high local anti-inflammatory activity .
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Triacetin-d5 is the deuterium labeled Triacetin. Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Dorzolamide-d5(hydrochloride) (L671152 hydrochloride-d5) is deuterium labeled Dorzolamide (hydrochloride). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
N-Desmethyl Sildenafil-d8 is the deuterium labeled N-Desmethyl Sildenafil (HY-117605). N-Desmethyl Sildenafil is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor .
Levocarnitine propionate-d5 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
N6-Methyladenosine-d3 (6-Methyladenosine-d3; N-Methyladenosine-d3) is a deuterium labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
rel-Ritonavir-d6 (rel-ABT 538-d6) is the deuterium labeled rel-Ritonavir. rel-Ritonavir is a relative configuration of Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to study of HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
2-Linoleoyl glycerol-d5 (2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
Glyceryl Triacetate-d9 is the deuterium labeled Triacetin . Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Dexamethasone-d3-1 (Hexadecadrol-d3-1; Prednisolone F-d3-1) is a deuterium labeled Dexamethasone (HY-14648). Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Levocarnitine propionate-d3 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa [4] .
Ethyl phenylglyoxylate-d5 (Ethyl benzoylformate-d5; Phenylglyoxylic acid ethyl ester-d5) is the deuterium labeled Ethyl phenylglyoxylate (HY-W016618). Ethyl phenylglyoxylate (Ethyl benzoylformate), the ethyl ester of phenylglyoxylic acid, is used as a synthetic reagent. Ethyl phenylglyoxylate is also a poor substrate but a potent inhibitor of chicken liver carboxylesterase. Additionally, Ethyl phenylglyoxylate exhibits photoreactivity, where its excited triplet carbonyl can initiate intermolecular hydrogen abstraction, radical coupling and cross-linking reactions .
17α-Hydroxyprogesterone-d8 is the deuterium labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
N-Methylpyrrolidone-d9 (NMP-d9) is deuterium labeled N-Methylpyrrolidone. N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an orally active organic polar solvent with teratogenicity and toxicity. N-Methylpyrrolidone is low in acute toxicity with a LD50 value of 3914 mg/kg in rats and of 4050 mg/kg in mice. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals [4].
Folic acid-d2 (Vitamin B9-d2) is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
N-Methylpyrrolidone-d3 is the deuterium labeled N-Methylpyrrolidone . N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an organic polar solvent. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals .
N,N'-Dinitrosopiperazine-d8 is the deuterium labeled N,N'-Dinitrosopiperazine . N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568 .
Tolterodine tartrate-d14 (Kabi-2234-d14) is deuterium labeled Tolterodine (tartrate). Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine. Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease [4].
Diethyltoluamide-d10 is the deuterium labeled Diethyltoluamide . Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects .
Acetyl tributyl citrate-d33 is the deuterium labeled Acetyl tributyl citrate (HY-W010981). Acetyl tributyl citrate (Tributyl O-acetylcitrate; ATBC) is an alternative plasticizer .
Mitotane-d8 is the deuterium labeled Mitotane . Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [4] .
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Ganciclovir-d5 is the deuterium labeled Ganciclovir. Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) .
13-cis Acitretin-d3 is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis .
Loratadine-d5-1 is a deuterated labeled Loratadine (HY-17043). Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
L-5-Hydroxytryptophan-d3 is the deuterium labeled L-5-Hydroxytryptophan. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [4] .
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats [4].
Citalopram-d3 ((±)-Citalopram-d3) hydrobromide is deuterium labeled Citalopram (hydrobromide). Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
Dexamethasone-d5-1 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
13C20, 15N10-Cyclic di-GMP ( 13C20, 15N10-c-di-GMP) is 13C and 15N labeled Cyclic-di-GMP (disodium). Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research [4] .
Tazobactam- 15N,d2 (CL-298741- 15N,d2) is 15N and deuterium labeled Tazobactam. Tazobactam (CL-298741) is a potent β-lactamases inhibitor and penicillin antibiotic. Tazobactam has antibacterial activity. Tazobactam can be used for pneumonia research .
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells [4].
Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
Uridine triphosphate- 13C9, 15N2 (UTP- 13C9, 15N2) sodium is a labeled Uridine triphosphate sodium. Uridine triphosphate sodium can be used in nucleic acid synthesis.
Adenine- 13C5,15C5 (6-Aminopurine- 13C5,15C5; Vitamin B4- 13C5,15C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Clascoterone-d5 (Cortexolone 17 alpha-propionate-d5) is the deuterated analog of Clascoterone. Clascoterone is a topical and peripheral androgen antagonist .
(-)-Epicatechin- 13C3 ((-)-Epicatechol- 13C3) is 13C labeled (-)-Epicatechin. (-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.
Chlophedianol- 13C6 is the 13C labeled Chlophedianol (HY-A0161). Chlophedianol is an orally active and potent antitussive agent. Chlophedianol can be used for the research of acute cough due to upper respiratory tract infections (URIs) .
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
Maribavir-d6 TFA (1263W94-d6 TFA; BW1263W94-d6 TFA; GW257406X-d6 TFA) is a deuterium labeled Maribavir (HY-16305). Maribavir is an orally active antiviral agent for cytomegalovirus (CMV) through inhibition of protein kinase UL97 and the following CMV DNA replication .
L-Asparagine- 15N2 monohydrate is the 15N-labeled L-Asparagine monohydrate (HY-W017443). L-Asparagine monohydrate is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine monohydrate can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia [4] .
Acetyl-L-carnitine-d9 (O-Acetyl-L-carnitine-d9) is deuterium labeled Acetyl-L-carnitine. Acetyl-L-carnitine (O-Acetyl-L-carnitine) is a compound involved in human metabolic research. It has relevant applications in predicting metabolite biomarker changes using the Recon 2 metabolic reconstruction model and integrating and analyzing multiple data types, but its specific activity mechanism is not described in detail based on the existing information .
D-Sorbitol-d-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
Dinoprost-d9 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
Phenethicillin sodium-d5 (Pheneticillin sodium-d5; α-Phenoxyethylpenicillin sodium-d5) is the deuterium labeled Phenethicillin sodium (HY-137945). Phenethicillin (α-Phenoxyethylpenicillin) sodium is a Penicillin, and has antimicrobial activity .
Perindopril-d3 (erbumine) is deuterated labeled Perindopril (erbumine) (HY-B0130A). Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure [4].
Atomoxetine-d5 (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
D-Sorbitol-d2-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
D-(+)-Trehalose-d2 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi .
D-Sorbitol-d2-1 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
(S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction .
L-Norleucine-d9 is the deuterium labeled L-Norleucine. L-Norleucine ((S)-2-Aminohexanoic acid) is an isomer of leucine, specifically affects protein synthesis in skeletal muscle, and has antivirus activity.
Meglutol-d3 is the deuterium labeled Meglutol . Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
Meta-Fexofenadine-d6 is the deuterium labeled meta-Fexofenadine. meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine . Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial .
(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
Skatole-d8 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38 .
Labetalol hydrochloride-d5 (AH-5158 hydrochloride-d5) is deuterium labeled Labetalol hydrochloride (HY-B1108). Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy [4].
Glycyl-Exatecan-d5 (Glycyl-DX-8951-d5) hydrochloride is deuterium labeled Glycyl-Exatecan (HY-128995A). Glycyl-Exatecan (Glycyl-DX-8951), a derivative of Exatecan (HY-13631), is an anticancer agent. Glycyl-Exatecan has significantly antitumor activity. Glycyl-Exatecan can be used for cancers like solid tumors research.
Ethyl 4-methylbenzenesulfonate-d5 (Ethyl p-toluenesulfonate-d5; Ethyl tosylate-d5) is deuterium labeled Ethyl 4-methylbenzenesulfonate (HY-W014895). Ethyl 4-methylbenzenesulfonate is a drug intermediate that can be used for the synthesis of alkyl and substituted alkyl fluorides.
Alfacalcidol-d7 is the deuterium labeled Alfacalcidol. Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis [4].
D-(+)-Trehalose-d14 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi .
Skatole-d3 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38 .
Cortisone-d2 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations [4] .
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
Duloxetine-d5 (oxalate) ((S)-Duloxetine-d5 (oxalate)) is deuterium labeled Duloxetine. Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
Palmitoylethanolamide-d5 (Palmidol-d5, PEA-15,15,16,16,16-d5) is deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract .
Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease [4].
Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
13-Methyltetradecanoic acid-d6 is a deuterated labeled 13-Methyltetradecanoic acid . 13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells .
Nonanoyl-CoA-d17 (Pelargonoyl-CoA-d17) is the deuterium labeled Nonanoyl-CoA (HY-E70246). Nonanoyl-CoA is a medium-chain fatty acyl-CoA that can be used as substrate for the medium-chain hydrolase .
Prednisone- 13C2,d2 (Dehydrocortisone- 13C2,d2) is 13C labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus .
C6 Ceramide-d11 is deuterated labeled C6 Ceramide (HY-19542). C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
2'-Deoxycytidine-5'-monophosphoric acid- 13C9, 15N3 dilithium is 13C and 15N-labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
Sulfameter- 13C6 (Sulfametoxydiazine- 13C6) is the 13C6 labeled Sulfameter (HY-B0213). Sulfameter (Sulfametoxydiazine) is an orally active long-acting sulfonamide antibiotic. Sulfameter is active against both Gram-positive and Gram-negative bacteria. Sulfameter can be used for the research of diseases such as respiratory and urinary tract infections .
D-Glucose- 13C2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Propane-1,2,3-triyl tritricosanoate-d5 (Glycerol Tritricosanoate-d5) is deuterium labeled Propane-1,2,3-triyl tritricosanoate. 1,2,3-Tritricosanoyl glycerol is a triacylglycerol that contains tricosanoic acid (HY-W009081) at the sn-1, sn-2, and sn-3 positions. It has been used as an internal standard for the quantification of fatty acids in the triglyceride component of human aortic endothelial cells (HAECs) grown in media supplemented with stearic and/or oleic acid.
Epeleuton-d5 (15(S)-HEPE-d5 ethyl ester) is deuterium labeled Epeleuton. Epeleuton is a second-generation synthetic N-3 fatty acid derivative with activity in patients with non-alcoholic fatty liver disease, although it did not reach the primary endpoints of alanine aminotransferase and liver stiffness, but it can significantly reduce triglycerides, glycated hemoglobin, plasma glucose and inflammatory markers .
Umbelliferone- 13C6 (7-Hydroxycoumarin- 13C6) is the 13C-labeled Umbelliferone (HY-N0573). Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in
chronic alcohol-fed rats [4].
Xylose- 13C5 (D-(+)-Xylose- 13C5) is 13C labeled Xylose. Xylose (D-(+)-Xylose) is a natural pentose sugar that is catalyzed by xylose isomerase to form xylulose, which is a key step in the anaerobic ethanol fermentation of Xylose. Xylose can be used by microorganisms to produce fuels, chemicals, and bulk industrial enzymes. Xylose provides the substances and energy for cells, as a carbon source for the biosynthesis of high-value chemicals and biofuel. Xylose can be used to fully explore lignocellulose resources and provide a new direction for microbia fermentation [4].
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM .
Droxidopa- 13C6 (L-DOPS- 13C6) is 13C labeled Droxidopa. Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) [4].
Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture .
D-Glucose- 13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose- 13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard .
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine . 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis [4].
Indomethacin- 13C6 (Indometacin- 13C6) is 13C labeled Indomethacin. Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research .
Oxybenzone- 13C6 (Benzophenone 3- 13C6) is the 13C-labeled Oxybenzone (HY-A0067). Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells .
Sildenafil-d3-1 (UK-92480-d3-1) is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
Estradiol- 13C6 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
Estradiol- 13C2 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
L-Serine- 13C3, 15N,d3 is the deuterium, 13C-, and 15-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Fluralaner- 13C2, 15N,d3 is the deuterium, 13C-, and 15-labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia .
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE . p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Treprostinil- 13C2-d1 (Sodium) (UT-15- 13C2-d1(sodium)) is deuterium and 13C labeled Treprostinil (sodium). Treprostinil (UT-15) sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
Rufinamide-d2 (CGP 33101-d2) is the deuterium labeled Rufinamide (HY-A0042). Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome [4].
Dehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality [4] .
(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
3,4,5-Trimethoxybenzoic acid-d3 is the deuterium labeled 3,4,5-Trimethoxybenzoic acid[1]. 3,4,5-Trimethoxybenzoic acid (Eudesmic acid;Trimethylgallic Acid) is a benzoic acid derivative. A building block in medicine and organic synthesis. 3,4,5-Trimethoxybenzoic acid exhibits antibacterial activity against S. aureus with MIC of 0.97 μg/mL .
Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality [4] .
Enrofloxacin-d5 (hydriodide) is the deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
3-Indoleacetic acid-d7 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
1-Linoleoyl Glycerol-d5 (1-Linoleoyl-rac-glycerol-d5; 1-Monolinolein-d5) is the deuterium labeled 1-Linoleoyl Glycerol (HY-111346). 1-Linoleoyl glycerol is a LpPLA2 inhibitor. 1-Linoleoyl glycerol acts as a precursor for synthesizing various functional lipids, such as phospholipids. 1-Linoleoyl glycerol mitigates inflammation induced by Apolipoprotein CIII (reduction of IL-6) .
Uridine triphosphate-d13 (UTP-d13 dilithium; Uridine 5'-triphosphate-d13) dilithium is deuterium labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Treprostinil- 13C2,d is the 13C- and deuterium labeled Treprostinil. Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
3-Indoleacetic acid-d5 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid-d5 can be used as internal standard for assay of IAA releases by alkaline hydrolysis of ester and amide conjugates .
N-Decyl-N,N-dimethyldecan-1-aminium-d6 (chloride) is a deuterated labeled N-Decyl-N,N-dimethyldecan-1-aminium (chloride) . N-Decyl-N,N-dimethyldecan-1-aminium chloride (Didecyldimethylammonium chloride) is a dialkyl-quaternary ammonium compound that is used in numerous products for its bactericidal, virucidal and fungicidal properties .
Tadalafil- 13C2,d3-1 (IC-351- 13C2,d3-1) is the deuterium and 13C-labeled Tadalafil (HY-90009A). Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
Retinyl acetate-d3 (ALK-001) is a deuterated Vitamin A. Retinyl acetate-d3 can be used for research of geographic atrophy (GA) secondary to age-related macular degeneration (AMD) .
IDO-IN-7-d10 (NLG-919 analogue-d10; GDC-0919 analogue-d10) is the deuterium labeled IDO-IN-7 (HY-13983). IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Bzo-poxizid-d9 (5C-MDA-19-d9, Petyl MDA-19-d9) is deuterium labeled Bzo-poxizid. Bzo-poxizid is a synthetic cannabinoid that is a psychoactive substance .
O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism .
Tazarotene-13C2,d2 (AGN 190168-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotene (HY-15388). Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
Medroxyprogesterone-d3 is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity .
rac Timolol-d5 (maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction .
(S)-Indoximod-d3 is the deuterium labeled (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer .
Nitroxoline-d5 (8-Hydroxy-5-nitroquinoline-d5) is deuterium labeled Nitroxoline. Nitroxoline (8-Hydroxy-5-nitroquinoline), an antibiotic, is an orally active antibiofilm agent. Nitroxoline reduces the formation and induces the dispersal of Pseudomonas aeruginosa biofilms by chelation of iron and zinc. Nitroxoline can be used for the urinary tract infections and cancer research .
N1-Methylpseudouridine-d3 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
2'-Deoxycytidine- 15N3 is the 15N labeled 2'-Deoxycytidine . 2'-Deoxycytidine, a deoxyribonucleoside, could inhibit biological effects of Bromodeoxyuridine (Brdu) .
Erlotinib- 13C6 hydrochloride is the 13C labeled Erlotinib Hydrochloride . Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM . Erlotinib- 13C6 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2'-Deoxycytidine-5'-monophosphoric acid-d12 dilithium is deuterium labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid . 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [4].
Adenosine monophosphate- 13C10, 15N5,d12 (AMP- 13C10, 15N5,d12) dilithium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Leflunomide- 13C6 (HWA486- 13C6) is 13C labeled Leflunomide. Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.
Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis [4]. Tamoxifen also can induce gene knockout of CreER transgenic mouse .
L-Histidine- 13C6, 15N3,d5 hydrochloride hydrate is the deuterium, 13C-, and 15-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Elvitegravir- 13C6 (GS-9137- 13C6) is 13C labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
Rilpivirine- 13C6 (R278474- 13C6) is 13C labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV(EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
Deoxycytidine triphosphate- 13C9, 15N3 (dCTP- 13C9, 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9, 15N3) dilithium is 13C and 15N-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Cytidine 5′-monophosphate- 13C9, 15N3 (5'-Cytidylic acid- 13C9, 15N3 dilithium; 5'-CMP- 13C9, 15N3) dilithium is 13C and 15N-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Cytidine- 13C9, 15N3 is the 13C and 15N labeled Cytidine . Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [4].
5'-Guanylic acid- 13C10, 15N5 (5'-GMP- 13C10, 15N5 dilithium; 5'-guanosine monophosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
L-Glutamine- 13C5, 15N2,d5 is the deuterium, 13C-, and 15-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Biotin- 13C5 (Vitamin B7- 13C5) is 13C labeled Biotin. Biotin, vitamin B7 and serves as a coenzyme for five carboxylases in humans, involved in the synthesis of fatty acids, isoleucine, and valine, and in gluconeogenesis. Biotin is necessary for cell growth, the production of fatty acids, and the metabolism of fats and amino acids .
Glucosylsphingosine- 13C6 (Glucopsychosine- 13C6) is the 13C-labeled Glucosylsphingosine (HY-N7745). Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide with neurotoxicity and is also a noncompetitively inhibitor of glucocerebrosidase with a Ki value of 30 μM. Glucosylsphingosine is promising for research of Krabbe and Gaucher disease.
Fosfructose- 13C6 (tetrasodium hydrate) is the 13C labeled Fosfructose (HY-106950). Fosfructose is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma .
2-Phenylethanol- 13C2 is 13C labeled 2-Phenylethanol (HY-B1290). 2-Phenylethanol (Phenethyl alcohol) is an aromatic alcohol with a rose-like odour. 2-Phenylethanol is a flavour and fragrance compound, and can be used as a preservative and anti-microbial agent. 2-Phenylethanol has antityrosinase and antimicrobial activities .
Sulfamethazine- 13C6 is a 13C-labeled Sulfamethazine (HY-A0178). Sulfamethazine (Sulfadimidine) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections) .
Colfosceril miristate-d13 (DMPC-d13) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Hydroxyprogesterone Caproate-d11 (17α-Hydroxyprogesterone hexanoate-d11; 17α-Hydroxyprogesterone caproate-d11) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate is a synthetic progestin, a steroid.
Ribitol- 13C5 (Adonitol- 13C5) is the 13C-labeled Ribitol (HY-100582). Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol.
VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc) .
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats [4] .
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
D-Fructose- 13C6,d7 is the deuterium and 13C labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants .
Menaquinone-4-d7 (Vitamin K2(MK-4)-d7) is the deuterium labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
Oleic acid-d9 is deuterium labeled Oleic acid (HY-N1446). Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activato .
α-Vitamin E-d11 ((+)-α-Tocopherol-d11) is the deuterium labeled α-Vitamin E (HY-N0683). α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant .
Colfosceril miristate-d9 (DMPC-d9) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Furagin- 13C3 (Furazidine- 13C3) is the 13C-labeled Furagin (HY-77036). Furagin (Furazidine), an analogue of Nitrofurantoin (HY-A0090), is an antibiotic with antibacterial activity against ESKAPE pathogens with MIC values of 0-32 μg/mL. Furagin inhibits human Carbonic anhydrases . Furagin is promising for research of cancer and urinary tract infections (UTIs) [4] .
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d67 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
1,3-Dipalmitin-d5 (1,3-Dipalmitoylglycerol-d5) is a deuterium labeled 1,3-Dipalmitin (HY-128792). 1,3-Dipalmitin (1,3-Dipalmitoylglycerol) is a cerebroside that can be found in Typhonium giganteum Engl .
Colfosceril miristate-d58 (DMPC-d58) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Tazarotenic acid-13C2,d2 (AGN 190299-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
Sapropterin-d3((6R)-BH4-d3) is deuterium labeled Sapropterin. Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU) .
Docosahexaenoic acid-d5 methyl ester is the deuterium labeled Docosahexaenoic Acid methyl ester. Docosahexaenoic Acid methyl ester is a methylated docosahexaenoic acid analog which can be intercalated into membrane phospholipids without being oxidized or hydrolyzed .
Oleic acid-d2) is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid ]. Oleic acid is a Na+/K+ ATPase activator .
Colfosceril miristate-d63 (DMPC-d63) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Deoxycytidine triphosphate-d14 (dCTP-d14 dilithium; 2′-Deoxycytidine-5′-triphosphate-d14) dilithium is deuterium labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
L-5-Hydroxytryptophan-d3-1 is the deuterium labeled L-5-Hydroxytryptophan . L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [4] .
(Rac)-Atomoxetine-d7 (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Thymidine- 15N2 is the 15N labeled Thymidine . Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication [4].
Oleic acid-d17 is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate . Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor [4] .
Cytidine-5'-triphosphate-d14 (Cytidine triphosphate-d14 dilithium; 5'-CTP-d14) dilithium is deuterium labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist .
Levofloxacin-d3 ((-)-Ofloxacin-d3) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity [4] .
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning [4].
Carbocisteine-d3 (Carbocysteine-d3) is deuterium labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research [4] .
Phenformin-d5 (hydrochloride) is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity .
Digoxigenin-d3 (Lanadigenin-d3) is the deuterium labeled Digoxigenin (HY-B1025). Digoxigenin (DIG) is a steroid. DIG is used for situ hybridization as a labeling molecule probe due to long shelf life and fast detection and high sensitivity of DIG-labeled riboprobes .
Pyridoxine-d2 (Pyridoxol-d2) is deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Fenoverine-d8 is the deuterium labeled Fenoverine. Fenoverine (Spasmopriv) is an orally active and powerful anti-spasmodic drug. Fenoverine reduces calcium ion influx by suppressing voltage dependent calcium channels. Fenoverine has antiemetic, analgesic, and antidiarrheal effects. Fenoverine induces rhabdomyolysis. Fenoverine can be used to study smooth muscle overexcitation related conditions such as gastrointestinal spasms .
Dipivefrin-d6 (hydrochloride) is deuterium labeled Dipivefrin (hydrochloride). Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma proagent that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea .
Diphenylmethane-d2 (Benzylphenyl-d2) is the deuterium labeled Diphenylmethane (HY-W008814). Diphenylmethane (Benzylphenyl) is an aromatic compound used as a drug intermediate. Diphenylmethane in the fragrance industry is used as an oxidizing agent and in soaps; in pesticides, as a synergist; and in dyes, as a plasticizer.
Ibuprofen-d3 ((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [4].
Norethindrone-d8 (Norethisterone-d8) is deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Levofloxacin-d8 is the deuterium labeled Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
Desacetylcephapirin-d6 sodium (Deacetylcephapirin-d6 sodium) is the deuterium labeled Desacetylcephapirin sodium (HY-131989). Desacetylcephapirin (Deacetylcephapirin) sodium is an active metabolite of Cephapirin (HY-A0153A). Desacetylcephapirin sodium has antimicrobial against S. aureus and coagulase-negative staphylococci mastitis pathogen .
Deltamethrin-d5 is the deuterium labeled Deltamethrin. Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis .
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
Temephos-d12 is the deuterium labeled Temephos . Temefos is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage .
Betulin-d3 (Trochol-d3) is deuterium labeled Betulin. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line .
Pyridoxine-d5 (Pyridoxol-d5) is a deuterium labeled Pyridoxine (HY-B1328). Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence . Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor .
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine(HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections [4].
Nordoxepin-d3 (hydrochloride) is the deuterium labeled Nordoxepin hydrochloride. Nordoxepin hydrochloride is an active metabolite of Doxepin hydrochloride (HY-B0725), which is an orally active tricyclic antidepressant .
Salvigenin-d9 is the deuterium labeled Salvigenin. Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties .
Bendroflumethiazide-d5 (Bendrofluazide-d5) is the deuterium labeled Bendroflumethiazide (HY-B1363).Bendroflumethiazide (Bendrofluazide) is an orally available diuretic. Bendroflumethiazide inhibits the electroneutral sodium-chloride symporter located in the apical membrane of the early segment of the distal convoluted tubule and can effectively lower blood pressure. Bendroflumethiazide is used in the study of hypertension and edema. Bendroflumethiazide has an antidiuretic effect in diabetes insipidus .
Bestatin-d10 (Ubenimex-d10) is deuterium labeled Bestatin. Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
Edoxudine-d5 (EUDR-d5) is the deuterium labeled Edoxudine (HY-B1011). Edoxudine is an antiviral active molecule and thymidine analog. Edoxudine is effective against herpes simplex virus .
Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Dyclonine-d9 (hydrochloride) is deuterium labeled Dyclonine (hydrochloride). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an effective component of Runhou tablets. Dyclonine hydrochloride has significant bactericidal and fungicidal activity .
Chlorpheniramine-d6 (Chlorphenamine-d6) is deuterium labeled Chlorpheniramine. Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research .
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma [4] .
Hexadecanal-d5 (Palmitaldehyde-d5) is deuterium labeled Hexadecanal. Hexadecanal (Palmitaldehyde) , a volatile long-chain aliphatic aldehyde, is emitted from human feces, skin, and breath. The receptor for hexadecanal(OR37B) is highly conserved across mammals. Hexadecanal may exert its effects by modulating functional connectivity between the brain substrates of social appraisal and the brain substrates of aggressive execution. Also, Hexadecanal is confirmed to be highly deterrent to the ant Lasius niger. Hexadecanal is promising for the research of startle responses and aggression [4]
Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
Nefopam-d3 (hydrochloride) is the deuterium labeled Nefopam hydrochloride. Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo .
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria .
Levamisole-d5 (hydrochloride) is the deuterium labeled Levamisole hydrochloride. Levamisole ((-)-Tetramisole) hydrochloride is an anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives. Levamisole hydrochloride has antiviral effects against HSV .
Ethambutol-d10 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Norethindrone-d7 (Norethisterone-d7) is the deuterium labeled Norethindrone (HY-B0554). Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Hydrocortisone-d2 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Pyridoxine-d3 is a deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway .
Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Lumefantrine-d9 is the deuterium labeled Lumefantrine. Lumefantrine is an antimalarial drug, used in combination with Artemether. The artemether-lumefantrine (AL) as the first- and second-line anti-malarial drugs.
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55) .
Deltamethrin-d6 (Decamethrin-d6) is deuterium labeled Deltamethrin. Deltamethrin (Decamethrin) is an orally active synthetic pyrethroid insecticide. Deltamethrin induces oxidative stress and results in inflammation and apoptosis via inhibiting Nrf2/HO-1 pathway. Deltamethrin has an anticancer effect by inducing apoptosis. Deltamethrin can be used extensively in pest control [4] .
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
Diphenylmethanol-d10 (Benzhydrol-d10) is the deuterium labeled Benzhydrol (HY-W004059). Diphenylmethanol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
Prednisone-d7 (Dehydrocortisone-d7) is deuterium labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus .
Desmethylmirtazapine-d6 hydrochloride (Normirtazapine-d6 hydrochloride) is the deuterium labeled Desmethylmirtazapine (HY-119223). Desmethylmirtazapine is an active metabolite of Mirtazapine that has antidepressant effects .
Pramocaine-d9 (hydrochloride) is deuterium labeled Pramocaine (hydrochloride). Pramocaine hydrochloride decreases the permeability of neuronal membranes to sodium ions, blocking both initiation and conduction of nerve impulses.
Anagliptin-d7 (SK-0403-d7) is deuterium labeled Anagliptin. Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4(DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively .
Ethotoin-d5 is the deuterium labeled Ethotoin . Ethotoin (Peganone) is an orally active anticonvulsant agent used in epilepsy research, Ethotoin is a hydantoin, similar to phenytoin .
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch .
Acenaphthylene-d8 is the deuterium labeled Acenaphthylene . Acenaphthylene is a polycyclic aromatic hydrocarbon (PAH). PAHs are derived naturally from coal and tar deposits, and produced by incomplete combustion of organic matter .
Econazole-d6 ((±)-Econazol-d6) is the deuterium labeled Econazole (HY-B0885). Econazole is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage [4] .
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent .
Torsemide-d7 is the deuterium labeled Torsemide. Torsemide (Torasemide) is an orally active loop diuretic. Torsemide has anti-aldosterone and vasodilatory effects. Torsemide also can be used for the research of heart failure, renal disease and hepatic cirrhosis .
Piperacillin-d5 is deuterium labeled Piperacillin. Piperacillin is kind of semisynthetic penicillins. Piperacillin has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Piperacillin has shown greater activity against β-lactamase-producing organisms than the other penicillins .
Lidocaine-d6 (Lignocaine-d6) is deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
Pitolisant-d6 (Tiprolisant-d6) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
Adrenosterone-d10 ((+)-Adrenosterone-d10) is the deuterium labeled Adrenosterone (HY-17462). Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells .
Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect [4].
Psychosine-d7 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell
Trigonelline-d3 (chloride) is the deuterium labeled Trigonelline chloride. Trigonelline chloride, an alkaloid with potential antidiabetic activity, is present in considerable amounts in coffee. Trigonelline chloride has anti-HSV-1 , antibacterial, and antifungal activities.
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Atovaquone-d5 is the deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome?bc1?complex. Atovaquone is against human and ?P. falciparum?cytochrome?bc1?activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia .
Dibucaine-d9 is the deuterium labeled Dibucaine(HY-B0552).Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor .
Pitolisant-d10 (Tiprolisant-d10) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Prednisone-d8 is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
Bendroflumethiazide-d7 (Bendrofluazide-d7) is deuterium labeled Bendroflumethiazide (HY-B1363). Bendroflumethiazide (Bendrofluazide) is an orally available diuretic. Bendroflumethiazide inhibits the electroneutral sodium-chloride symporter located in the apical membrane of the early segment of the distal convoluted tubule and can effectively lower blood pressure. Bendroflumethiazide is used in the study of hypertension and edema. Bendroflumethiazide has an antidiuretic effect in diabetes insipidus .
Amitriptylinoxide-d6 (Equilibrin-d6) is the deuterium labeled Amitriptylinoxide (HY-107032). Amitriptylinoxide (Equilibrin) is an analogue and metabolite of amitriptyline with similar antidepressant efficacy .
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
Ditiocarb-d10 sodium (Sodium diethyldithiocarbamate-d10) is the deuterium labeled Ditiocarb sodium (HY-B1637). Ditiocarb sodium (Sodium diethyldithiocarbamate) is an orally active copper reagent. Ditiocarb sodium exhibits activities such as antioxidation, chelation, anti-tumor effects, immunomodulation, and anti-HIV properties. Ditiocarb sodium can be used in the research of tumors, inflammatory, and immune-related diseases .
Pefloxacin-d3 (Pefloxacinium-d3) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies [4] .
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin? is a Histamine 1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant .
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis [4] .
Furaltadone-d5 is the deuterium labeled Furaltadone (HY-B1148A). Furaltadone, a nitrofuran agent, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci .
Psychosine-d5 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell.
Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium lepraeInhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy [4] .
Nefopam-d3 is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells .
Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies [4] .
Imidaprilat-d3 (6366A-d3) is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease .
DTAC-d3 (Dodecyltrimethylammonium-d3 chloride) is the deuterium labeled DTAC (HY-W096983). DTAC is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Bopindolol-d9 ((±)-Bopindolol-d9) is the deuterium labeled Bopindolol (HY-B1562). Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
Inosinic acid- 13C5 (5'-IMP- 13C5) is the 13C-labeled Inosinic acid (HY-108213). Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant, or as the dietary supplement to improve the yield and meat quality of pigs .
Chlorogenic acid- 13C3 (Heriguard- 13C3; NSC-407296- 13C3) is 13C- and 15N-labeled Chlorogenic acid (HY-N0055). Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb.. It plays several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension .
Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
SARM1-IN-7 is a potent active site (orthosteric) and orally active SARM1 inhibitor. SARM1-IN-7 continuously activates the enzymatic activity of SARM1, thereby exacerbating the depletion of NAD at sub-minimal concentrations. SARM1-IN-7 demonstrated dual benefits in the SARM1-activated cell models and mouse models: a high dose exerted a cell/neuron protective effect, while a low dose exacerbated cell/neuron damage. SARM1-IN-7 can be used for the study of axon degeneration .
ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
L-Theanine- 13C2, 15N2 (L-Glutamic Acid γ-ethyl amide- 13C2, 15N2) is the 13C- and 15N-labeled L-Theanine (HY-15121). L-Theanine (L-Glutamic Acid γ-ethyl amide) is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective, anticancer and anti-oxidative activities. L-Theanine can pass through the blood–brain barrier and is orally active.
Cytidine-d13 (Cytosine β-D-riboside-d13) is deuterium labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function .
Thymidine- 13C10 (DThyd- 13C10; NSC 21548- 13C10) is 13C-labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Cytidine 5′-monophosphate-d12 (5'-Cytidylic acid-d12 dilithium; 5'-CMP-d12) dilithium is deuterium labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid-d12 (5'-GMP-d12 dilithium; 5'-guanosine monophosphate-d12) dilithium is deuterium labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Estrone- 13C3 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Ritonavir- 13C3 is 13C labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM .
D-Mannitol- 13C6 is the 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
L-Glutathione reduced-d5 (GSH-d5; γ-L-Glutamyl-L-cysteinyl-glycine-d5) is the deuterium labeled L-Glutathione reduced (HY-D0187). L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
Omeprazole metabolite Omeprazole sulfone (methoxy-d3) is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Sarcosine- 13C3 (N-Methylglycine- 13C3; Sarcosin- 13C3) is the 13C-labeled Sarcosine (HY-101037). Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
N-Acetyl mesalazine-d3 (N-Acetyl-5-aminosalicylic acid-d3) is the deuterium labeled N-Acetyl mesalazine (HY-66008). N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the primary intestinal metabolite of 5-Aminosalicylic Acid (HY-15027) and serves as a biomarker for evaluating the efficacy of 5-Aminosalicylic Acid (HY-15027). N-Acetyl mesalazine can scavenge free radicals, reduce DNA base hydroxylation, and ameliorate mucosal inflammation. N-Acetyl mesalazine can be used in the study of diseases such as colitis and colon cancer .
Guanosine- 15N5 is the 15N labeled Guanosine . Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Nicotinamide- 13C6 is the 13C-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Guanosine triphosphate- 15N5,d14 (GTP- 15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
L-Tryptophan- 13C11 is the 13C-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
6-(γ,γ-Dimethylallylamino)purine-d6 is the deuterium labeled 6-(γ,γ-Dimethylallylamino)purine (HY-112103). 6-(γ,γ-Dimethylallylamino)purine is a plant growth substance .
Cytidine-d2 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function .
Pyrroloquinoline quinone- 13C3 (PQQ- 13C3) sodium is an isotope of Pyrroloquinoline quinone. Pyrroloquinoline quinone (PQQ), a redox co-factor, is an anionic, redox-cycling orthoquinone. Pyrroloquinoline quinone is isolated from cultures of methylotropic bacteria and tissues of mammals. Pyrroloquinoline quinone is an essential nutrient for mammals and is important for immune function .
Desogestrel- 13C2,d2-1 (Org-2969- 13C2,d2-1) is the deuterium labeled and 13C-labeled Desogestrel (HY-12516). Desogestrel (Org-2969) is a third-generation progesterone analogue contained in many oral contraceptive preparations. Desogestrel is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups [4].
Estrone- 13C2 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Glucosamine- 13C6 (D-Glucosamine- 13C6) is 13C labeled Glucosamine. Glucosamine (D-Glucosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes .
Cyromazine- 13C3 is the 13C3 labeled Cyromazine. Cyromazine is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects.
L-Tryptophan- 15N2 is the 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
(E,E)-Farnesol-d6 (trans,trans-Farnesol-d6) is deuterium labeled (E,E)-Farnesol (HY-Y0248). (E,E)-Farnesol (trans,trans-Farnesol) is a quorum-sensing molecule of Candida species. (E,E)-Farnesol can inhibit the growth, metabolism and biofilm formation of various Candida species, and affect their morphology and invasiveness .
(R,R)-Secoisolariciresinol diglucoside-d6 is deuterated labeled (R,R)-Secoisolariciresinol diglucoside (HY-N6937). (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells .
Guanosine- 13C10 is the 13C labeled Guanosine (HY-N0097). Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Adenosine monophosphate- 15N5,d12 (AMP- 15N5,d12) dilithium is deuterium and 15N labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Cytidine-d is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catechol
Tricaprilin- 13C3 (Trioctanoin- 13C3) is a 13C-labeled Tricaprilin (HY-B1804) . Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
Clomipramine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Clomipramine (hydrochloride). Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD) .
D-Glucose- 13C3-1 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Methoxsalen- 13C,d3 (8-Methoxypsoralen- 13C,d3) is the deuterium and 13C-labeled Methoxsalen (HY-30151). Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) .Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Dihydroartemisinin- 13C,d5 (Dihydroqinghaosu- 13C,d5) is the deuterium labeled and 13C-labeled Dihydroartemisinin (HY-N0176). Dihydroartemisinin is a potent anti-malaria agent.
D-Glucose- 13C,d is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C3-2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
Decitabine- 13C5 (5-Aza-2'-deoxycytidine- 13C5) is 13C labeled Decitabine. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .
Tedizolid- 13C,d3 is the 13C- and deuterium labeled Tedizolid. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Lumateperone- 13C,d3 (ITI-007- 13C,d3) tosylate is 13C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia [4].
Vanillin- 13C6 is the 13C labeled Vanillin . Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine .
Rufinamide- 15N,d2 (CGP 33101- 15N,d2) is the deuterium and 15N labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome [4].
2-Methoxybenzoic acid- 13C6 is the 13C-labeled 2-Methoxybenzoic acid. 2-Methoxybenzoic acid (NSC 3778) is used as an internal standard of salicylic acid and its putative biosynthetic precursors in cucumber leaves. Another known use is in the synthesis of Benextramine.
Lamotrigine- 13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
3-O-Methyldopa-d3 (3-Methoxy-L-tyrosine-d3) is deuterium labeled 3-O-Methyldopa (HY-113468A). 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa has certain antidepressant and neuroprotective activities. 3-O-Methyldopa can be used in the research of nervous system diseases such as depression and Parkinson's disease .
L-Theanine-d5 is the deuterium labeled L-Theanine. L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake .
Hypoxanthine- 13C5 is a 13C-labeled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Vitamin D3- 13C5 is the 13C-labeled Vitamin D3 (HY-15398). Vitamin D3 (Cholecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells .
L-Glutamine- 15N2,d5 is the deuterium and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability [4].
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Vitamin K1- 13C6 is the 13C-labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism.
Adenosine- 13C10 (Adenine riboside- 13C10; D-Adenosine- 13C10) is 13C-labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis [4] .
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
Procainamide- 13C2 hydrochloride is 13C labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Vadadustat- 13C6 (PG-1016548- 13C6) is 13C labeled Vadadustat. Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor . Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo .
Dutasteride- 13C6 is the 13C labeled Dutasteride . Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
Fosamprenavir- 13C6 is the 13C-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .
Adrenosterone- 13C3 ((+)-Adrenosterone- 13C3) is the 13C-labeled Adrenosterone (HY-17462). Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells .
D-Sorbitol- 13C6 is the 13C labeled D-Sorbitol . D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement .
3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) hydrate is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa hydrate inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa hydrate has certain antidepressant and neuroprotective activities. 3-O-Methyldopa hydrate can be used in the research of nervous system diseases such as depression and Parkinson's disease .
Lodoxamide- 15N2,d2 (U-42585E (free acid)- 15N2,d2) is the deuterium and 15N-labeled Lodoxamide (HY-14270). Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
Adenosine- 13C5 is the 13C labeled Adenosine . Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
Pentetic acid- 13C5 (Diethylenetriaminepentaacetic acid- 13C5) is the 13C-labeled Pentetic acid (HY-B1335). Pentetic acid (Diethylenetriaminepentaacetic acid) is an orally active compound with biodegradability used to construct magnetic adsorbent, which can simultaneously remove heavy metal and dye from complex wastewater. Pentetic acid can form strong metal complexes, which prevents metal ions from catalysing the decomposition of peroxygen chemicals, especially hydrogen peroxide [4].
Pantethine- 15N2 is the 15N2 labeled Pantethine. Pantethine is an orally active lipid-lowering agent. Pantethine has anti-tumor, anti-inflammatory and anti-SARS-COV virus activities. Pantethine is also a neuroprotective agent. Pantethine can be used in the study of Alzheimer's disease, Parkinson's disease, major depression, systemic sclerosis and pantothenate kinase-related neurodegeneration [4] .
L-Serine- 13C3 is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Histamine- 13C5, 15N3 (Ergamine- 13C5, 15N3) is the 13C and 15N labeled isotope of Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
Deoxythymidine-5'-triphosphate- 15N2,d15 (dTTP- 15N2,d15) dilithium is deuterium and 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Vitamin D3- 13C3 is the 13C-labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Topiramate-13C6 (McN 4853-13C6) is the 13C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
Thyroxine hydrochloride- 13C6 is the 13C-labeled L-Thyroxine. L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4) .
ATP- 15N5,d14 (Adenosine 5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Etravirine- 13C3 (R165335- 13C3) is the 13C-labeled Etravirine (HY-90005). Etravirine (R165335; TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Glycidamide- 13C3 (Oxiranecarboxamide- 13C3) is the 13C-labeled Glycidamide (HY-119329). Glycidamide is the genotoxic metabolite of Acrylamide. Glycidamide can react with proteins, such as hemoglobin, or with DNA, and induces genotoxic effects .
Adenosine- 15N5 (Adenine riboside- 15N5; D-Adenosine- 15N5) is the 15N labled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
Zonisamide- 13C6 (AD 810- 13C6) is 13C labeled Zonisamide. Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy [4].
Saracatinib-d3 (AZD0530-d3) (ZG5129) is the deuterium-labeled analog of Saracatinib (HY-10234). Saracatinib-d3 is an inhibitor of the Src kinase, which can inhibit severe sepsis caused by bacterial or various microbial infections .
Perindopril-d5 (S-9490-d5) is deuterium labeled Perindopril. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension [4].
Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
Iodopropynyl butylcarbamate-d9 (IPBC-d9) is the deuterium labeled Iodopropynyl butylcarbamate (HY-W009335). Iodopropynyl butylcarbamate (IPBC) is a potent fungicide and preservative, which has been used in the paints, coatings, wood preservatives, personal care, and cosmetics industries .
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders .
Nabumetone-d3 is the deuterium labeled Nabumetone. Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the proagent of the active metabolite 6MNA.
Eletriptan-d3 is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively .
Vericiguat-d3 (BAY1021189-d3) hydrochloride is a deuterated Vericiguat with tracer functionality. Vericiguat is an orally available stimulator of guanylate cyclase .
Licofelone-d6 is the deuterium labeled Licofelone . Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins [4].
Cyprodinil-d5(CGA-219417-d5) is the deuterium labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
Phytosphingosine-d7(4-Hydroxysphinganine-d7) is deuterium labeled Phytosphingosine. Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes [4] .
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation .
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
Dienogest-d6 is deuterium labeled Dienogest (HY-B0084). Dienogest is an orally active progesterone receptor agonist that can be used in the study of endometriosis .
Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B .
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Upadacitinib-d5 is the deuterium labeled Upadacitinib. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Quinapril-d5 hydrochloride (CI-906-d5) is the deuterium labeled Quinapril hydrochloride. Quinapril hydrochloride (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications .
Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM .
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM) .
Ertugliflozin-d9 is deuterated labeled Ertugliflozin (HY-15461). Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2 . Has the potential for the treatment of type 2 diabetes mellitus .
Dinotefuran-d3 is the deuterium labeled Dinotefuran . Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors .
Penicillin G-d5 (potassium) is the deuterium labeled Penicillin G potassium. Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas .
Trifloxystrobin-d3 is the deuterium labeled Trifloxystrobin (HY-123230). Trifloxystrobin (CGA 279202) is a type of fungicide. Trifloxystrobin has toxicity, antiparasitic activity and induce apoptosis, oxidative stress and DNA damage. Trifloxystrobin can be used for the reaesrch of fungal diseases [4] .
Trandolapril-d5 is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF) .
Dansyl chloride-d6 is the deuterium labeled Dansyl chloride (HY-D0017). Dansyl chloride is a reagent that produces stable blue or blue-green fluorescent sulfonamide adducts in the reaction of aliphatic and aromatic amines with primary amino groups, and is widely used for modified amino acids, protein sequencing and amino acid analysis .
Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer [4].
Voxelotor-d6 (GBT 440-d6) is deuterium labeled Voxelotor. Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment .
Etrasimod-d9 (APD334-d9) is a deuterium labeled Etrasimod (HY-12789). Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells. .
Posaconazole-d5 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity .
Mexiletine-d3 (hydrochloride) is deuterium labeled Mexiletine (hydrochloride). Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1][2].
Atenolol-d6 ((RS)-Atenolol-d6) is deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris .
Ergothioneine-d9 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant .
Cuminaldehyde-d8 is deuterated labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Flunixin-d3 is the deuterium labeled Flunixin. Flunixin Meglumine is a potent inhibitor of COX used as analgesic agent with anti-inflammatory and antipyretic activity .
Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively .
Permethrin-d6 (NRDC-143-d6) is deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) [4] .
Amoxapine-d8 is the deuterium labeled Amoxapine. Amoxapine (CL-67772) is a norepinephrine reuptake blocker and a 5-HT2/5-HT3 antagonist. Amoxapine can be used for the research of depression. Amoxapine has antibacterial activity. Amoxapine can enhance the killing effect of macrophages on mycobacterium by inducing autophagy, while protecting the cells from death [4].
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
Diethyl cromoglycate-d5 (Diethylchromoglycate-d5) is the deuterium labeled Diethyl 5,5'-((2-hydroxypropane-1,3-diyl)bis(oxy))bis(4-oxo-4H-chromene-2-carboxylate) (HY-W099125).
Resorufin-d6 is the deuterium labeled Resorufin. Resorufin (NSC 12097) is a highly fluorescent pink dye for the detection of ROS/RNS and a second analyte .
Iodobenzene-d5 is the deuterium labeled 1-Iodobenzene. Iodobenzene can undergo Ullmann coupling reaction on copper catalyst to generate biphenyl. Iodobenzene can undergo Suzuki reaction with phenylboronic acid to generate biphenyl .
Parbendazole-d3 is the deuterium labeled Parbendazole. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects .
Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels .
Ledipasvir-d16 (GS-5885-d16) is deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Blonanserin-d5 (AD-5423-d5) is a deuterium labeled Blonanserin (HY-13575). Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic .
Glycolithocholic acid-d5 (Lithocholylglycine-d5) is the deuterium labeled Glycolithocholic acid (HY-116374). Glycolithocholic acid (Lithocholylglycine), an endogenous metabolite, is a glycine-conjugated secondary bile acid. Glycolithocholic acid can be used to diagnose ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH) and primary sclerosing cholangitis (PSC) [4].
Treprostinil-d7 (UT-15-d7) is a deuterated version of Treprostinil (HY-100441). Treprostinil is a highly potent DP1 and EP2 agonist with EC50s of 0.6 nM and 6.2 nM, respectively [4] .
Anastrozole-d12 is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM .
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage .
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research [4].
Danicamtiv-d6 (MYK-491-d6) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
Lauryl benzalkonium-d7 (Dimethylaurylbenzylammonium-d7) chloride is the deuterium labeled Lauryl benzalkonium chloride. Lauryl benzalkonium chloride is a cationic surfactant .
Dolasetron-d5 is deuterated labeled Dolasetron (HY-B0750). Dolasetron (MDL-73147) is a 5-HT3 receptor antagonist with potential for treatment of chemotherapy-induced nausea and vomiting.
Crizotinib-d9 (PF-02341066-d9) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
Benzyl alcohol-d5 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives . Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ropinirole-d14 hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Canagliflozin-d6 is the deuterium labeled Canagliflozin . Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively .
Parecoxib-d5 (SC 69124-d5) is deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
Losartan-d2 is the deuterium labeled Losartan . Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Pemetrexed-d5 is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
Methylprednisolone-d2 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels [4].
Ropinirole-d3 (SKF 101468-d3) is deuterium labeled Ropinirole. Ropinirole (SKF 101468) is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole has no affinity for the D1 receptors. Ropinirole has the potential for Parkinson's disease .
Tazarotene-d6 (AGN 190168-d6) is deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
Tigecycline-d9 is deuterium labeled Tigecycline. Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL . MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively .
Zafirlukast-d6 is deuterated labeled Zafirlukast (HY-17492). Zafirlukast (ICI 204219) is a potent orally active leukotriene D4(LTD4)receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Ritodrine-d3 (hydrochloride) is the deuterium labeled Ritodrine (hydrochloride). Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
Prochloraz-d7 (BTS 40542-d7) is the deuterium labeled Prochloraz (HY-B0845). Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM .
Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity .
Permethrin-d9 is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
Losartan-d9 is the deuterium labeled Losartan . Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Ozenoxacin-d3 is the deuterium-labeled Ozenoxacin (HY-14957). Ozenoxacin-d3 is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Alfuzosin-d7 is the deuterium labeled Alfuzosin . Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) .
Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
1-Octanol-d5 is deuterated labeled 1-Octanol (HY-W032013). 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Leniolisib-d5 is a deuterated labeled Leniolisib . Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
Treprostinil-d9 (UT-15-d9) is the deuterium-labeled Treprostinil (HY-100441) . Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
1-Octanol-d17 is the deuterium labeled 1-Octanol . 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Diphenyl Phosphate-d10 (DPhP-d10) is the deuterium labled Diphenyl Phosphate (HY-W008151). Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.
Cefiderocol-d6 (S-649266-d6) is a deuterated labeled Cefiderocol (HY-17628). Cefiderocol is a siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less .
Sulindac-d3 is deuterium labeled Sulindac. Sulindac (MK-231) is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.
Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
Iodobenzene-d2 is the deuterium labeled 1-Iodobenzene. Iodobenzene can undergo Ullmann coupling reaction on copper catalyst to generate biphenyl. Iodobenzene can undergo Suzuki reaction with phenylboronic acid to generate biphenyl .
Creatinine-d5 is the deuterium labeled Creatinine. Creatinine (NSC13123) is a break-down product of creatine phosphate in muscle, and is usually produced at a fairly constant rate by the body .
Tandospirone-d8 (SM-3997-d8) is deuterium labeled Tandospirone. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms [4].
Dimethylamine-d6 hydrochloride is a deuterium labeled Dimethylamine hydrochloride. Dimethylamine hydrochloride is the immediate precursor of dimethylnitrosamine, a known potent carcinogen in a wide variety of animal species .
Terbinafine-d3 (TDT 067-d3) is deuterium labeled Terbinafine. Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
Goserelin-d10 (ICI 118630-d10) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
Pazopanib-d3 (GW786034-d3) is deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Fluorofenidone-d3 (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
Penicillin V-d5 (potassium) is the deuterium labeled Penicillin V Potassium . Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis [4] .
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Methoxyamine-d3 (O-Methylhydroxylamine-d3) hydrochloride is the deuterium labeled Methoxyamine hydrochloride. Methoxyamine hydrochloride is an orally active and potent base excision repair (BER) inhibitor .
Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Albendazole-d3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a agent indicated for the treatment of a variety of worm infestations .
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
Nirmatrelvir-d6 (PF-07321332-d6) is deuterium labeled Nirmatrelvir. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
Capsaicin-d3 is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects[1][2].
Povorcitinib-d6 (INCB54707-d6) is the deuterium labeled Povorcitinib (HY-145588). Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) .
Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
Benzyl alcohol-d7 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Ambroxol-d5 (hydrochloride) is the deuterium labeled Ambroxol hydrochloride. Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research .
Ethopabate-d5 (Ethyl pabate-d5) is the deuterium labeled Ethopabate (HY-B2138). Ethopabate (Ethyl pabate) is an orally active antiparasitic agent. Ethopabate is often used in combination with Amprolium hydrochloride (HY-B0937A) and others to prevent and treat poultry coccidiosis, leucosis, and other diseases .
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist .
Selinexor-d5 (KPT-330-d5) isthe deuterium labeled Selinexor (HY-17536). Selinexor (KPT-330), an analog of KPT-185, is an orally active and selective CRM1 inhibitor .
Bifenox-d3 is the deuterium labeled Bifenox. Bifenox (MC-4379) is a nitrophenyl ether herbicide. Bifenox disrupts cellular membrane, inhibits photosynthesis and inhibits the protoporphyrinogen oxidase. Bifenox increases the ROS production in the microalgae Chlamydomonas reinhardtii .
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Apalutamide-d3 is the deuterium labeled Apalutamide . Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM .
Trifloxystrobin-d6 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h .
Tadalafil-d3 is the deuterium labeled Nortadalafil. Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea .
Celecoxib-d7 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM .
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator [4].
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
Abemaciclib-d8 is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
Ditiocarb-d10 (Diethyldithiocarbamic acid-d10) is the deuterium labeled Ditiocarb (HY-126363) . Ditiocarb (Diethyldithiocarbamic acid) is an accelerator of the rate of copper cementation. Ditiocarb (Diethyldithiocarbamic acid) reduces the incidence of HIV infection, and also enhances adjuvant immunoresearch of high risk breast cancer [4].
Emtricitabine-d2 (BW1592-d2) is deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Dimethyl phthalate-d6 is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins .
Remdesivir-d5 (GS-5734-d5) is a deuterium labeled Remdesivir (HY-104077). Remdesivir (GS-5734) is a nucleoside analogue with effective antiviral activity. Remdesivir can inhibit the synthesis of viral DNA or RNA. Remdesivir can be used for the research of infection, such as SARS-CoV and MHV infection .
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Capsaicin-d7 is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects .
Omeprazole-d6 (H 16868-d6) is deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Parecoxib-d3 is the deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor . N-ethylmaleimide specific inhibits phosphate transport in mitochondria . N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor .
Eprinomectin-d3 (MK-397-d3) is the deuterium-labeled Eprinomectin (HY-12643). Eprinomectin is a type of avermectin. Eprinomectin，as a broad-spectrum fungicide，has insecticidal，insecticidal and acaricidal activities. Eprinomectin induces apoptosis and autophagy in prostate cancer cells and has antitumor activity .
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
Flurbiprofen-d3 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
Glyceryl monostearate-d5 (GMS-d5) is deuterium labeled Glyceryl monostearate. Glyceryl monostearate (GMS) is a single-tailed lipidic monoglyceride that can be used to synthesize nanoliposomes for drug delivery .
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al) .
Puromycin-d3 (dihydrochloride) is the deuterium labeled Puromycin dihydrochloride. Puromycin dihydrochloride (CL13900 dihydrochloride), an aminonucleoside antibiotic, inhibits protein synthesis .
Enalapril-d3 (MK-421-d3) is deuterium labeled Enalapril. Enalapril (MK-421) is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research .
Olmesartan-d6 (RNH-6270-d6) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure .
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
Vapendavir-d5 is the deuterium labeled Vapendavir. Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
Flurbiprofen-d5 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
Aspartame-d3 is the deuterium labeled Aspartame. Aspartame (SC-18862) is a methyl ester of a dipeptide. Aspartame can be used as a synthetic nonnutritive sweetener. Aspartame is composed of phenylalanine (50%), aspartic acid (40%) and methanol (10%) .
Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium labeled Oxybenzone (HY-A0067). Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells .
Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity .
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Rupintrivir-d7 is a deuterated labeled Rupintrivir . Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect .
Goserelin-d7 (ICI 118630-d7) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Simvastatin-d6 (MK 733-d6) is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
Ertugliflozin-d5 is the deuterium labeled Ertugliflozin . Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2 . Has the potential for the treatment of type 2 diabetes mellitus .
Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Riociguat-d3 (BAY 632521-d3) is deuterium labeled Riociguat. Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
Methoprene-d7 is the deuterium labeled Methoprene . Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist .
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Chenodeoxycholic acid-d2 (CDCA-d2) is deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Teneligliptin-d5 (MP-513-d5) is deuterium labeled Teneligliptin. Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4(DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus [4] .
Spisulosine-d3 (ES-285-d3) is deuterium labeled Spisulosine (HY-13626). Spisulosine is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation. Spisulosine induces apoptosis in PC-3 and LNCaP cells .
Terbuthylazine-desethyl-d9 is the deuterium labeled Terbuthylazine-desethyl . Terbuthylazine-desethyl (Desethylterbuthylazine) is a chloro dealkylated metabolite of Terbuthylazine (a triazine herbicide) .
Probucol-d6 is deuterium labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
Deupirfenidone-d3 is the deuterium labeled Pirfenidone (HY-B0673). Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Brinzolamide-d5 (hydrochloride) is the deuterium labeled Brinzolamide hydrochloride . Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research .
Luliconazole-d3 (NND 502-d3) is deuterium labeled Luliconazole. Luliconazole (NND 502)?is a topical antifungal imidazole antibiotic with broad-spectrum and potent antifungal activity. Luliconazole can be used for the research of skin infection, including?dermatophytosis, tinea corporis, tinea pedis?et al .
Ethylenediaminetetraacetic acid-d16 is the deuterium labeled Ethylenediaminetetraacetic acid . Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds [4].
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
Cefditoren-d3 (sodium) (ME 1206-d3) is deuterium labeled Cefditoren (sodium). Cefditoren sodium (ME 1206) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren sodium has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren sodium can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections .
Quabodepistat-d7 (OPC-167832-d7) is deuterium labeled Quabodepistat. Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with?an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis?caused by?Mycobacterium tuberculosis .
Azimilide-d8 (NE-10064-d8) dihydrochloride is the deuterium labeled Azimilide dihydrochloride (HY-18600A). Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation [4].
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
Lauryl benzalkonium-d5 chloride (Dimethylbenzyllaurylammonium-d5 chloride) is the deuterium labeled Lauryl benzalkonium chloride (HY-B1549). Lauryl benzalkonium (Dimethylbenzyllaurylammonium) chloride is a cationic surfactant that may produce some irritant contact dermatitis (ICD) to the skin .
Mexiletine-d3 (KOE-1173-d3) is deuterium labeled Mexiletine. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research [4] .
Tonabersat-d6 (SB-220453-d6) is deuterium labeled Tonabersat. Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system .
Losartan-d6 hydrochloride is deuterated labeled Losartan potassium (HY-17512A). Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis [4] .
Valsartan-d3 is the deuterium labeled Valsartan . Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
Solabegron-d8 (GW 427353-d8) is deuterium labeled Solabegron. Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM . Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome .
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity .
Varespladib-d7 (LY315920-d7) is a deuterated labeled Varespladib (HY-13402). Varespladib is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM .
Oseltamivir-d3 (phosphate)eis the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Mycophenolic acid-d3 (Mycophenolate-d3) is deuterium labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
Amitraz-d6 (BTS-27419-d6) is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
DL-dithiothreitol-d10 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. When DL-dithiothreitol is oxidized, it forms a stable six-membered ring with an internal disulfide bond .
Crizotinib-d8 (PF-02341066-d8) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514) . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
Fostemsavir-d8 (BMS-663068-d8) is deuterium labeled Fostemsavir. Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.
Nemonoxacin-d3 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
1-Octanol-d2 is the deuterium labeled 1-Octanol . 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Enasidenib-d6 (AG-221-d6) is the deuterium labeled Enasidenib (HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Hydroxymetronidazole-d2 is the deuterium labeled Hydroxymetronidazole(HY-136440).Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle .
Imeglimin-d3 (EMD 387008-d3) is deuterium labeled Imeglimin. Imeglimin (EMD 387008) is an oral glucose-lowering agent. Imeglimin improves insulin sensitivity. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function .
Omeprazole-d3 (H 16868-d3) is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
Ambroxol-d5 (NA-872-d5) is deuterium labeled Ambroxol. Ambroxol (NA-872), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research .
Ampyrone-d3 is the deuterium labeled Ampyrone (HY-B1398). Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy .
Piroxicam-d3 (CP-16171-d3) is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively .
Debutyldronedarone-d7 is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans.Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent .
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
Eltrombopag-d3 (SB-497115-d3) is deuterium labeled Eltrombopag. Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well [4] .
Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
Prasugrel-d3 is the deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Glycoursodeoxycholic acid-d5 (Ursodeoxycholylglycine-d5) is the deuterium labeled Glycoursodeoxycholic acid (HY-N1424). Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid.
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
Ivacaftor-d18 is the deuterium labeled Ivacaftor . Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively .
Alfuzosin-d6 (SL 77499-d6) is deuterium labeled Alfuzosin. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) .
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
Ivosidenib-d5 (AG-120-d5) is deuterium labeled Ivosidenib. Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
Naproxen-d3 is the deuterium labeled Naproxen. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ethaboxam-d5 (Intego solo-d5) is the deuterium labeled Ethaboxam (HY-107492). Ethaboxam is a β-tubulin inhibitor that can be used as anti-oomycete fungicide .
Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Ergothioneine-d3 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant .
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) [4] .
Pirfenidone-d5 (AMR69-d5) is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
Sotalol-d6 is the deuterium labeled Sotalol. Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent [4].
Diflunisal-d3 is the deuterium labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
Methylprednisolone-d3 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels .
Famciclovir-d6 (BRL 42810-d6) is deuterium labeled Famciclovir. Famciclovir (BRL 42810) is an orally active nucleoside analogue. Famciclovir is an antiviral agent with potent activities against HBV, HSV and VZV. Famciclovir can be used for the research of herpesvirus infection .
2-Acetamidophenol-d3 (Orthocetamol-d3) is the deuterium labeled 2-Acetamidophenol (HY-W015600). 2-Acetamidophenol (Orthocetamol) is a regulator that targets ferroptosis and glutathione metabolic pathways, is the ortho-regioisomer of Paracetamol (HY-66005). 2-Acetamidophenol has anti-atherosclerotic activity, and inhibiting total cholesterol (TC) and triglyceride (TG) in a zebrafish hyperlipidemia model with IC50s for 30 μM and 40 μM, respectively. 2-Acetamidophenol upregulates the expression of glutathione synthesis-related genes (such as GCLC, GCLM, GSS) and iron ion transport genes (such as FPN1, FTH), reduces the accumulation of intracellular reactive oxygen species (ROS) and ferrous ions (Fe2+), and enhances the activity of glutathione peroxidase GPX4, thereby inhibiting macrophage phagocytosis of oxidized low-density lipoprotein (ox-LDL) and foam cell formation .
Afloqualone-d7 (HQ-495-d7) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome .
Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9) is the deuterium labeled Tylvalosin (HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
Ciprofloxacin-d8 (hydrochloride) is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Ropinirole-d7 hydrochloride is the deuterium labeled Ropinirole hydrochloride . Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Linezolid-d3 (PNU-100766-d3) is a deuterium labeled Linezolid (PNU-100766). Linezolid is a synthetic antibiotic that acts by inhibiting the initiation of bacterial protein synthesis .
Anisylacetone-d5 (p-Methoxybenzylacetone-d5) is deuterium labeled Anisylacetone. Anisylacetone (p-Methoxybenzylacetone) is a male fruit fly attractant .
Niclosamide-d3 (BAY2353-d3) is deuterium labeled Niclosamide. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells [4]. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction [4].
Dapoxetine-d7 (hydrochloride) is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI) .
Lusutrombopag-d13 is deuterium labeled Lusutrombopag. Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
Valdecoxib-d3 is the deuterium labeled Valdecoxib. Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain .
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Chenodeoxycholic Acid-d7 (CDCA-d7) is the deuterium labeled Chenodeoxycholic Acid (HY-76847). Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor .
Relebactam-d9 (MK-7655-d9) is deuterium labeled Relebactam. Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases and KPC) and class C (AmpC) enzymes. Relebactam shows antibacterial activity .
(±)-Duloxetine-d3 (hydrochloride) is deuterium labeled (±)-Duloxetine (hydrochloride). (±)-Duloxetine ((Rac)-Duloxetine) hydrochloride is the racemate of Duloxetine hydrochloride. Duloxetine hydrochloride, a serotonin-norepinephrine reuptake inhibitor, can be used for diabetic neuropathic pain and fibromyalgia as well as major depressive disorder research .
Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Niraparib-d5 (MK-4827-d5) is the deuterium labeled Niraparib (HY-10619). Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
Telcagepant-d8 (MK-0974-d8) is deuterium labeled Telcagepant. Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
Pazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Vericiguat-d6 (BAY1021189-d6) is deuterium labeled Vericiguat. Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
Ozenoxacin-d3 (hydrochloride) is the deuterium labeled Ozenoxacin hydrochloride. Ozenoxacin hydrochloride is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections .
Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
Penicillamine-d3 is the deuterium labeled Penicillamine. Penicillamine (D-(-)-Penicillamine) is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.
Triclabendazole-d3 is the deuterium labeled Triclabendazole (HY-B0621). Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors .
Pimozide-d5 (R6238-d5) is the deuterium labeled Pimozide (HY-12987). Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
Isoeugenol-d3 is deuterated labeled Isoeugenol (HY-N1952). Isoeugenol is an essential oil constituent of nutmeg, clove, and cinnamon. Isoeugenol inhibits growth of Escherichia coli and Listeria innocua with MICs of 0.6 mg/mL and 1 mg/mL, respectively .
Glycocyamine-d2 is the deuterium labeled Glycocyamine. Glycocyamine (Guanidinoacetic acid), a precursor of creatine, is a replacement of dietary arginine and could support overall energy homeostasis of the bird.
Brigatinib-d11 (AP-26113-d11) is deuterium labeled Brigatinib. Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC .
Ziprasidone-d88 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Albendazole-d7 is the deuterium labeled Albendazole. Albendazole is a broad-spectrum parasiticide with high effectiveness and low host toxicity. Albendazole is used for the research gastrointestinal parasites in humans and animals .
Eugenol acetate-d3 is the deuterated labeled Eugenol acetate (HY-W014612). Eugenol acetate (Eugenyl acetate) is an antibacterial, anticancer, anti-inflammatory and antioxidant. Eugenol acetate inhibits NF-κB and enhances the expression of p53 and p21 (WAF1). Eugenol acetate can prevent chemically induced skin cancer, inhibit cancer cell proliferation and induce apoptosis [4].
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Dexpanthenol-d6 is deuterium labeled D-Panthenol. D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .
Equilin-d2 (7-Dehydroestrone-d2) is deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism .
Ropinirole-d3 hydrochloride is the deuterium labeled Ropinirole hydrochloride . Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
DL-Arginine-d7 hydrochloride is deuterium labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Valsartan-d9 is deuterium labeled valsartan. Valsartan is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Biperiden-d5 (hydrochloride) is the deuterium labeled Biperiden hydrochloride. Biperiden (KL 373) hydrochloride is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
Nadifloxacin-d5 (OPC7251-d5) is deuterium labeled Nadifloxacin (HY-B0506). Nadifloxacin (OPC7251) is a broad-spectrum quinolone antibiotic. Nadifloxacin inhibits bacterial DNA gyrase and topoisomerase IV, interfering with DNA replication. It also suppresses the production of proinflammatory cytokines (such as IL-1α, IL-6, and IL-8). Nadifloxacin exhibits antibacterial activity against various pathogens, including Propionibacterium acnes and Staphylococcus aureus. Nadifloxacin also exhibits anti-inflammatory activity. Nadifloxacin can be used in the research of skin infections such as acne vulgaris, folliculitis, and impetigo [4] .
Tulobuterol-d9 (hydrochloride) is the deuterium labeled Tulobuterol. Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength .
Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4(M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
Tezacaftor-d6 (VX-661-d6) is deuterium labeled Tezacaftor. Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation [4].
Norfloxacin-d8 is the deuterium labeled Norfloxacin. Norfloxacin (MK-0366) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
Omeprazole sulfide-d3 is the deuterium labeled Omeprazole sulfide. Omeprazole metabolite Omeprazole sulfide (Ufiprazole) is a metabolite of Omeprazole, which is a proton pump inhibitor.
Tiludronate-d5 (sodium)mis the deuterium labeled Tiludronate disodium. Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties [4].
Ceftazidime-d5 is the deuterium labeled Ceftazidime. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
Methotrexate metabolite-d3 is the deuterium labeled Methotrexate metabolite. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent .
Ramelteon-d3 (TAK-375-d3) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
Eliglustat-d15 (Genz 99067-d15) is deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM .
DL-dithiothreitol-d6 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
Olodaterol-d3 hydrochloride (BI1744-d3 hydrochloride) is the deuterium labeled Olodaterol hydrochloride (HY-14301A). Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis .
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
Diltiazem-d6 (hydrochloride) (CRD-401-d6 (hydrochloride)) is deuterium labeled Diltiazem (hydrochloride). Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
Sucrose-d14 is the deuterium labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preferen
Chlortetracycline-d6 (hydrochloride) is the deuterium labeled Chlortetracycline hydrochloride. Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
Empagliflozin-d6 (BI 10773-d6) is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2 .
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
Ribociclib-d6 (LEE011-d6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Vilanterol-d12 (GW642444-d12) is deuterium labeled Vilanterol. Vilanterol (GW642444) is a long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM .
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor [4] .
DL-Phenylephrine-d3 hydrochloride ((±)-Phenylephrine-d3 hydrochloride) is the deuterium labeled DL-Phenylephrine hydrochloride (HY-W014726). DL-Phenylephrine ((±)-Phenylephrine) hydrochloride is a selective agonist of the alpha1-adrenergic receptor, exhibiting potent vasoconstrictive activity.
Dronedarone-d6 (SR 33589-d6) is deuterium labeled Dronedarone. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4 .
Tenidap-d3 is the deuterium labeled Tenidap. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties . Tenidap is also a specific SLC26A3 inhibitor .
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker .
Etiracetam-d3 is the deuterium labeled Etiracetam. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .
Pemigatinib-d6 (INCB054828-d6) is deuterium labeled Pemigatinib. Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma .
Tetramethylthiuram Monosulfide-d12 (TMTM-d12) is the deuterium labeled Tetramethylthiuram monosulfide (HY-W020246). Tetramethylthiuram monosulfide (TMTM) is an active compound. Tetramethylthiuram monosulfide (TMTM) can be used for the research of rubber and various biochemical studies .
Medetomidine-d3 (hydrochloride) is the deuterium labeled Medetomidine hydrochloride. Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor .
Nicardipine-d3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure .
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Radotinib-d6 is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .
Moxonidine-d3 (BDF5895-d3) is deuterium labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis [4] .
Dimesna-d8 (BNP-7787-d8) is the deuterium labeled Dimesna (HY-B1022). Dimesna combined with anticancer chemotherapeutic agents to reduce nephrotoxicity.
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Aripiprazole-d8 (OPC-14597-d8) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.
Ribociclib-d8 is the deuterium labeled Ribociclib . Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Itraconazole-d9 is the deuterium labeled Itraconazole . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor [4] .
Cilnidipine-d7 is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel [4]. Antihypertensive effects .
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
Ciprofloxacin-d8 (hydrochloride monohydrate) is the deuterium labeled Ciprofloxacin (hydrochloride monohydrate). Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Raltegravir-d3 (potassium) is the deuterium labeled Raltegravir potassium. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection .
Sodium 2-oxopropanoate-d3 is the deuterium labeled Sodium 2-oxopropanoate . Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS .
Terbinafine-d3 hydrochloride is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM . Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria .
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Isoxepac-d6 (HP 549-d6) is the deuterium labeled Isoxepac (HY-W050088). Isoxepac (HP 549) is an orally active non-steroidal anti-inflammatory agent. Isoxepac can inhibit Carrageenan (HY-125474) paw oedema, adjuvant-induced polyarthritis, and prostaglandin synthesis. Isoxepac (200 mg) has an analgesic effect after meniscectomy with a low incidence of side effects. Isoxepac can be used in the research of inflammatory (rheumatoid arthritis) and pain-related diseases .
Ciprofloxacin-d8 is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Acetohydrazide-d3 (Ethanehydrazonic acid-d3) is deuterium labeled Acetohydrazide. Acethydrazide is an organic building that undergo catalytic hydrogenation to produce N′-methyl acethydrazide (MAH) .
Imiquimod-d7 (R 837-d7) is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Acetylpyrazine-d3 is deuterated labeled Acetylpyrazine (HY-W007692). Acetylpyrazine (2-Acetylpyrazine) is used to form many polycyclic compounds, as useful structures in pharmaceuticals and perfumes. Acetylpyrazine is a component of the folates (vitamin B compounds) .
HMMNI-d3 (Hydroxy Dimetridazole-d3) is deuterium labeled HMMNI (HY-W008216). HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazol (HY-B1244). Dimetridazole is a nitroimidazole class agent that combats protozoan infections .
Sildenafil-d5 (UK-92480-d5) is deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) [4] .
Debutyldronedarone-d6 (hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent .
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [4].
Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
Venlafaxine-d9 (Wy 45030-d9) is a deuterium labeled Venlafaxine (HY-B0196). Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
Valsartan-d8 is the deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Posaconazole-d7 (SCH 56592-d7) is deuterium labeled Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Danicamtiv-d3 (MYK-491-d3) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
Mexiletine-d6 (KOE-1173-d6) is deuterium labeled Mexiletine. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research [4] .
Methylprednisolone-d7 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels .
Elesclomol-d2 (STA-4783-d2) is a deuterium labeled Elesclomol (HY-12040). Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research [4].
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
Ensifentrine-d6 (RPL-554-d6) is deuterium labeled Ensifentrine. Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
Selpercatinib-d3 (LOXO-292-d3) is deuterium labeled Selpercatinib. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity .
Sarafloxacin-d8 (A-56620-d8) hydrochloride is the deuterium labeled Sarafloxacin hydrochloride. Sarafloxacin hydrochloride (A-56620 hydrochloride) is a quinolone antibiotic drug.
Cilostazol-d2 (OPC 13013-d2) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM . Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria .
Cilostazol-d6 (OPC 13013-d6) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors [4].
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Posaconazole-d3 (SCH 56592-d3) is deuterium labeled Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Ketoprofen-d3 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively .
Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .
Carteolol-d9 (hydrochloride) is the deuterium labeled Carteolol hydrochloride. Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma .
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
Lisinopril-d5 is the deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation [4] .
Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Atenolol-d7 is the deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris .
Tazarotene-d8 is the deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris .
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis .
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment .
Donepezil-d7 (hydrochloride) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .
Bendamustine-d7 hydrochloride (SDX-105-d7) is the deuterium labeled Bendamustine hydrochloride (HY-B0077). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule?depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of?bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity .
Adinazolam-d5 (U 41123-d5) is a deuterium labeled Adinazolam (HY-A0198). Adinazolam is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities .
Puromycin-d3 is the deuterium labeled Puromycin. Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
Betaxolol-d7 (hydrochloride) is the deuterium labeled Betaxolol hydrochloride. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
Ethylenediaminetetraacetic acid-d12 is the deuterium labeled Ethylenediaminetetraacetic acid . Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds [4].
Evogliptin-d9 (DA-1229-d9) is deuterium labeled Evogliptin. Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation [4].
Elagolix-d6 (sodium) (NBI-56418-d6 (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. [4] .
Hyodeoxycholic acid-d5 is the deuterium labeled Hyodeoxycholic acid. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
Doxazosin-d8 is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors .
Sunitinib-d10 (SU 11248-d10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively) .
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor .
Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Ponatinib-d8 (AP24534-d8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Rabeprazole-d3 sodium the deuterium labeled Rabeprazole sodium (HY-B0656A). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an b>IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
Cinacalcet-d3 (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [4] .
Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
1-PalMitoyl-2-arachidoyllecithin-d9-1 (1-Palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine-d9-1) is deuterium labeled 1-PalMitoyl-2-arachidoyllecithin. 1-Palmitoyl-2-arachidonoyl-sn-glycero-3-PC (PAPC) is a phospholipid containing palmitic acid (16:0) and arachidonic acid (20:4) at the sn-1 and sn-2 positions, respectively, that is found in biological membranes. PAPC is oxidized in vivo, and its oxidation products are involved in chronic inflammation and vascular disease. PAPC has been used to study signaling of oxidized phospholipids. Levels of PAPC are decreased in isolated human multiple myeloma cells .
Sanguinarine chloride- 13C,d3 (Sanguinarin chloride- 13C,d3) is the deuterium labeled Sanguinarine chloride (HY-N0052A). Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
Bosutinib- 13C,d3 (SKI-606- 13C,d3) is 13C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively .
Iloperidone- 13C,d3 (HP 873- 13C,d3) is 13C labeled Iloperidone. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms .
dGTP- 15N5 (2'-Deoxyguanosine-5'-triphosphate- 15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Ethyl linoleate- 13C18 is the 13C labeled Ethyl linoleate. Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Adenosine 5'-diphosphate- 13C5 (Adenosine diphosphate- 13C5) is the 13C-labeled Adenosine 5'-diphosphate (HY-W010918). Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
Ethynyl Estradiol- 13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Miconazole-d5 (nitrate) (2,4-Dichlorobenzyloxy-d5) is the deuterium labeled Miconazole nitrate. Miconazole nitrate (R18134 nitrate) is an imidazole antifungal agent. Miconazole nitrate also has antibacterial effects .
(Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
Adenine- 15N5 (6-Aminopurine- 15N5; Vitamin B4- 15N5) is 15N labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Levoglucosan-d7 is the deuterium labeled Levoglucosan. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature .
Thiamine- 13C3 (hydrochloride) is the 13C-labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Nε,Nε,Nε-Trimethyllysine-d9 (chloride) is the deuterium labeled Nε,Nε,Nε-Trimethyllysine (chloride) . Nε,Nε,Nε-Trimethyllysine chloride serves as a precursor for gut flora-dependent formation of N,N,N-trimethyl-5-aminovaleric acid (TMAVA) .
Butylparaben- 13C6 is the 13C labeled Butylparaben . Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
Adenosine monophosphate- 13C10, 15N5 (AMP- 13C10, 15N5) is the 13C- and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
2'-Deoxyadenosine-5'-triphosphate- 15N5,d14 (dATP- 15N5,d14) dilithium is deuterium and 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Adenine-15N5 hydrochloride hydrate (6-Aminopurine-15N5 hydrochloride hydrate) is the deuterium labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis .
Adenine- 13C5 (6-Aminopurine- 13C5; Vitamin B4- 13C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
AalphaC- 15N3 (2-Amino-α-carboline- 15N3) is 15N labeled AalphaC. AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
L-DOPA- 13C6 is the 13C-labled L-DOPA . L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease [4].
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al [4] .
Cobimetinib- 13C6 (GDC-0973- 13C6; XL518- 13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078) . Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor .
1-Stearoyl-sn-glycero-3-phosphocholine-d35 is deuterium labeled 1-Stearoyl-sn-glycero-3-phosphocholine (HY-125771). 1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylate is the deuterium labeled Rasagiline (mesylate) (HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
N,N-dimethyl-N′-p-tolylsulfamide-d7(4-Dimethylaminosulfotoluidide-d7; N,N-Dimethyl-N-Tolylsulfonyldiamide-d7) is the deuterium labeled N,N-dimethyl-N′-p-tolylsulfamide (HY-W286414).
Dapsone- 15N2 (4,4′-Diaminodiphenyl sulfone- 15N2) is 15N labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
Dabigatran- 13C6 is the 13C labeled Dabigatran . Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
Riboflavin- 13C5 is the 13C-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Neopterin- 13C5 (D-(+)-Neopterin- 13C5; D-erythro-Neopterin- 13C5) is the deuterium labeled Neopterin (HY-W040055) . Neopterin (D-(+)-Neopterin), a catabolic product of guanosine triphosphate (GTM), serves as a marker of cellular immune system activation .
dGTP- 15N5,d14 (2'-Deoxyguanosine-5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
(±)-1,2-Propanediol- 13C3 is 13C labeled (±)-1,2-Propanediol (HY-Y0921). (±)-1, 2-propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol that is often used as an excipient in many active molecular preparations to increase the solubility and stability of the active molecule. (±)-1, 2-propanediol can affect the neurobehavior of zebrafish .
C18 Dihydroceramide-d3-1 (N-octadecaoyl-D-eytho-Dihydosphigosie-d3) is deuterium labeled C18 Dihydroceramide. C18 Dihydroceramide is an ester product .
Oseltamivir acid-13C,d3 (GS 4071-13C,d3; Ro 64-0802-13C,d3) is a 13C- and deuterium-labeled Oseltamivir acid (HY-13318). Oseltamivir acid is the active metabolite of Oseltamivir phosphate and inhibits influenza virus neuraminidase (IC50=2 nM). Oseltamivir acid is orally active and can be used to study influenza A/B infections [4] .
Artemether- 13C,d3 (Dihydroqinghaosu methyl ether- 13C,d3) is the deuterium and 13C-labeled Artemether (HY-N0402). Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria .
Menaquinone-7- 13C6 is the 13C-labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors . Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS) .
2'-Deoxycytidine-5'-monophosphoric acid- 15N3 is the 15N labeled 2'-Deoxycytidine-5'-monophosphoric acid . 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
Cefotiam- 13C, 15N2 (SCE-963- 13C, 15N2) is the 13C- and 15N-labeled Cefotiam (HY-B0734). Cefotiam (SCE-963) is a parenteral cephalosporin antibiotic. Cefotiam has broad-spectrum activity against Gram-positive and Gram-negative bacteria .
N6-Methyladenosine- 13C3 (6-Methyladenosine- 13C3) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities .
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels [4].
N-Acetyl mesalazine-d3-1 (N-Acetyl-5-aminosalicylic acid-d3-1) is deuterium labeled N-Acetyl mesalazine (HY-66008). N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the primary intestinal metabolite of 5-Aminosalicylic Acid (HY-15027) and serves as a biomarker for evaluating the efficacy of 5-Aminosalicylic Acid (HY-15027). N-Acetyl mesalazine can scavenge free radicals, reduce DNA base hydroxylation, and ameliorate mucosal inflammation. N-Acetyl mesalazine can be used in the study of diseases such as colitis and colon cancer .
Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death .
L-Glutathione reduced-d5 (GSH-d5) ammonium is the deuterium labeled L-Glutathione reduced (HY-D0187). L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
Exemestane- 13C,d2 is 13C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Tofacitinib- 13C,d3 (Tasocitinib- 13C,d3) is 13C labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
ATP- 13C10, 15N5 is the 13C and 15N labeled ATP . ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation .
Mitotane- 13C6 is the 13C labeled Mitotane . Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [4] .
Uridine-13C9,15N2 (β-Uridine-13C9,15N2) is 13C and 15N labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Zearalenone- 13C7 (Mycotoxin F2- 13C7) is 13C labeled Zearalenone. Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts .
Cytidine-d2-1 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catech
Ethyl Paraben- 13C6 (Ethyl parahydroxybenzoate- 13C6) is 13C labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Betaine- 13C3 (Trimethylglycine- 13C3) is the 13C labeled isotope of Betaine (HY-B0710). Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns [1,2]. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity .
Ritonavir- 13C,d3 is the 13C- and deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Folic acid-13C6 is a deuterated labeled Folic acid . Folic acid (Vitamin B9) is a orally active essential nutrient from the B complex group of vitamins. Folic acid shows antidepressant-like effect. Folic acid sodium reduces the risk of neonatal neural tube defects. Folic acid can be used to the research of megaloblastic and macrocytic anemias due to folic deficiency [4] .
L-Ascorbic acid- 13C6 is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor . L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells [4].
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor . Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
17α-Hydroxyprogesterone- 13C3 is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
rU Phosphoramidite- 13C2,d1 (DMT-2'O-TBDMS-rU phosphoramidite- 13C2,d1) is deuterium and 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Folic acid- 13C5 is the 13C-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
D-Mannitol- 13C,d2 is the deuterium and 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Ornidazole- 13C2, 15N2 is the 13C, 15N labeled Ornidazole. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease .
N-Acetylneuraminic Acid- 13C,d3 (N-Acetyl-β-D-neuraminic acid- 13C,d3) is the deuterium labeled and 13C-labeled N-Acetyl-β-D-neuraminic acid (HY-75278).
Levulinic acid- 13C3 (4-Oxovaleric acid- 13C) is the 13C-labeled Levulinic acid (HY-Y0839). Levulinic acid is a precursor for the synthesis of biofuels, such as ethyl levulinate. Levulinic acid is also a 5-keto-pentanoic acid. Levulinic acid can be utilized by the cells as a cosubstrate for biopolymer synthesis. Levulinic acid can be used in antibacterial research .
Zearalenone- 13C18 (Mycotoxin F2- 13C18; Toxin F2- 13C18) is the 13C labeled Zearalenone (HY-103447) . Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts .
Mandelic Acid- 13C8 ((±)-Mandelic acid- 13C8) is the 13C-labeled Mandelic acid (HY-W015591). Mandelic acid ((±)-Mandelic acid), an alpha-hydroxycarboxylic acid, has been widely used as an intermediate of pharmaceutical and fine chemicals. Mandelic acid shows antimicrobial activity and has been used for the research of urinary tract infections and vaginal trichomoniasis. Mandelic acid exhibits high sperm-immobilizing activity and low vaginal irritation .
Doxorubicinone- 13C,d3 (Adriamycin aglycone- 13C,d3) is 13C labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
Uridine 5'-monophosphate- 15N2,d11 (5'- Uridylic acid- 15N2,d11) dilithium is deuterium and 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa [4] .
Mitotane- 13C12 (2,4′-DDD- 13C12) is 13C labeled Mitotane. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [4][4] .
Propyl paraben- 13C6 (Propyl parahydroxybenzoate- 13C6) is 13C labeled Propylparaben. Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods. Propylparaben disrupts follicular growth and steroidogenic function by altering cell cycle, apoptosis and steroidogenic pathways. Propylparaben also reduced sperm count and motility in rats [4] .
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
Trans-Anethole-d3 is deuterated labeled Trans-Anethole (HY-N0367). Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor [4] .
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
Tricaine-d5 methanesulfonate is the deuterium labeled Tricaine methanesulfonate (HY-W011777). Tricaine methanesulfonate (MS-222) is a commonly used agent that can suppress or relieve pain. agent for immobilization of aquatic species. Tricaine methanesulfonate, the most widely used agent that can suppress or relieve pain. in fish, has been shown to induce embryotoxic effects in zebrafish .
Phenylglyoxylic acid-d5 (Benzoylformic acid-d5) is a deuterium labeled Phenylglyoxylic acid (HY-W010255). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human. Phenylglyoxylic acid can be used as drug intermediate for synthesis of antineoplastic compounds .
2,6-Dimethoxyphenol-d6 (Syringol-d6) is deuterated labeled 2,6-Dimethoxyphenol (HY-W003972). 2,6-Dimethoxyphenol is a phenolic compound that scavenges free radicals and exhibits antioxidant activity. 2,6-Dimethoxyphenol is the substrate for determining laccase activity .
Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Hydroxy Itraconazole-d6 (R-63373-d6) is deuterium labeled Hydroxy Itraconazole. Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
Pentyl 4-hydroxybenzoate-d11 (Amylparaben-d11) is the deuterium labeled Pentyl 4-hydroxybenzoate (HY-W267444). Pentyl 4-hydroxybenzoate (Amylparaben) is a type of paraben compound commonly used as a preservative, it has antibacterial properties and is related to the inhibition of induced oxygen consumption .
(Rac)-Levomepromazine-d3 (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors .
Ornidazole-d5 is deuterium labeled Ornidazole. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease .
Octanoic acid-d15 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Lignoceric acid-d3 is the deuterium labeled Lignoceric acid . Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research .
Piperonyl butoxide-d9 is the deuterium labeled Piperonyl butoxide.Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice [4].
Amifampridine-d3(3,4-Diaminopyridine-d3) is deuterium labeled Amifampridine. Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research .
Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8 .
Nanofin-d2 (2,6-Lupetidine-d2) is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
CX516-d10 is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) .
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Metazachlor-d6 (BAS 479H-d6) is a deuterium labeled Metazachlor (HY-136373). Metazachlor (BAS 479H) is a herbicide belonging to the chloroacetamides class. Metazachlor can inhibit the synthesis of very long chain fatty acids during the germination and emergence of weed seeds, thereby interfering with cell division and tissue differentiation, and thus hindering the normal growth and development of weeds .
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Farnesyl pyrophosphate-d3 (Farnesyl diphosphate-d3) is a deuterium labeled Farnesyl pyrophosphate (HY-113037B). Farnesyl pyrophosphate is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
Aripiprazole (1,1,2,2,3,3,4,4-d8) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM .
Deruxtecan-d5 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
DPPC-d66 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Alfuzosin-d7 (hydrochloride) is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Scopolamine-d3 hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc [4] .
Djalonensone-d3 is a deuterium labeled Djalonensone (HY-W013863). Djalonensone, isolated from the roots of Anthocleista djalonensis (Loganiaceae), is an important taxonomic marker of the plant species .
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Cariprazine-d8-1 (RGH-188-d8-1) is the deuterium labeled Cariprazine (HY-14763). Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma .
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
Stigmasterol-d5-1 is deuterium labeled Stigmasterol. Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases .
Ketotifen-d3 (HC 20-511-d3) is deuterium labeled Ketotifen. Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention [4].
DPPC-d75 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Nonanoic acid-d3 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Cyfluthrin-d6 (β-Cyfluthi-d6) is deuterium labeled Cyfluthrin. Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product .
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
trans-Stilbene-d10 ((E)-Stilbene-d10) is the deuterium labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
D-Leucine-d10 is the deuterium labeled D-Leucine. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro .
Arachidic acid-d2 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Parecoxib-d5 sodium is the deuterium labeled Parecoxib sodium. Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo .
Levocarnitine propionate-d9 hydrochloride (L-Propionylcarnitine-d9 chloride) is deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride is used to study diseases such as renal function deterioration, congestive heart failure, and intermittent claudication .
Homovanillic acid-d5 (Vanilacetic acid-d5) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage .
N-Arachidonylglycine-d8 is a deuterated labeled N-Arachidonylglycine . N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration .
Banoxantrone-d12 is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Vortioxetine-d3 (Lu AA 21004-d3) is a deuterium labeled Vortioxetine (HY-15414). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
Tenofovir alafenamide-d6 (GS-7340-d6) is deuterium labeled Tenofovir alafenamide. Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor .
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
Dabigatran etexilate-d11 (BIBR 1048-d11) is the deuterium labeled Dabigatran etexilate (HY-10274). Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation .
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
Apixaban-d3 (BMS-562247-01-d3) is the deuterium labeled Apixaban (HY-50667) . Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590), is the first deuterium approved worldwide for the research of Huntington's disease, or other hyperkinetic movement disorders .
Nimodipine-d7 is the deuterium labeled Nimodipine. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders .
Fosetyl-aluminum-d15 (Fosetyl-Al-d15) is the deuterium labeled Fosetyl-aluminum. Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops .
Prednisolone acetate-d8 is the deuterium labeled Prednisolone acetate. Prednisolone acetate (Prednisolone 21-acetate) is an adrenal cortico hormones, with anti-inflammatory, anti-allergic and immune suppressive effects.
Docosanoic acid-d2 (Behenic acid-d2) is deuterium labeled Docosanoic acid (HY-W013049).
Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Lignoceric acid-d47 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research .
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
N-Desbutyl bupivacaine-d6 (Desbutylbupivacaine-d6) is the deuterium labeled N-Desbutyl Bupivacaine (HY-W045132). N-Desbutyl Bupivacaine (compound 100) is a metabolite of Bupivacaine (HY-B0405), an NMDA receptor inhibitor and SCN5A antagonist .
(S)-(+)-Ibuprofen-d3 is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects .
Taurocholic acid-d5 (Taurocholic Acid-d5) is deuterium labeled Taurocholic acid. Taurocholic acid (N-Choloyltaurine) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid has immunoregulation effect .
Farnesyl pyrophosphate-d6 (Farnesyl diphosphate-d6) is a deuterium labeled Farnesyl pyrophosphate (HY-113037B). Farnesyl pyrophosphate is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Decanoyl-L-carnitine-d3 ((-)-Decanoylcarnitine-d3) is deuterium labeled Decanoyl-L-carnitine. Decanoyl-L-carnitine has stimulatory effect on the formation of desaturated fatty acid metabolites from both [1- 14C]-22:4 (n-6) and [1- 14C]-22:5 (n-3) .
Granisetron-d6 (BRL 43694-d6) is deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
2,6-Dimethoxyphenol-d3 (Syringol-d3) is the deuterium labeled 2,6-Dimethoxyphenol (HY-W003972) . 2,6-Dimethoxyphenol is a phenolic compound that scavenges free radicals and exhibits antioxidant activity. 2,6-Dimethoxyphenol is the substrate for determining laccase activity .
Azelaic acid-d14 is the deuterium labeled Azelaic acid . Azelaic acid is an organic compound produced by the ozonolysis of oleic acid;component of a number of hair and skin conditioners .
L-Valine-d1 ((S)-Valine-d1) is the deuterium labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
(S)-Lisinopril-d5 (sodium) (MK-521-d5 (sodium)) is deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
1-Phenylpyrrole-d9 (N-Phenylpyrrole-d9) is the deuterium labeled 1-Phenylpyrrole (HY-124891). 1-Phenylpyrrole (N-Phenylpyrrole) has dual fluorescent properties. 1-Phenylpyrrole displays a single band in nonpolar solvents and a second red-shifted fluorescent band in polar solvents .
Homovanillic acid-d3 (Vanilacetic acid-d3) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
N-(2,6-Dimethylphenyl)-2-(piperazin-1-yl)acetamide-d6 (N-[(2-chlorophenyl)carbamoyl]phenylalanine-d6) is deuterium-labeled CVT-2738 (HY-W009512). CVT-2738 is an orally active metabolite of Ranolazine (HY-B0280). CVT-2738 has a protective effect against isoprenaline (HY-108353)-induced myocardial ischemia in mice. CVT-2738 can be used in myocardial ischemia research .
Octanoic acid-d3 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .
1-Eicosanol-d41 (Arachidyl alcohol-d41) is the deuterium labeled 1-Eicosanol (HY-W004263) . 1-Eicosanol is a natural compound with antioxidant activity found in Justicia insularis leaves. 1-Eicosanol can be used as an antioxidant .
Mometasone furoate-d3 is a deuterium labeled Mometasone furoate. Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity .
Veratrole-d6 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Cyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
Prednisone acetate-d3 is the deuterium labeled Prednisone acetate. Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties .
Octanoic acid-d2 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Propofol-d14 (2,6-Diisopropylphenol-d14) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
Oxcarbazepine-d8-1 is a deuterium of Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Oxcarbazepine-d8-1 has anti-cancer and anticonvulsant effects .
Cilazapril-d5 (Ro 31-2848-d5) trifluoroacetate is the deuterium labeled Cilazapril (HY-A0043). Cilazapril is an angiotensin-converting enzyme (ACE) inhibitor used for the study of hypertension and congestive heart failure.
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
Ethyl acetoacetate-d5 is the deuterium labeled Ethyl acetoacetate . Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds [4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm .
L-Arginine-d7 (hydrochloride) is the deuterium labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Octanoic acid-d5 is the deuterium labeled Octanoic acid . Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Eslicarbazepine-d3 (BIA 2-194-d3) is the deuterium labeled Eslicarbazepine (HY-114703). Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
Uridine-d12 (β-Uridine-d12) is the deuterium labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Docosanoic acid-d43 (Behenic acid-d43) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Taurochenodeoxycholic acid-d5 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
Deruxtecan-d2 is the deuterium labeled Deruxtecan (HY-13631E) . Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
eCF506-d5 (NXP900-d5) is deuterated labeled eCF506 (HY-112096). eCF506 is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer .
Ulipristal acetate-d3 (CDB-2914-d3) is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma .
Pyridoxal Phosphate-d3 is the deuterium labeled Pyridoxal 5'-phosphate. Pyridoxal 5'-phosphate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′-phosphate (PMP) .
Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). Carbidopa, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
Nanofin-d5 (2,6-Lupetidine-d5) is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
Calcium phosphorylcholine-d9 (chloride) is the deuterium labeled Calcium phosphorylcholine chloride. Calcium phosphorylcholine chloride is the main phospholipid component in eukaryotic biofilms. Calcium phosphorylcholine chloride exists in commensal or pathogenic bacteria associated with eukaryotes in prokaryotes. Calcium phosphorylcholine chloride exhibits a surprising range of immunomodulatory properties .
Isradipine-d6 is the deuterium labeled Isradipine . Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease [4].
Homovanillic acid-d2 (Vanilacetic acid-d2) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
Ethyl palmitate-d31 is the deuterium labeled Ethyl palmitate. Ethyl palmitate, a fatty acid ethyl ester (FAEE), shows a marked preference for the synthesis of ethyl palmitate and ethyl oleate over other FAEEs in human subjects after ethanol consumption. Ethyl palmitate is used as a hair- and skin-conditioning agent .
N,N-Dimethylacetamide-d3 is the deuterium labeled N,N-Dimethylacetamide . N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent .
Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells .
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
N,N-Dimethylacetamide-d6 is the deuterium labeled N,N-Dimethylacetamide . N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent .
trans-Stilbene-d12 ((E)-Stilbene-d12) is the deuterium labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
Moroxydine hydrochloride-d8 (ABOB hydrochloride-d8) is the deuterium labeled Moroxydine (ABOB) hydrochloride (HY-B0420A). Moroxydine hydrochloride is a broad-spectrum agent with multi-antiviral activities against DNA and RNA viruses, including influenza virus, herpes simplex, varicella zoster, measles, mumps disease, hepatitis C virus, etc. Moroxydine hydrochloride exhibits excellent antiviral activity and shows low cytotoxicity to cells infected by dsRNA viruses (grass carp reovirus, GCRV) and large DNA viruses (giant salamander iridovirus, GSIV). Moroxydine hydrochloride blocks the GCRV-induced cytopathic effects and eliminates nucleocapsids in ctenopharyngodon idella kidney (CIK) cells to keep the normal morphological structure. Moroxydine hydrochloride significantly inhibits the apoptosis, the caspase 3 activity, Bax expression and down-regulates Bcl-2 levels [1][2][3].
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
ar-Turmerone-d3 is the deuterium labeled ar-Turmerone. ar-Turmerone ((+)-ar-Turmerone) is an orally active and major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities. ar-Turmerone induces apoptosis in U937 cells. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation in vitro and in vivo, and can be used for various neurologic disorders study [4] .
Arachidic acid-d3 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
D-Serine-d3 ((R)-Serine-d3) is a deuterium labeled D-Serine (HY-100808). D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration .
Velpatasvir-d3 (GS-5816-d3) is deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases [4].
Alfuzosin-d3 hydrochloride is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Daurisoline-d5 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Candesartan Cilexetil-d11 (TCV-116-d11) is deuterium labeled Candesartan Cilexetil. Candesartan Cilexetil (TCV-116) is an angiotensin II receptor inhibitor. Candesartan Cilexetil ameliorates the pulmonary fibrosis and has antiviral and skin wound healing effect. Candesartan Cilexetil can be used for the research of high blood pressure [4] .
Octreotide-d8 (SMS 201-995-d8) is deuterium labeled Octreotide. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
Abiraterone acetate-d3 (CB7630-d3) is deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598) .
Granisetron-d6 (Hydrochloride) (BRL 43694A-d6) is deuterium labeled Granisetron (Hydrochloride). Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
Tetraethylammonium bromide-d20 (TEA bromide-d20) is the deuterium labeled Tetraethylammonium bromide (HY-W014408). Tetraethylammonium bromide is a quaternary ammonium salt consisting of a positively charged tetraethylammonium cation and a negatively charged bromide anion. This compound is commonly used as a phase transfer catalyst in organic chemical reactions, facilitating the transfer of reactants between immiscible phases. It can also be used as a reagent for the synthesis of various organic compounds, an electrolyte in electrochemical experiments, and a source of tetraethylammonium ions in biochemical and pharmacological research.
Phenytoin-d5 (5,5-Diphenylhydantoin-d5) is deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
Taurochenodeoxycholic acid-d9 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively [4].
Prosulfocarb-d7 (S-Benzyl dipropylthiocarbamate-d7) is deuterium labeled Prosulfocarb. Prosulfocarb is a herbicide with a rapidly growing use trend. Prosulfocarb is used in winter cereals to help address the problem of increasing biotic resistance of weeds to certain pesticides. Environmental and food effects of prosulfocarb have been observed, and its transfer pattern from target crops to non-target areas has been studied. The volatility effect of prosulfocarb is an important factor explaining the inefficiency of isolated area contamination and marginal protection against residue spread .
Adipic acid-d10 (Hexanedioic acid-d10) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Veratrole-d2 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Cyclohexanecarboxylic acid-d11 is the deuterium labeled Cyclohexanecarboxylic acid . Cyclohexanecarboxylic acid is a Valproate structural analogue with anticonvulsant action .
Fosinopril-d5 (SQ28555-d5 (free acid)) is deuterium labeled Fosinopril. Fosinopril (SQ28555 free acid) is the ester proagent of angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an Ki value of 1.675 μM .
Tolcapone-d7 (Ro 40-7592-d7) is the deuterium labeled Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4].
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
Octreotide-d8 (acetate) (SMS 201-995-d8 (acetate)) is deuterium labeled Octreotide. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
DPPC-d71 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Butamben-d9 is the deuterium labeled Butamben. Butamben (Butyl 4-aminobenzoate) results in long-lasting relief from pain, without impairing motor function or other sensory functions .
9-Fluorenol-d9 (9-Hydroxyfluorene-d9) is the deuterium labeled 9-Fluorenol (HY-W016388). 9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 μM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo .
Trihydroxycholestanoic acid-d5 (Coprocholic acid-d5) is deuterium labeled Trihydroxycholestanoic acid. Trihydroxycholestanoic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Refsum Disease, D Bifunctional Protein Deficiency and Infantile Refsum Disease [4][4] .
Tazarotenic acid-d6 is deuterium labeled Tazarotenic acid. Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
Cyproheptadine hydrochloride-d3 (Cyproheptadine HCl-d3) is the deuterium labeled Cyproheptadine hydrochloride (HY-B0366A). Cyproheptadine hydrochloride is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders .
Suberic acid-d12 is the deuterium labeled Suberic acid . Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency .
Tropicamide-d3 is the deuterium labeled Tropicamide . Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
Myrcene-d6 is the deuterium labeled Myrcene. Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity [4] .
(S)-Lisofylline-d5 ((S)-Lisophylline-d5) is the deuterium labeled (S)-Lisofylline (HY-109854). (S)-Lisofylline is a kind of Lisofline enantiomer with optical activity. (S)-Lisofylline can interconversion with pentoxifylline .
Tenofovir alafenamide-d5 fumarate (GS-7340-d5 fumarate) is the deuterium labeled Tenofovir alafenamide fumarate (HY-15232A). Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Nanofin-d2 (2,6-Lupetidine-d2) hydrochloride is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
1-Undecanol-d23 (Undecyl alcohol-d23) is the deuterium labeled 1-Undecanol (HY-W004292). 1-Undecanol (Undecyl alcohol) is the main product generated from the degradation of 2-tridecanone by Pseudomonas bacteria isolated from the soil. 1-Undecanol can enhance the attraction of Grapholita molesta to sex pheromone traps .
Banoxantrone-d12 (dihydrochloride) is the deuterium labeled Banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Finerenone-d5 (BAY 94-8862-d5) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
Benserazide-d3 (hydrochloride) is the deuterium labeled Benserazide hydrochloride (HY-B0404A). Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma .
TRIA-662-d3 is the deuterium labeled TRIA-662 . TRIA-662 (1-Methylnicotinamide chloride) is an endogenous metabolite. TRIA-662 shows antithrombotic and anti-inflammatory activities .
Veratrole-d10 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Gliquidone-d6 is deuterium labeled Gliquidone. Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Benazepril-d5 hydrochloride is deuterium labeled Benazepril hydrochloride. Benazepril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy .
Nisoldipine-d3 is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.
Tempol-d17 is the deuterium labeled Tempol . Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS) .
Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4 .
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
(±)-Carnitine-d9 (chloride) is the deuterium labeled (±)-Carnitine chloride. (±)-Carnitine chloride exists in two isomers, known as D and L. L-carnitine plays an essential role in the β-oxidation of fatty acids and also shows antioxidant, and anti-inflammatory activities.
D-Valine-d8 is the deuterium labeled D-Valine. D-Valine is the enantiomer of L-Valine (HY-N0717). L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid.
Arachidic acid-d39 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Nitrendipine-d5 is the deuterium labeled Nitrendipine (HY-B0424). Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma [4] .
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
trans-Stilbene-d2 ((E)-Stilbene-d2) is the deuterium labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
Hydroxy Itraconazole-d8 is the deuterium labeled Hydroxy Itraconazole (HY-12772). Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
Salmeterol-d5 is a deuterated labeled Salmeterol . Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata .
SAR405838-d10 (MI-77301-d10) is the deuterium labeled SAR405838 (HY-18986). SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity .
Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties .
Muscarine-d9 (iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist .
Silybin B-d3 (Silibinin B-d3) is a deuterated Silybin B (HY-N7046). Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity [4].
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
Tazarotenic acid-d8 (AGN 190299-d8) is the deuterium labeled Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene (HY-15388) .
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms [4] .
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
DPPC-d13 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Mianserin-d3 (hydrochloride) is the deuterium labeled Mianserin hydrochloride. Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
N,N-Dimethylacetamide-d9 is the deuterium labeled N,N-Dimethylacetamide . N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent .
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma [4] .
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Ospemifene-d5 (FC-1271a-d5) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
Adipic acid-d8 (Hexanedioic acid-d8) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
Methyl methanesulfonate-d3 is the deuterium labeled Methyl methanesulfonate (HY-W004702). Methyl methanesulfonate is an alkylating agent which transfers methyl groups, and induces DNA damage. Methyl methanesulfonate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Theobromine-d3 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Nonanoic acid-d17 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers . DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice .
Rimsulfuron-d6 is deuterium labeled Rimsulfuron. Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide for postemergence use in maize to control grasses and some broadleaf weeds .
Metformin-d6 (1,1-Dimethylbiguanide-d6) is a deuterated labeled Metformin (HY-B0627). Metformin inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [4] .
Moxifloxacin-d3 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin hydrochloride is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
DL-Dipalmitoylphosphatidylcholine-d62 is deuterium labeled DL-Dipalmitoylphosphatidylcholine. DL-Dipalmitoylphosphatidylcholine (DL-DPPC) is a biochemical reagent .
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents .
Ciclopirox-d11 is the deuterium labeled Ciclopirox. Ciclopirox (HOE296b) is a synthetic antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic .
25-Hydroxycholesterol-d6 (25-OHC-d6) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells .
Docosanoic acid-d3 (Behenic acid-d3) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
5-Fluorouracil-d is the deuterium labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer . 5-Fluorouracil also inhibits HIV .
DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers . DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice .
Rufinamide- 15N,d2-1 (CGP 33101- 15N,d2-1) is 15N- and deuterium-labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome [4].
2-Deoxy-D-glucose- 13C6 (2-DG- 13C6) is 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
Vanillin- 13C,d3 is the 13C and deuterium labeled Vanillin . Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine .
PSI-6206- 13C,d3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
13,14-Dihydro-15-keto prostaglandin D2-d9 (DK-PGD2-d9) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay . Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses .
DSPC-d9 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d9) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
L-Cysteine- 13C3, 15N,d3 is the deuterium, 13C-, and 15-labeled L-Isoleucine (HY-Y0337). L-isoleucine is a nonpolar hydrophobic amino acid . L-Isoleucine is an essential amino acid.
L-Serine- 15N,d3 is the deuterium and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
D-(+)-Trehalose-13C12 is a 13C isotope labeled version of D-(+)-Trehalose (HY-N1132). D-(+)-Trehalose,which is widespread, can be used as a food ingredient and pharmaceutical excipient .
DSPC-d74 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d74) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
Guanosine triphosphate- 13C10, 15N5 (tetraammonium) is the 13C and 15N labeled Guanosine triphosphate tetraammonium . Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19 .
DSPC-d70 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d70) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
DL-Alanine- 13C2, 15N (DL-2-Aminopropionic acid- 13C2, 15N) is 13C and 15N labeled DL-Alanine. DL-alanine, an orally active amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver [4] .
3-Indoleacetic acid-2,2-d2 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Adenosine monophosphate- 13C10, 15N5 (AMP- 13C10, 15N5) disodium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
L-Histidine- 13C6, 15N3 hydrochloride hydrate is the 13C- and 15N-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
DSPC-d13 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d13) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
DSPC-d79 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d79) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
L-Thyroxine- 13C6-1 (Levothyroxine- 13C6-1; T4- 13C6-1) is a 13C labeled L-Thyroxine (HY-18341). L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4) .
p-Anisic acid- 13C6 is the 13C-labeled p-Anisic acid. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties .
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy [4] .
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [4].
DSPC-d83 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
LysoPC(14:0/0:0)-d7 (14:0 Lyso PC-d7) is deuterium labeled LysoPC(14:0/0:0). LysoPC(14:0/0:0) is a lysophospholipid (LyP). It is a monoglycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. LysoPC(14:0/0:0) has potent antispasmodic effect .
Lamivudine-13C,15N2,d2 (BCH-189-13C,15N2,d2) is a 13C, 15N, and deuterium labeled Lamivudine (HY-B0250). Lamivudine is an orally active and blood-brain barrier permeable nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine inhibits HIV reverse transcriptase 1 and 2 and hepatitis B virus (HBV) reverse transcriptase [4].
5-Methyltetrahydrofolic acid- 13C6 (5-Methyl THF- 13C6) is 13C labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases .
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .
Adenosine monophosphate- 13C10, 15N5(AMP- 13C10, 15N5) is the 13C-labeled and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Thymidine-5'-monophosphate- 13C10, 15N2 (disodium) is the 13C and 15N labeled Thymidine-5'-monophosphate disodium salt . Thymidine-5'-monophosphate disodium salt is an endogenous metabolite.
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
(±)11(12)-EET-d11 methyl ester (11,12-EET methyl ester-d11) is the deuterium labeled (±)11(12)-EET methyl ester (HY-139938). (±)11(12)-EET methyl ester is a type of epoxyeicosatrienoic acid (EET). EETs are endogenous lipid signaling molecules with cardioprotective and vasodilatory actions. (±)11(12)-EET methyl ester binds to and activates GPR132. (±)11(12)-EET methyl ester enhances hematopoietic induction and engraftment in mice and zebrafish .
Mirogabalin- 13C2,d1 (Mixture of Diastereomers) is a 13C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
Intermediate of tranexamic Acid- 13C2, 15N (Aminomethylbenzoic acid- 13C2, 15N) is 13C and 15N labeled 4-(Aminomethyl)benzoic acid. 4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
Cytidine-5'-triphosphate- 13C5 (Cytidine triphosphate- 13C5) is the 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii .
2'-Deoxycytidine-5'-monophosphoric acid- 13C9 dilithium is the 13C-labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite .
Valdecoxib- 13C2, 15N (SC 65872- 13C2, 15N) is the 13C- and 15N-labeled Valdecoxib (HY-15762). Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
(+/-)-Catechin Gallate- 13C3 is the 13C-labeled (-)-Catechin gallate. (-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract .
Uridine triphosphate- 15N2 (UTP- 15N2 dilithium; Uridine 5'-triphosphate- 15N2) dilithium is 15N labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
5-Methyltetrahydrofolic acid- 13C5 is the 13C-labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid .
L-Valine- 13C5, 15N,d8 ((S)-Valine- 13C5, 15N,d8) is the deuterium, 13C-, and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Acid Orange 7- 13C6 (Orange II- 13C6) is the 13C-labeled Acid orange 7 (HY-N1442). Acid Orange 7 (Orange II; D&C Orange NO. 4) is an azo dye widely used in the textile, food and cosmetic industries. Acid Orange 7 is mainly used as a colorant by combining with fibers and other substances through azo bonds. Acid Orange 7 has a maximum absorption wavelength at 484-485 nm, and the concentration is measured using a UV-visible spectrophotometer. Acid Orange 7 is difficult to degrade and has a certain degree of toxicity. It is often used to study various sewage treatment technologies and photocatalytic degradation reactions, and to evaluate the removal effects of different treatment methods on organic pollutants .
O-Phospho-L-serine- 13C3 (L-Serine O-phosphate- 13C3) is the 13C-labeled O-Phospho-L-serine (HY-15129). O-Phospho-L-serine is the immediate precursor to L-cystein in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2 .
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
L-Glutamine- 13C5, 15N2 is the 13C- and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
O-Desmethyl midostaurin- 13C6 (CGP62221- 13C6; O-Desmethyl PKC412- 13C6) is the 13C-labeled O-Desmethyl Midostaurin (HY-129491). O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo . Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM.
p,p'-DDE- 13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Imatinib- 13C,d3 (STI571- 13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively [4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
Deoxythymidine-5'-triphosphate- 13C10, 15N2 (dTTP- 13C10, 15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Cinnamic acid- 13C3 (3-Phenylacrylic acid- 13C3) is the 13C labeled Cinnamic acid (HY-N0610A). Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells .
3-Indoleacetic acid- 13C6 is the 13C labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
DL-Lysine- 13C6, 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6, 15N2 hydrochloride) is 13C and 15N-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
L-Valine- 13C5, 15N,d2 ((S)-Valine- 13C5, 15N,d2) is the deuterium, 13C-, and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Uridine triphosphate- 13C9 (UTP- 13C9 dilithium; Uridine 5'-triphosphate- 13C9) dilithium is 13C-labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Guanosine 5'-diphosphate- 13C10, 15N5 (GDP- 13C10, 15N5) dilithium is 13C and 15N-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
Sofosbuvir- 13C,d3 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Adenosine 5'-diphosphate- 15N5 (Adenosine diphosphate- 15N5 dilithium) dilithium is 15N labeled Adenosine 5'-diphosphate (HY-W010918). Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms [4] .
2-Methylcitric acid-d3 is the deuterium labeled 2-Methylcitric acid. 2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate .
PIPES-d18 is the deuterium labeled PIPES . PIPES (1,4-Piperazinediethanesulfonic acid) is an important component of PIPES buffer agent used in biochemistry .
1-Methylguanosine-d3 (N1-Methylguanosine-d3) is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol . Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin .
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .
Idasanutlin-d3-1 (RG7388-d3-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of MDM2/p53. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .
Methyl cinnamate-d7 is deuterated labeled Methyl cinnamate (HY-W017212). Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway .
Cholestenone-d7 is deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop
Oxaceprol-d3 (N-Acetyl-L-hydroxyproline-d3) is deuterium labeled Oxaceprol. Oxaceprol (N-Acetyl-L-hydroxyproline), an orally active derivative of L-proline, possesses distinct anti-inflammatory activity. Oxaceprol is usually used for the research of osteoarthritis and rheumatoid arthritis .
Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate . Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
Resolvin D3-d5 is the deuterium labeled Resolvin D3. Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation .
Rosuvastatin-d3 (ZD 4522-d3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals .
Dimethyl adipate-d8 (Hexanedioic acid dimethyl ester-d8) is the deuterium labeled Dimethyl adipate (HY-W015301). Dimethyl adipate is an aliphatic dicarboxylate compound. Dimethyl adipate is mainly used as a plasticizer and an intermediate in organic synthesis.
Azilsartan mepixetil-d5 (QR-01019-d5) is deuterium labeled Azilsartan mepixetil. Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A) .
Tridecanoic acid-d25 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation .
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation .
Melatonin-d7 is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation [4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
(Rac)-Valsartan-d9 is deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator .
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Ribavirin- 13C2 (Ribasphere- 13C2) is the 13C-labeled Ribavirin (HY-B0434). Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.
Hippuric acid-d2 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
1-Methylinosine-d3 is the deuterium labeled 1-Methylinosine. 1-Methylinosine is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA .
Danicamtiv-d3-1 (MYK-491-d3-1) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
Tridecanoic acid-d2 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation .
Brexpiprazole S-oxide-d8 (DM-3411 D8) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
N-Desmethyl Selegiline-dd5 hydrochloride is the deuterium labeled N-Desmethyl Selegiline hydrochloride . N-Desmethyl Selegiline-d5 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Degarelix-d7 (FE 200486-d7 free base) is deuterium labeled Degarelix. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
1-Aminopropan-2-ol-d6 (Monoisopropanolamine-d6) is the deuterium labeled 1-Aminopropan-2-ol (HY-W015969). 1-Aminopropan-2-ol is a microbial metabolism of amino alcohol metabolism via propionaldehyde and acetaldehyde in a species of Pseudomonas .
2-Phenylglycine-d5 is the deuterium labeled 2-Phenylglycine. 2-Phenylglycine (DL-α-Phenylglycine) is a metabolite in breast milk during the W2 to W4 lactation period .
Isovanillin-d3 is the deuterium labeled Isovanillin . Isovanillin is an aldehyde oxidase inhibitor . Antispasmodic activities . Antidiarrheal activities [4].
Leukotriene B4-d5(LTB4-d5) is deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs [4].
(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
Methyl tetradecanoate-d27 is the deuterium labeled Methyl myristate. Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma .
Docosahexaenoic acid ethyl ester-d5 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects .
Bifenox-d3-1 (Modown-d3; MC-4379-d3) is the deuterium labeled Bifenox (HY-136513). Bifenox (Modown; MC-4379) is a potent herbicide. Bifenox increases the ROS production. Bifenox causes cellular membrane disruption, inhibition of photosynthesis .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Levomefolic acid-d3 (L-5-MTHF-d3) is deuterium labeled Levomefolic acid. Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .
(Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist .
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively .
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Resolvin D1-d5 is the deuterium labeled Resolvin D1. Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α-mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages .
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid Budesonide (HY-13580). 16α-Hydroxyprednisolone formation is catalyzed by isoenzymes within the cytochrome P450 3A (CYP3A) subfamily. 16α-Hydroxyprednisolone formation can be inhibited by antibodies targeting the CYP3A subfamily .
4-Hydroxypropranolol-d7 (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .
Leukotriene E4-d5 is the deuterium labeled Leukotriene E4. Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
(R)-Pioglitazone-d1 ((R)-U 72107-d1) is a stabilized and deuterated R-enantiomer of pioglitazone, exhibiting pharmacological properties that are beneficial for NASH treatment, including modulation of mitochondrial function, non-steroidal anti-inflammatory effects, and glucose-lowering capabilities.
L-Histidine-d5 hydrochloride hydrate is the deuterium labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 .
Fluoxetine-d6 (LY-110140 (free base)-d6) is deuterium labeled Fluoxetine. Fluoxetine (LY-110140 free base) is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively .
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
L-Histidine-d3 hydrochloride hydrate is the deuterium labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons .
Asymmetric dimethylarginine-d7 (hydrochloride hydrate) is the deuterium labeled Asymmetric dimethylarginine. Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a num
Albendazole-d3-1 (SKF-62979-d3-1) is the deuterium labeled Albendazole (HY-B0223). Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells [4] .
L-(+)-Ampicillin-d5 (L-(+)-α-Aminobenzylpenicillin-d5) is the deuterium labeled L-(+)-Ampicillin (HY-B0522C). L-(+)-Ampicillin (L-(2S) ampicillin) is the L-isomer of Ampicillin (HY-B0522). Ampicillin is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria .
11-Oxo etiocholanolone-d5 (11-Ketoetiocholanolone-d5) is the deuterium labeled 11-Oxo etiocholanolone (HY-113457). 11-Oxo etiocholanolone (11-Ketoetiocholanolone) is a steroid. 11-Oxo etiocholanolone is a key indicator for detecting cortisol metabolites in feces and urine. 11-Oxo etiocholanolone has the potential to be a pheromone .
Guanosine triphosphate-d14 (GTP-d14) dilithium is a deuterium labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19 .
Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM [4].
DL-dithiothreitol-d10-1 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases [4]
o-Phenanthroline-d8 is the deuterium labeled o-Phenanthroline. o-Phenanthroline (1,10-Phenanthroline), a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells. o-Phenanthroline (1,10-Phenanthroline) forms a red chelate with Fe2+ that absorbs maximally at 510 nm. o-Phenanthroline (1,10-Phenanthroline) is also a MMP inhibitor .
2-Hydroxymethyl olanzapine-d3 (LY-290411-d3) is a deuterium labeled 2-Hydroxymethyl olanzapine. 2-Hydroxymethyl olanzapine is a metabolite of Olanzapine. .
Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
3-Hydroxy Midostaurin-d5 is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively .
Acetyl coenzyme A-d3 (Acetyl-CoA-d3) is the deuterium labeled Acetyl coenzyme A (HY-114293). Acetyl-coenzyme A (Acetyl-CoA) is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A is also a key precursor of lipid synthesis [4].
Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
Alfuzosin (hydrochloride)-d6 (SL 77499-10-d6) is deuterium labeled Alfuzosin (hydrochloride). Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH) .
Sudan I-d5 is a the deuterated Sudan I. Sudan I is a diazo-conjugate red dye and can be used as an additive to products such as oils, solvents or polishes. Sudan I inhibits growth of bacterial strains Clostridium perfringens and L. rhamnosus .
1-Octanol-d2-1 is deuterated labeled 1-Octanol (HY-W032013). 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Sarafloxacin-d8 (hydrochloride trihydrate) is the deuterium labeled Sarafloxacin hydrochloride trihydrate. Sarafloxacin hydrochloride trihydrate is a quinolone antibiotic compound .
Nemonoxacin-d3-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
Hippuric acid-d5 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
Adenosine monophosphate-d12 (AMP-d12) dilithium is deuterium labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Eliglustat-d15 (tartrate) is the deuterium labeled Eliglustat. Eliglustat tartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Ethyl butyrylacetate-d5 (Ethyl 3-oxohexanoate-d5) is the deuterium labeled Ethyl butyrylacetate (HY-W015487). Ethyl butyrylacetate is an organic compound belonging to the class of esters. Synthesized by the reaction of ethyl acetate, butyric acid and acetic anhydride. Ethyl butyrylacetate has a fruity aroma and is commonly used as a flavoring agent in various food and beverages such as candies, ice cream and soft drinks. It is also used as a fragrance ingredient in perfumes and personal care products. In addition to its use in the food and fragrance industries, Ethyl butyrylacetate is also used in industrial settings, such as in the production of solvents.
Vitamin D4-d5 is the deuterium labeled Vitamin D4. Vitamin D4 (22-Dihydroergocalciferol) is a Vitamin D derived from fungi. The precursor of Vitamin D4 is 22,23-dihydroergosterol .
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
Itopride-d6 (HSR803-d6 (free base)) is deuterium labeled Itopride. Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .
Perindoprilat-d3 disodium is deuterated labeled Perindoprilat (HY-B1433). Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research .
Bendamustine-d8 is the deuterium labeled Bendamustine . Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
rac-Trandolapril-d5 (rac-RU44570-d5) is deuterium labeled Trandolapril. Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
Cholestenone-d5 is the deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells .
Voriconazole N-oxide-d3 (Voriconazole oxynitride-d3) is deuterium labeled Voriconazole N-oxide. Voriconazole N-oxide (Voriconazole oxynitride) is a potent antifungal agent. Voriconazole N-oxide has phototoxicity and photocarcinogenicity. Voriconazole N-oxide does not sensitize keratinocytes to ultraviolet B (UVB) .
2,3-Oxidosqualene-d6 (Squalene oxide-d6) is a deuterium labeled 2,3-Oxidosqualene (HY-114296). 2,3-Oxidosqualene (Squalene oxide) is an intermediate in the biological synthesis of sterols from squalene .
Prostaglandin D2-d9 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals . Prostaglandin D2 is one of the most potent endogenous sleep promoting substances . PGD2 plays a protective role by suppressing inflammation .
Bimatoprost-d5 is a deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog and is a topical hypotensive agent frequently used for treating ocular hypertension and glaucoma. Bimatoprost also has an antiadipogenic effect .
Methyl paraben-d3 (Methyl 4-hydroxybenzoate-d3) is the deuterium labeled Methyl paraben (HY-N0349). Methyl Paraben is a standardized methyl paraben allergen isolated from Yunnan hemlock (Tsuga dumosa). Methyl Paraben is commonly used as a stable, non-volatile preservative. Methyl Paraben increases histamine release and cellular regulation of immunity, blocks sodium channels, and prevents ischemia-reperfusion injury [4].
Tridecanoic acid-d9 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation .
Linagliptin-d3-1 (BI 1356-d3-1) is the deuterium labeled Linagliptin (HY-10284). Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM .
Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule?depolymerization with an IC50 value of 0.2 μM . Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of?bcl-2?and?bcl-xL?gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis .
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively .
Lurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM .
rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142) . Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively .
22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone (HY-131543). 22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcoholic metabolite with antiprogestational and antiglucocorticoidal activities, which contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. The relative binding affinity of 22-Hydroxy Mifepristone to the human glucocorticoid receptor is 48% .
Kinetin riboside-d5 (N6-Furfuryladenosine-d5) is the deuterium labeled Kinetin riboside (HY-101055). Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM .
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
Norethindrone acetate-d8 is the deuterium labeled Norethindrone acetate. Norethindrone acetate is a female hormone used for the research of endometriosis . Norethindrone acetate-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Alogliptin-d3 is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes .
Miconazole-d5 (nitrate) is the deuterium labeled Miconazole. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects .
Ethyl 3-oxopentanoate-d3 (Ethyl Propionylacetate-d3) is the deuterium labeled Ethyl 3-oxopentanoate (HY-78211). Ethyl 3-oxopentanoate is an organic ester compound commonly used as a reactant or solvent in organic synthesis. It can be used as an important raw material for the preparation of pharmaceuticals, food flavors, spices and other products. In addition, because of its stability and reactivity in certain chemical reactions, it is also widely used in some industrial productions. Although Ethyl 3-oxopentanoate has no direct application in the medical field, it still plays an important role in chemical research and industry.
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Paroxetine-d6-1 is a deuterated labeled Paroxetine . Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs .
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation [4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
Ipidacrine-d9 (NIK-247-d9 (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases [4] .
Benzyl benzoate-d12 is the deuterium labeled Benzyl benzoate . Benzyl benzoate (Benzoic acid benzyl ester) is a fragrance ingredient in cosmetic products. Benzyl benzoate can be used for the research of Scabies and Demodex-associated inflammatory skin conditions [4].
Donepezil-d7 (E2020-d7 (free base)) is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
2-Acetylthiazole- 13C2 is 13C labeled 2-Acetylthiazole (HY-Y0045). 2-Acetylthiazole (1-(1,3-Thiazol-2-yl)ethanone; 1-(Thiazol-2-yl)ethanone; Methyl 2-thiazolyl ketone) is a flavor compound. 2-Acetylthiazole is a kind of biological materials or organic compounds that are widely used in life science research .
Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine . Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity .
Deoxycytidine triphosphate- 13C9 (dCTP- 13C9 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9) dilithium is 13C-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
DMT-dA(bz) Phosphoramidite- 13C10, 15N5 is the 13C and 15N labeled DMT-dA(bz) Phosphoramidite . DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA .
Cytidine-5'-triphosphate- 13C9 (Cytidine triphosphate- 13C9 dilithium; 5'-CTP- 13C9) dilithium is 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
2'-Deoxyadenosine-5'-triphosphate- 13C10, 15N5 tetraammonia is the 13C10 and 15N5 labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase .
Menaquinone-4- 13C6 is the 13C-labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
Cytidine-5'-triphosphate- 15N3 (Cytidine triphosphate- 15N3 dilithium; 5'-CTP- 15N3) dilithium is 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
Estrone 3-methyl ether- 13C6 is a 13C-labeled Estrone 3-methyl ether (HY-79576). Estrone 3-methyl ether (Oestrone methyl ether; 3-O-Methylestrone) is a synthetic intermediate useful for synthesis of estrogen receptor modulator .
Hexadecane-1,2- 13C2 (n-Hexadecane-1,2- 13C2) is the 13C labeled Hexadecane (HY-W099580). Hexadecane (n-Hexadecane) is a saturated hydrocarbon of alkanes or paraffins and can be used as an organic solvent. Hexadecane is a component of petroleum, belongs to hydrophobic substrates, and is a model substance for studying bacterial degradation of hydrophobic compounds .
Thymine- 13C5, 15N2 (5-Methyluacil- 13C5, 15N2) is 13C and 15N labeled Thymine. Thymine is one of the four nucleobases in the nucleic acid of DNA and can be a target for actions of 5-fluorouracil (5-FU) in cancer treatment, with a Km of 2.3 μM .
dGTP- 13C10, 15N5 (2'-Deoxyguanosine-5'-triphosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Deoxycytidine triphosphate- 15N3 (dCTP- 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3) dilithium is 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
2'-Deoxyadenosine-5'-triphosphate- 13C10, 15N5 (dATP- 13C10, 15N5) dilithium is 13C and 15N-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
5-Hydroxymethylfurfural- 13C6 (2-Hydroxymethyl-5-furfural- 13C6; 2-Formyl-5-hydroxymethylfuran- 13C6) is a 13C labeled 5-Hydroxymethylfurfural (HY-Y0051). 5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from Cornus officinalis, inhibits yeast growth and fermentation as stressors.
p,p'-DDD- 13C12 is 13C labeled p,p'-DDD. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT .
Oleic acid- 13C18 is the 13C labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
Rapamycin- 13C,d3-1 (Sirolimus- 13C,d3-1) is the deuterium labeled and 13C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
2'-Deoxycytidine- 13C, 15N3 (Deoxycytidine- 13C, 15N3) is 13C and 15N labeled 2'-Deoxycytidine. 2'-Deoxycytidine, a deoxyribonucleoside, can inhibit biological effects of Bromodeoxyuridine (Brdu). 2'-Deoxycytidine is essential for the synthesis of nucleic acids, that can be used for the research of cancer .
Droxidopa- 13C2, 15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood-brain barrier .
Acetaminophen- 13C2, 15N is the 13C and 15N labeled Acetaminophen . Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent [4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor .
Hydrocinnamic acid-2,3- 13C2 is the 13C-labeled Hydrocinnamic acid. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities.
Cytidine 5′-monophosphate- 13C9 (5'-Cytidylic acid- 13C9 dilithium; 5'-CMP- 13C9) dilithium is 13C-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid- 13C10 (5'-GMP- 13C10 dilithium; 5'-guanosine monophosphate- 13C10) dilithium is 13C-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
N-Acetyl mesalazine- 13C6 (N-Acetyl-5-aminosalicylic acid- 13C6) is a deuterated labeled N-Acetyl mesalazine (HY-66008). N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the primary intestinal metabolite of 5-Aminosalicylic Acid (HY-15027) and serves as a biomarker for evaluating the efficacy of 5-Aminosalicylic Acid (HY-15027). N-Acetyl mesalazine can scavenge free radicals, reduce DNA base hydroxylation, and ameliorate mucosal inflammation. N-Acetyl mesalazine can be used in the study of diseases such as colitis and colon cancer .
(E,E)-Farnesol- 13C3 (trans,trans-Farnesol- 13C3) is the 13C-labeled (E,?E)?-?Farnesol (HY-Y0248). (E, E)-Farnesol (trans,trans-Farnesol;(2E,6E)-Farnesol) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Uridine 5'-monophosphate- 13C9, 15N2 disodium is the 13C and 15N labeled Uridine 5'-monophosphate disodium salt (HY-W013175). Uridine 5'-monophosphate (5'-Uridylic acid) disodium salt is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate disodium salt can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Cytidine- 13C9 (Cytosine β-D-riboside- 13C9) is 13C labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function .
Fmoc-Asp(OtBu)-OH-d3 (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate-d3) is deuterium labeled Fmoc-Asp(OtBu)-OH. Fmoc-Asp(OtBu)-OH (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate) is a aspartate derivative containing amine protecting group Fmoc. Fmoc-Asp(OtBu)-OH can be used for peptide synthesis .
rU Phosphoramidite- 13C9, 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9, 15N2) is 13C and 15N-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Cytidine- 15N3 is the 15N labeled Cytidine . Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [4].
2'-Deoxyguanosine 5'-monophosphate- 13C10, 15N5 (dGMP- 13C10, 15N5) disodium is the 13C and 15N labeled 2'-Deoxyguanosine 5'-monophosphate disodium (HY-W013159). 2'-Deoxyguanosine 5'-monophosphate (5′-dGMP) disodium is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a reactant involved in analysis of self-assembling in solution and nucleation/growth of G-qudruplexes, nucleophilic trapping and reductive alkylation. 2'-Deoxyguanosine 5'-monophosphate disodium can be used as an oxidizable target. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative and is a nucleotide precursor used in DNA synthesis .
Cytidine 5′-monophosphate- 15N3 (5'-Cytidylic acid- 15N3 dilithium; 5'-CMP- 15N3) dilithium is 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Acetyl-L-carnitine hydrochloride- 13C3 (O-Acetyl-L-carnitine hydrochloride- 13C3) is the 13C-labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression .
Uridine 5'-monophosphate- 13C9, 15N2 (5'- Uridylic acid- 13C9, 15N2) dilithium is 13C and 15N-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Sulfadimethoxine- 13C6 is the 13C-labeled Sulfadimethoxine. Sulfadimethoxine (Sulphadimethoxine) is a sulfonamide antibiotic used to treat many infections .
Mebeverine acid-d5 (Mebeverine metabolite Mebeverine acid-d5) is the deuterium labeled Mebeverine Acid (HY-12769). Mebeverine acid is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine.
1,3,5-Trimethoxybenzene-d3 (Trimethyl phloroglucinol-d3) is the deuterium labeled 1,3,5-Trimethoxybenzene (HY-Y0678). 1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor .
Sulfachloropyridazine- 13C6 is the 13C6 labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
N-Acetyl-L-methionine-d3 is the deuterium labeled N-Acetyl-L-methionine. N-Acetyl-L-methionine, a human metabolite, is nutritionally and metabolically equivalent to L-methionine. L-methionine is an indispensable amino acid required for normal growth and development .
6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
Zeranol-d5-1 (α-Zearalanol-d5-1) is the deuterium labeled Zeranol (HY-N6709). Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity .
D-Glutamic acid-d5 is the deuterium labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods .
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Borocaptate- 10B12 (BSH- 10B12) sodium is a boron-10 labeled Borocaptate (HY-142041). Borocaptate sodium is a boron-containing compound that can be used as a therapeutic agent in boron neutron capture therapy (BNCT), exhibiting anticancer activity .
3-Methoxytyramine-d3 hydrochloride (3-O-methyl Dopamine-d3 hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride (HY-103638). 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1).
5,6-Dihydro-5-methyluracil-d6 is the deuterium labeled 5,6-Dihydro-5-methyluracil. 5,6-Dihydro-5-methyluracil (Dihydrothymine), an intermediate breakdown product of thymine, comes from animal or plants. 5,6-Dihydro-5-methyluracil (Dihydrothymine) can be toxic when present at abnormally high levels .
3-O-Methyltolcapone-d7 (Ro 40-7591 d7) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4] .
Valerylcarnitine-d9 (C5:0 L-carnitine-d9) is the deuterium labeled Valerylcarnitine (HY-113266). Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines .
L-Alanine-d7 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Betamethasone dipropionate-d10 is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
Benzisothiazolinone-13C5 (1,2-Benzothiazol-3-one-13C5) is a 13C-labeled Benzisothiazolinone. Benzisothiazolinone is widely used as an antiseptic and antibacterial agent .
ATP-d14 (Adenosine 5'-triphosphate-d14) dilithium is deuterium labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Mebeverine acid-d3 (Mebeverine metabolite Mebeverine acid-d3) is the deuterium labeled Mebeverine Acid (HY-12769). Mebeverine acid is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine.
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model [4].
Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
Glibenclamide- 13C6 (Glyburide- 13C6) is 13C labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability [4]. Glibenclamide can induce autophagy .
L-Glutamine-d5 is the deuterium labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Epiallopregnanolone-d5 (5α,3β-THDOC-d5) is deuterium labeled Epiallopregnanolone. Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer .
2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity .
(2R)-Isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate-d5 is the deuterium labeled (2R)-isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate [
(S)-Verapamil-d6 ((S)-(-)-Verapamil-d6) hydrochloride is the deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
PAC-1-d8 (Procaspase activating compound 1-d8) is the deuterium labeled PAC-1 (HY-13523). PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC50 of 2.08 μM.
Ceftriaxone-d3 (disodium) is the deuterium labeled Ceftriaxone. Ceftriaxone is a third-generation cephalosporin antibiotic with excellent activity against many gram-negative, and reasonable activity against most gram-positive microorganisms. Anti-inflammatory and antioxidant characteristics .
Indolelactic acid-d5 is the deuterium labeled Indolelactic acid. Indolelactic acid is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures.
Adenosine-d is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
O-Toluic acid-d7 is the deuterium labeled o-Toluic acid . o-Toluic acid (2-Methylbenzoic acid) is a benzoic acid substituted by a methyl group at position 2. O-Toluic acid plays a role as a xenobiotic metabolite.
Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects [4] .
Diethyl phosphate-d10-1 is the deuterium labeled Diethyl phosphate. Diethylphosphate (Diethyl phosphoric acid) is an orally active organophosphorus pesticides metabolite. Diethylphosphate can interfere with thyroid hormone-related mechanisms and affect intestinal microbes in rats .
(±)11(12)-EET-d11 is the deuterium labeled (±)11(12)-EET. (±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective [4] .
Ribavirin- 13C5 is the 13C-labeled Ribavirin. Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV.
Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
Homovanillic acid-d3-1 (Vanilacetic acid-d3-1) is deuterated labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
L-Alanine-d3 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
MCA-d3 (7-Methoxycoumarin-4-acetic acid3) is the deuterium labeled MCA (HY-W027544) . MCA is a Coumarin (HY-N0709) derivative. MCA quantitates platelet-activating factor (PAF) by high-performance liquid chromatography with fluorescent detection. MCA can modify FRET peptide substrates for analyzing protease activities .
2-Hydroxy Ibuprofen-d6 is the deuterium labeled 2-Hydroxy Ibuprofen. 2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively .
Norethindrone- 13C2 (Norethisterone- 13C2) is the 13C labeled Norethindrone (HY-B0554) . Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea [4] .
TCEP-d12 (hydrochloride) (Tris(2-?carboxyethyl)?phosphine hydrochloride-d12) is deuterium labeled TCEP (hydrochloride). TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry [4] .
Calcifediol-d3 is a deuterium labeled Calcifediol. Calcifediol, is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels .
Veratrole-d2-1 is the deuterium labeled Veratrole (HY-B1812). Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
d-KLA Peptide-d30 (D-(KLAKLAK)2-d30) is the deuterium labeled d-KLA Peptide (HY-P10285). d-KLA Peptide is a synthetic pro-apoptotic peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrial membrane. d-KLA Peptide activates biochemical pathways associated with apoptosis, including the activation of caspase family proteins and PARP (poly ADP ribose polymerase). d-KLA Peptide can be used to carry and deliver genes or small molecules to enhance anti-tumor effects .
Migalastat-d5 (GR181413A-d5 (free base)) is deuterium labeled Migalastat. Migalastat (GR181413A free base) is an orally active α-galactosidase A molecular chaperone, with an IC50 value of 0.04 μM for human α-Gal A. Migalastat binds to the active site of certain unstable mutant forms of α-galactosidase A, facilitating their transport to the lysosome. After dissociation in the acidic environment, Migalastat enables the mutant α-galactosidase A to exhibit biological activity .
Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
D-Threonine-d2 (H-D-Thr-OH-d2) is the deuterium labeled D-Threonine (HY-W012874). D-Threonine is one of the important unnatural amino acids used as chiral building blocks in pharmaceutical drugs. D-Threonine is a metabolite of Saccharomyces cerevisiae. D-Threonine is cleaved into glycine and acetaldehyde by the catalytic action of D-threonine aldolase.
Mebeverine acid-d5 (Mebeverine metabolite Mebeverine acid-d5) hydrochloride is deuterium labeled Mebeverine acid hydrochloride. Mebeverine acid hydrochloride is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid hydrochloride is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid hydrochloride is an important marker for oral Mebeverine.
Ercalcidiol-d3 is the deuterium labeled Ercalcidiol. Ercalcidiol is a metabolite of Vitamins D2. Ercalcidiol can be used as an indicator of vitamins D status .
14(S)-HDHA-d5 (14(S)-HDoHE-d5) is deuterium labeled 14(S)-HDHA. 14(S)-HDHA (14(S)-HDoHE) is an oxygenation product of Docosahexaenoic acid (DHA). 14(S)-HDHA is a marker reflecting activation of a Docosahexaenoic acid carbon 14-lipoxygenation pathway .
1-Decanol-d2-2 is deuterated labeled 1-Decanol (HY-Y1004). 1-Decanol is used in the production of lubricants, surfactants, plasticizers and solvents. It has also been used to study the thermal properties of polymeric monolithic stationary phases and to enhance homopolyglycine acceptor function. Used in cosmetics, daily flavors, and food flavors.
1-Butynylbenzene-d5 is the deuterium labeled 1-Butynylbenzene . 1-Butynylbenzene-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ibufenac- 13C6 (Dytransin- 13C6) is the 13C-labeled Ibufenac (HY-W040672). Ibufenac (Dytransin) is an orally active nonsteroidal anti-inflammatory agent. Ibufenac exerts anti-inflammatory, analgesic and antipyretic effects. Ibufenac is being studied for the treatment of rheumatic diseases such as rheumatoid arthritis .
Moxifloxacin-d5 (BAY 12-8039-d5 (free base)) is deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Estriol- 13C3 is the 13C-labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Dimetridazole-d3 (1,2-Dimethyl-5-nitroimidazole-d3) is a deuterium labeled Dimetridazole (HY-B1244). Dimetridazole is a nitroimidazole antibiotic. Dimetridazole inhibits protein synthesis in cultures of Campylobacter jejuni. Dimetridazole is genotoxic. Dimetridazole can be used in the research of protozoal and bacterial infections [4].
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide . Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect [4].
Doxercalciferol-d6 (1.alpha.-Hydroxyvitamin D2-d6) is deuterium labeled Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
Ciraparantag-d8 (PER977-d8) tetrahydrochloride diacetate is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban [4].
DL-Alanine-d3 is the deuterium labeled DL-Alanine. DL-alanine, an amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine, and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver [4] .
(E)-β-Farnesene-d6 is deuterated labeled (E)-β-Farnesene (HY-N7364). (E)-β-Farnesene (trans-β-Farnesene) is an aphid alarm pheromone, which can be found in Phlomis aurea Decne essential oil. (E)-β-Farnesene shows good binding score with a value of -30.64 kcal/mol to the CDK2 receptor. (E)-β-Farnesene also exhibits good affinity to odorant-binding protein 3 (OBP3). (E)-β-Farnesene can be used as a feeding stimulant for the sand fly Lutzomyia longipalpis [4].
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .
DL-Alanine-d7 (DL-2-Aminopropionic acid-d7) is deuterium labeled DL-Alanine. DL-alanine, an orally active amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver [4] .
2-Sec-butyl-3-methoxypyrazine-d3 is deuterated labeled cis-?Jasmone (HY-N7058). Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies .
p-Toluic acid-d3 is the deuterium labeled p-Toluic acid . p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
3-Methoxybenzeneboronic acid-d3 is the deuterium labeled 3-Methoxybenzeneboronic acid (HY-W000854). 3-Methoxybenzeneboronic acid (3-Methoxyphenylboronic acid) is a boronic acid derivative. 3-Methoxybenzeneboronic acid shows best suitable binding pattern at the active site by interacting non-covalently with amino acid residues of proteins. 3-Methoxybenzeneboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities . Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling . Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation .
Abemaciclib metabolite M20-d8 is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor .
Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
3,4-Dehydro Cilostazol-d11 is deuterated labeled 3,4-Dehydro Cilostazol (HY-135910). 3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study .
Patulin- 13C7 (Terinin- 13C7) is the 13C labeled Patulin (HY-N6779) . Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage [4] .
Calcifediol-d6 monohydrate is the deuterium labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels .
2-Hydroxypalmitic acid-d30 (2-Hydroxyhexadecanoic acid-d30) is deuterium labeled 2-Hydroxypalmitic acid. 2-Hydroxypalmitic acid is an intermediate in phytosphingosine metabolism .
Deoxythymidine-5'-triphosphate-d15 (dTTP-d15) dilithium is the deuterium labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA .
Calcitriol-d3 is the deuterium labeled Calcitriol . Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist [4] .
1,3-Dimethoxybenzene-d3 (Resorcinol dimethyl ether-d3) is the deuterium labeled 1,3-Dimethoxybenzene (HY-34487). 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds .
Histamine- 15N3 is the 15N3-labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
H-D-Trp-OH-d5 (D-Tryptophan-d5) is the deuterium labeled H-D-Trp-OH. H-D-Trp-OH is a D-stereoisomer of tryptophan and occasionally found in naturally produced peptides such as the marine venom peptide.
Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
Perospirone-d8 (SM-9018-d8 (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
NAPQI-d3 (N-Acetyl-4-benzoquinone Imine-d3) is the deuterium labeled NAPQI (HY-W017464). NAPQI is the toxic metabolite of Acetaminophen (HY-66005). NAPQI is also an inhibitor of enzymes in the vitamin K cycle. NAPQI is rapidly detoxified by glutathione (GSH), but in situations of GSH deficiency, excess NAPQI reacts with cysteine residues in proteins, causing cell death and toxicity in the liver .
DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers . DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice .
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299 .
Ibuprofen- 13C6 ((±)-Ibuprofen- 13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [4] .
Moxifloxacin-d3-1 hydrochloride (BAY 12-8039-d3-1) is a deuterium labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Histamine- 13C5 is the 13C labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
(Rac)-DPPC-d6 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [4] .
Gimeracil- 13C3 (Gimestat- 13C3) is the 13C-labeled Gimeracil (HY-17469). Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD) .
(±)14,15-DiHETrE-d11 ((±)14(15)-DiHET-d11) is the deuterium labeled (±)14,15-DiHETrE (HY-143664). (±)14,15-DiHETrE is an epoxide hydrolases enzymatically hydrated metabolite of (±)14(15)-EET .
2-(Benzhydrylsulfinyl)acetic acid-d10 (Modafinil acid-d10) is the deuterium labeled 2-(Benzhydrylsulfinyl)acetic acid (HY-W103882). 2-Benzhydrylsulfinylacetic acid (Modafinil acid) is the metabolite of modafinil .
p-Toluic acid-d7 is the deuterium labeled p-Toluic acid . p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Sulfacetamide- 13C6 (Sulphacetamide 13C6) is the 13C6 labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
2-Phenylethyl isothiocyanate-d5 isothiocyanate-d5 is the deuterium labeled 2-Phenylethyl isothiocyanate[1]. 2-Phenylethyl isothiocyanate is a potent antifungal agent. 2-Phenylethyl isothiocyanate significantly inhibited spore germination and mycelial growth of Alternaria alternata, with a MIC (minimum inhibitory concentration) of 1.22 mM. The antifungal effect of 2-Phenylethyl isothiocyanate against Alternaria alternata might be via reduction in toxin content and breakdown of cell membrane integrity[2][3].
Farnesyl pyrophosphate-d2 (Farnesyl diphosphate-d2) triammonium is a deuterium labeled Farnesyl pyrophosphate triammonium (HY-113037C). Farnesyl pyrophosphate ammonium is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate ammonium is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate ammonium is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Tetrahydrofolic acid- 13C6 (L-5,6,7,8-Tetrahydrofolic acid- 13C6) is 13C labeled Tetrahydrofolic acid. Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid .
Fmoc-Trp(Boc)-OH- 13C11, 15N2 (Fmoc-L-Trp(Boc)-OH- 13C11, 15N2) is the 13C-labeled and 15N-labeled Fmoc-Trp(Boc)-OH (HY-W008034). Fmoc-Trp(Boc)-OH (Fmoc-L-Trp(Boc)-OH) is an amino acid derivative with protective groups. Fmoc-Trp(Boc)-OH can self-assemble into stable and pH-responsive spherical nanoparticles, which can load and release bioactive molecules, with good biocompatibility and high cell uptake rate. Fmoc-Trp(Boc)-OH can be used in research on drug delivery .
3-Chloropropane-1,2-diol dipalmitate- 13C3 is 13C labeled 3-Chloropropane-1,2-diol dipalmitate. 3-Chloropropane-1,2-diol dipalmitate is a free fatty acid consisting mainly of diesters .
(R)-3-Hydroxybutanoic acid- 13C2 sodium is the 13C labeled (R)-3-Hydroxybutanoic acid sodium (HY-W015851). (R)-3-Hydroxybutanoic acid sodium is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones .
Tetrahydrofolic acid- 13C5 (L-5,6,7,8-Tetrahydrofolic acid- 13C5) is 13C labeled Tetrahydrofolic acid. Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid .
Guanidine- 13C, 15N3 (hydrochloride)is the 13C-labeled and 15N-labeled Guanidine hydrochloride. Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins .
L-Phenylalanine- 13C9, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Levoglucosan- 13C6 is the 13C labeled Levoglucosan . Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature .
Brivudine- 13C, 15N2 (Bromovinyldeoxyuridine- 13C, 15N2) is 13C and 15N labeled Brivudine. Brivudine is a thymidine analogue with antiviral activity, indicated for the early treatment of acute herpes zoster.
Avanafil- 13C5 (TA1790- 13C5) is 13C labeled Avanafil. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
5-Methyl-1H-benzotriazole-d6 (5-Methylbenzotriazole-d6) is the deuterium labeled 5-Methyl-1H-benzotriazole (HY-W086988). 5-Methyl-1H-benzotriazole is a biological material or organic compound that can be used in life science research .
3-Hydroxybutyric acid-d2 (sodium) is the deuterium labeled 3-Hydroxybutyric acid sodium . 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids .
3-Epiglycyrrhetinic acid-d2 (3α-Glycyrrhetic acid-d2) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
Riluzole- 13C6 (PK 26124- 13C6) is 13C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
N-Nitrosodibutylamine-d18 is the deuterium labeled N-Nitrosodibutylamine . N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water .
Progesterone-d9 is the deuterium labeled Progesterone. Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.
Acemetacin- 13C6 (TVX 1322- 13C6) is 13C labeled Acemetacin. Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
trans-Cinnamic acid-d7 is the deuterium labeled trans-Cinnamic acid . trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1 .
Dapagliflozin- 13C6 (BMS-512148- 13C6) is 13C labeled Dapagliflozin. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Ketorolac- 13C6 (RS37619- 13C6) is 13C labeled Ketorolac. Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorolac tromethamine is also a DDX3 inhibitor that can be used for cancer research [4].
Tranexamic acid- 13C6 (Cyclocapron- 13C6) is 13C labeled Tranexamic acid. Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis [4] .
Cyprodinil- 13C6 (CGA-219417- 13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate . Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research . Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells [4] .
Sulfamerazine- 13C6 (RP2632- 13C6) is 13C labeled Sulfamerazine (HY-B0512). Sulfamerazine (RP-2632) is a sulfonamide antibacterial. Sulfamerazine, the monomethyl derivative of sulfadiazine, is 2-sulfanilamido-4-methylpyrimidine. Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthesizes.
p-Cresol sulfate-d7 (potassium) is the deuterium labeled p-Cresyl sulfate potassium. p-Methylphenyl potassium sulfate is a prototype protein-bound uremic toxin[1][2].
Sucrose- 13C6 is the 13C labeled Sucrose . Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preference, and diabetes, et al .
Dimethyl Phthalate- 13C2 (DMP- 13C2) is the 13C-labeled Dimethyl phthalate (HY-N7106). Dimethyl phthalate (DMP) can be used as a plasticizer to impart flexibility to rigid polyvinyl chloride (PVC) resin. Additionally, Dimethyl phthalate is an oral active endocrine disruptor that can cause ovarian dysfunction in mice. Dimethyl phthalate can also induce oxidative stress and apoptosis in cells, thereby affecting blood and red blood cell function in rats .
N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide .
Adenosine monophosphate- 13C5 (AMP- 13C5) is 13C labeled Adenosine monophosphate. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Bis(1-chloro-2-propyl) phosphate-d12 is deuterium labeled Bis(1-chloro-2-propyl) phosphate. Bis(1-chloro-2-propyl) phosphate (BCIPP) is a metabolite of organophosphate flame retardants (OPFR) that may alter energy metabolism by influencing the levels of steroid hormones, such as cortisol and cortisone. Bis(1-chloro-2-propyl) phosphate holds potential for research on metabolism-related diseases caused by environmental exposure .
Amiloride- 15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride . Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC ) and urokinase-type plasminogen activator receptor (uTPA ). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2 [4]) channel.
Bexarotene- 13C6 (LGD1069- 13C6) is 13C labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
N-Dodecyl-β-D-maltoside-d25 (Lauryl Maltoside-d25) is deuterium labeled N-Dodecyl-β-D-maltoside (HY-128974). N-Dodecyl-β-D-maltoside is a non-ionic detergent. N-Dodecyl-β-D-maltoside has strong adsorption on alumina, titanium dioxide and hematite. N-Dodecyl-β-D-maltoside can promote the reactivation of various proteins. N-Dodecyl-β-D-maltoside can effectively stabilize photoactive reaction center complexes (RCs) and inhibit the degradation of Rhodopseudomonas spheroides R-26 reaction center in solution. N-Dodecyl-β-D-maltoside can be used for purification and stabilization of RNA polymerase and for detection of protein-lipid interactions [4].
Ivosidenib- 13C5 (AG-120- 13C5) is 13C labeled Ivosidenib. Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
N-Nitrosodibutylamine-d9 is the deuterium labeled N-Nitrosodibutylamine . N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water .
3-Epiglycyrrhetinic acid-d3 (3α-Glycyrrhetic acid-d3) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Sodium 2-oxopropanoate- 13C3 is the 13C-labeled Sodium 2-oxopropanoate. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS .
Florfenicol- 13C6 (SCH-25298- 13C6) is 13C labeled Florfenicol. Florfenicol ((-)-Florfenicol) is an orally active broad-spectrum antibacterial antibiotic with anti-inflammatory, pro apoptotic, and immunomodulatory functions .
Prasugrel-13C6 is a deuterated labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Ketoprofen- 13C6 (RP-19583- 13C6) is 13C labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity .
1-Bromo-3-methoxybenzene-d3 is the deuterium labeled 1-Bromo-3-methoxybenzene. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
trans-Cinnamic acid-d5 is the deuterium labeled trans-Cinnamic acid . trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1 .
Famotidine- 13C3 (MK-208- 13C3) is the 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
N-Palmitoyl-D-sphingomyelin-d9 (Sphingomyelin 16:0-d9) is deuterium labeled N-Palmitoyl-D-sphingomyelin. N-Palmitoyl-D-sphingomyelin (Sphingomyelin 16:0) (Compound SM-03) can be used for the synthesis of lipid nanoparticles .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
Ethyl 11(E)-octadecenoate-d5 (Vaccenic acid ethyl ester-d5) is the deuterium labeled Ethyl 11(E)-octadecenoate (HY-166122). Ethyl 11(E)-octadecenoate is an ester product.
Diclofenac- 13C6 (Sodium) is the 13C6 labeled Diclofenac (Sodium). Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
Penicillin V- 13C6 (potassium) is the 13C6 labeled Penicillin V (potassium). Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis.
Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
Docosahexaenoic acid ethyl ester-d5-1 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects .
Methyl(E)-cinnamate-d7 is the deuterium labeled Methyl (E)-cinnamate . Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry .
dGTP-d14 (2'-Deoxyguanosine-5'-triphosphate-d14) dilithium is deuterium labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Vandetanib- 13C6 is a 13C labeled Vandetanib (HY-10260) . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
Paroxetine-d2 (CTP 347) is a deuterium labeled Paroxetine (HY-122272). Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches [4].
Ivacaftor- 13C6 (VX-770- 13C6) is 13C labeled Ivacaftor. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities .
Anthracene-9-carboxylic acid-d9 is the deuterium labeled Anthracene-9-carboxylic acid . Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells .
Pomalidomide- 13C5 (CC-4047- 13C5) is 13C labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
2-Oxopropanoate- 13C2 (sodium) is the 13C labeled Sodium 2-oxopropanoate . Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS .
Mead acid-d6 is the deuterium labeled Mead acid. Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency .
Acetyl-L-carnitine-d3 (O-Acetyl-L-carnitine-d3) hydrochloride is the deuterium labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression [4].
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation [4] .
Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Gallic acid-d2 is the deuterium labeled Gallic acid . Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2) . Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities .
Pragliflozin- 13C6 (ASP1941- 13C6) is 13C labeled Ipragliflozin. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent .
Luliconazole- 13C7 (NND 502- 13C7) is 13C labeled Luliconazole. Luliconazole (NND 502)?is a topical antifungal imidazole antibiotic with broad-spectrum and potent antifungal activity. Luliconazole can be used for the research of skin infection, including?dermatophytosis, tinea corporis, tinea pedis?et al .
Mono(5-carboxy-2-ethylpentyl) phthalate-d9 (MECPP-d9) is the deuterium labeled Mono(5-carboxy-2-ethylpentyl) phthalate (HY-133675). Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking .
Sulcatone-d5 (6-Methyl-5-hepten-2-one-d5) is the deuterium labeled Sulcatone (HY-W010435). Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis [4].
DMT-dA(bz) Phosphoramidite-d9 (DA-CE phosphoramidite-d9) is deuterium labeled DMT-dA(bz) Phosphoramidite (HY-W013059). DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA.
3,3-Dimethylbutyric acid-d9 (tert-Butylacetic acid-d9) is a deuterated derivative of 3,3-Dimethylbutyric acid, which is a short-chain branched carboxylic acid and can be used in organic synthesis .
Favipiravir- 13C3 is the 13C labeled isotope of Favipiravir- 13C3(HY-14768 ).Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
Empagliflozin- 13C6 (BI 10773- 13C6) is 13C labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2 .
Saxagliptin- 13C2 (BMS-477118- 13C2) is 13C labeled Saxagliptin. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4(DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
DL-Arginine- 13C6 hydrochloride is 13C-labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide .
Exatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research .
Bezafibrate- 13C6 (BM15075- 13C6) is 13C labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
D,L-Sulforaphane glutathione-d5 (DL-SFN-GSH-d5) is deuterium labeled DL-Sulforaphane glutathione. DL-Sulforaphane glutathione (DL-SFN-GSH) is a metabolite of Sulforaphane (HY-13755) in rat plasma .
Sumatriptan-d6 is the deuterium labeled Sumatriptan. Sumatriptan is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research .
(E)-10-Hydroxynortriptyline-d3 is a deuterium labeled (E)-10-Hydroxy Nortriptyline. (E)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression .
Fludioxonil- 13C3 (CGA-173506- 13C3) is 13C labeled Fludioxonil. Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells [4].
2-Hydroxyestrone- 13C6 is the 13C-labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic .
Sumatriptan-d5 is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [4].
Meclofenamic acid- 13C6 is the 13C6 labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker.
Methyl (E)-cinnamate-d5 is the deuterium labeled Methyl (E)-cinnamate . Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry .
Ezetimibe- 13C6 (SCH 58235- 13C6) is the 13C-labeled Ezetimibe (HY-17376). Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Amprenavir- 13C6 (VX-478- 13C6) is 13C labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.09 μM.
Loratadine- 13C6 (SCH 29851- 13C6) is 13C labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
1-Naphthoic acid-d7 (Naphthalene-1-carboxylic acid-d7) is the deuterium labeled 1-Naphthoic acid (HY-Y0236). Naphthalene-1-carboxylic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Urea- 15N2 is the 15N-labeled Urea. Urea is a powerful protein denaturant via both direct and indirect mechanisms . A potent emollient and keratolytic agent . Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function . Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Rimeporide- 15N3 (hydrochloride) (EMD-87580- 15N3 (hydrochloride)) is 15N labeled Rimeporide hydrochloride. Rimeporide hydrochloride (EMD-87580 hydrochloride) is a potent and selective inhibitor of the Na +/H + exchanger (NHE-1).
Nimesulide- 13C6 (R805- 13C6) is 13C labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
Betrixaban- 13C6 (PRT054021- 13C6) is 13C labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
Tazarotene- 13C6 (AGN 190168- 13C6) is 13C labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2-Ketoglutaric acid-d6 (Alpha-Ketoglutaric acid-d6) is the deuterium labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
Amiloride- 15N3 (MK-870- 15N3) is 15N labeled Amiloride. Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC ) and urokinase-type plasminogen activator receptor (uTPA ). Amiloride is a blocker of polycystin-2 (PC2; TRPP2 ) channel.
Deferasirox- 13C6 (ICL 670- 13C6) is 13C labeled Deferasirox. Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload .
Atenolol- 13C6 ((RS)-Atenolol- 13C6) is 13C labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris .
Hippuric acid- 13C6 (Benzoylglycine- 13C6) is 13C labeled Hippuric acid. Hippuric Acid is an orally active metabolite. Hippuric Acid can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Hippuric Acid decreases NRF2, MMP9 and leads to ROS accumulation. Hippuric Acid activates TGFβ/SMAD signaling. Hippuric Acid improves hyperuricemia and colitis. Hippuric Acid can also be used in cardiovascular disease research [4].
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Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation .
DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals [4].
Diflunisal- 13C6 (MK-647- 13C6) is 13C labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .
Dimethyl phthalate- 13C6 (DMP- 13C6) is the 13C-labeled Dimethyl phthalate (HY-N7106). Dimethyl phthalate (DMP) can be used as a plasticizer to impart flexibility to rigid polyvinyl chloride (PVC) resin. Additionally, Dimethyl phthalate is an oral active endocrine disruptor that can cause ovarian dysfunction in mice. Dimethyl phthalate can also induce oxidative stress and apoptosis in cells, thereby affecting blood and red blood cell function in rats .
16-Ketoestradiol-d5 (16-keto-17β-Estradiol-d5) is the deuterium labeled 16-Ketoestradiol (HY-W587691). 6-Ketoestradiol is an active metabolite of the endogenous estrogen estrone .
Isosorbide dinitrate- 13C6 is the 13C labeled Isosorbide dinitrate . Isosorbide dinitrate (ISDN) is an NO donor that prevents LV remodeling and degradation of cardiac function following myocardial infarction (MI) .
trans-2-Decenal-d2 is deuterated labeled trans-2-Decenal (HY-W015551). trans-2-Decenal is an important raw material and intermediate used in organic synthesis, medicine, pesticides and dyes.
2-(Dodecyloxy)ethanol-d25 (Ethylene glycol monododecyl ether-d25) is the deuterium labeled 2-(Dodecyloxy)ethanol (HY-W250300). 2-(Dodecyloxy)ethanol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Angiotensin II human- 13C6, 15N TFA (Ang II- 13C6, 15N TFA) is 13C- and 15N-labeled Angiotensin II human (TFA) (HY-13948B). Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions .
Liothyronine- 13C9, 15N is the 13C and 15N labeled Liothyronine . Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively [4].
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N) is the 13C and 15N labeled AICAR (HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
Nicotinamide- 15N, 13C3 is the 13C-labeled and 15N-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Tofacitinib- 13C3, 15N (Tasocitinib- 13C3, 15N) is 13C and 15N labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
2-(1-Ethoxyethylidene)malononitrile- 13C2 (Propanedinitrile, 2-(1-ethoxyethylidene)- 13C2) is the 13C-labeled 2-(1-Ethoxyethylidene)malononitrile (HY-W008403).
Entecavir- 13C2, 15N (BMS200475- 13C2, 15N; SQ34676- 13C2, 15N) is a 13C- and 15N-labeled Entecavir (HY-13623). Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
Tegafur- 13C, 15N2 (FT 207- 13C, 15N2) is the 13C- and 15N-labeled Tegafur (HY-17400). Tegafur (FT 207; NSC 148958) is a chemotherapeutic 5-FU proagent used in the treatment of cancers; is a component of tegafur-uracil.
L-Serine- 13C3, 15N is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Mandelic acid-2,3,4,5,6-d5 is the deuterium labeled Mandelic acid. Mandelic acid ((±)-Mandelic acid), an alpha-hydroxycarboxylic acid, has been widely used as an intermediate of pharmaceutical and fine chemicals. Mandelic acid shows antimicrobial activity and has been used for the research of urinary tract infections and vaginal trichomoniasis. Mandelic acid exhibits high sperm-immobilizing activity and low vaginal irritation .
Serotonin- 13C2, 15N hydrochloride is the 13C- and 15N-labeled Serotonin hydrochloride (HY-B1473). Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Hypoxanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Didanosine- 13C2, 15N (2',3'-Dideoxyinosine- 13C2, 15N; ddI- 13C2, 15N) is the 13C- and 15N-labeled labeled Didanosine (HY-B0249). Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
Hypoxanthine- 13C2, 15N is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Cefdinir- 13C, 15N2 (FK-482- 13C, 15N2) is 13C and 15N labeled Cefdinir. Cefdinir (FK-482) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for infections caused by several Gram-negative and Gram-positive bacteria. Cefdinir can be used for the research of common bacterial infections of the ear, sinus, throat, and skin .
2'-Deoxyguanosine- 13C, 15N2 (Deoxyguanosine- 13C, 15N2; Guanine deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled 2'-Deoxyguanosine (HY-17563). 2’-Deoxyguanosine (Deoxyguanosine) is a purine nucleoside with a variety of biological activities. 2’-Deoxyguanosine can induce DNA division in mouse thymus cells. 2’-Deoxyguanosine is a potent cell division inhibitor in plant cells .
Zileuton- 13C2, 15N is 15N and 13C labeled Zileuton (HY-14164). Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
Lamotrigine- 13C7, 15N (LTG- 13C7, 15N) is 13C and 15N labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
6-Mercaptopurine- 13C2, 15N is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
1,2-Dioleoyl-sn-glycero-3-phosphocholine-d9 is deuterium labeled 1,2-Dioleoyl-sn-glycero-3-phosphocholine. 1,2-Dioleoyl-sn-glycero-3-phosphocholine (DOPC) is a phospholipid and is commonly used alone, or with other components, in the generation of micelle
Fenofibric acid- 13C8 (FNF acid- 13C8) is 13C labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine-d70 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine. 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE) is a phosphoethanolamine (PE) lipid that can be used in the synthesis
Uridine- 13C9 (β-Uridine- 13C9) is a 13C9-labeled form of Uridine (HY-B1449). Uridine (β-Uridine) is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Oxiran-2-ylmethyl hexadecanoate-d31 is deuterium labeled Glycidyl palmitate. Glycidyl Palmitate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
D-Ribofuranose- 13C5 (D-Ribose- 13C5) is the 13C-labeled D-Ribofuranose (HY-113375). D-Ribofuranose (D-Ribose) is an endogenous metabolite present in Cerebrospinal_Fluid that can be used for the research of Ribose 5 Phosphate Isomerase Deficiency and Medium Chain Acyl Co A Dehydrogenase Deficiency .
Taurine- 13C2 is the 13C-labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
trans-2-Hexenal-d2-1 is the deuterium labeled trans-2-Hexenal (HY-128429). trans-2-Hexenal ((E)-2-Hexenal) is a volatile compound widely present in fresh plants, vegetables, and fruits, with a unique leafy aroma. trans-2-Hexenal has antifungal activity and can also inhibit the germination of soybean seeds and the growth of seedlings. In addition, trans-2-Hexenal can be used to determine low-molecular-weight carbonyl compounds that are reactive with biological nucleophiles in biological samples .
Uridine 5'-monophosphate-d11 (5'- Uridylic acid-d11) dilithium is deuterium labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Lansoprazole sulfone- 13C6 (AG-1813- 13C6) is 13C labeled Lansoprazole sulfone. Lansoprazole sulfone (AG-1813) is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease .
L-Phenylalanine-d is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
L-Phenylalanine-d2 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Avibactam sodium salt- 13C5 (NXL-104- 13C5) is 13C labeled Avibactam (sodium). Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
DPPG-d62 (sodium) is deuterium labeled DPPG. DPPG sodium (1,2-Dipalmitoyl-sn-glycero-3-PG sodium) is a phospholipid containing the long-chain(16:0) palmitic acid inserted at the sn-1 and sn-2 positions. DPPG sodium is used in the generation of micelles, l
L-Valine- 13C5 ((S)-Valine- 13C5) is the 13C-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Ibuprofen- 13C,d3 is the 13C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively .
L-Arginine- 13C6 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Benzene-1,3,5-tricarboxylic acid-d3 is the deuterium labeled Benzene-1,3,5-tricarboxylic acid (HY-78985). Benzene-1,3,5-tricarboxylic acid (Trimesic acid) is a scaffold. Benzene-1,3,5-tricarboxylic acid enhances the binding ability of bicyclic peptides to proteins and improves the mechanical stability of hydrogels .
Phosphoenolpyruvic acid (potassium)- 13C2 is the 13C labeled Phosphoenolpyruvic acid potassium (HY-W008807) . Phosphoenolpyruvic acid (Phosphoenolpyruvate) potassium is a glycolysis metabolite with a high-energy phosphate group. Phosphoenolpyruvic acid potassium is involved in glycolysis and gluconeogenesis, and used as energy source to produce ATP, under the energy-limited conditions. Phosphoenolpyruvic acid potassium also exhibits cytoprotective and anti-oxidative properties .
L-Arginine- 15N2 (hydrochloride) is the 15N-labeled L-Arginine (hydrochloride). L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
L-Phenylalanine-d7 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Nifedipine-13C8 is a deuterated labeled Nifedipine . Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
Homovanillic Acid- 13C6 (Vanilacetic acid- 13C6) is the 13C-labeled Homovanillic acid (HY-N0384). Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
L-Phenylalanine-d8 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Indole-3-carboxaldehyde- 13C (3-Formylindole- 13C) is a 13C labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde (3-Formylindole), a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin .
Diethylene glycol-d8 (2,2'-Oxybis(ethan-1-ol)-d8) is the deuterium labeled Diethylene glycol (HY-B1952). Diethylene glycol has excellent solubility and reactivity in certain chemical reactions and can help accelerate the activation of certain reactants.
Myrcene- 13C3 is 13C labeled Myrcene (HY-N0803). Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity [4] .
Tolfenamic acid- 13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
Cefadroxil- 13C6 (BL-S 578- 13C6) is 13C labeled Cefadroxil (HY-B1190). Cefadroxil is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain [4] .
N-(Phenylacetyl-d5)glycine is the deuterium labeled Phenylacetylglycine. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion .
2,4-Di-tert-butylphenol-d19(2,4-DTBP-d19) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
Saquinavir- 13C6 (Ro 31-8959- 13C6) is 13C labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells .
DPPC-13C2 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [4] .
Adipic acid- 13C2 (Hexanedioic acid- 13C2) is 13C labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Vitamin B12- 13C7 is the 13C-labeled Vitamin B12. Vitamin B12 is a vitamin. Vitamin B12 plays a key role in the normal functioning of the brain and nervous system, and for the formation of blood .
N4-Acetylsulfamethoxazole- 13C6 (Acetylsulfamethoxazole- 13C6) is the 13C-labeled N4-Acetylsulfamethoxazole (HY-W013266). N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of?Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections .
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Lactic acid- 13C2 (DL-Lactic acid- 13C2) sodium is the 13C-labeled Lactic acid sodium . Lactic acid (DL-Lactic acid) sodium is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium is an oncometabolite and has immune protective role of lactate in anti-tumor immunity . Lactic acid sodium also has antimicrobial activity, which can be used as a food preservative .
Phenylglyoxylic acid- 13C8 (Benzoylformic acid- 13C8) is the 13C-labeled Phenylglyoxylic acid (HY-W010255). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human. Phenylglyoxylic acid can be used as drug intermediate for synthesis of antineoplastic compounds .
N-Hexanoyl-L-Homoserine lactone-d3 (C6-HSL-d3) is deuterium labeled N-Hexanoyl-L-homoserine lactone. N-Hexanoyl-L-homoserine lactone is a short-chained N-acyl homoserine lactone (AHL). Diatoms are frequently found in association with Proteobacteria, many members of which employ cell-to-cell communication via AHLs in aquatic habitats .
Pyruvic acid- 13C2 (Acetylformic acid- 13C2) is the 13C-labeled Pyruvic acid (HY-Y0781). Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats.
Ercalcitriol-d3 is the deuterium labeled Ercalcitriol. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Glycolic acid- 13C2 is the 13C-labeled Glycolic acid (HY-W015967). Glycolic acid- 13C2 is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
Secalciferol-d6 is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification .
2,4-Di-tert-butylphenol-d21(2,4-DTBP-d21) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
Triacetonamine-d17 (2,2,6,6-Tetramethyl-4-piperidone-d17) is the deuterium labeled Triacetonamine. Triacetonamine has oral activity and can induce acute liver failure (ALF) in rats .
Diphenyl ether- 13C12 is 13C labeled Diphenyl ether. Oxydibenzene is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Moxonidine- 13C,d3 (BDF5895- 13C,d3) is the 13C-labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
Uridine- 13C5 (β-Uridine- 13C5) is a 13C labeled Uridine (HY-B1449). Uridine (β-Uridine) is a nucleoside compound consisting of uracil and a ribose ring, which are linked by a β-N1- glycosyl bond.
Fructose-alanine- 13C6 is 13C labeled Fructose-alanine. Fructose-alanine, an amadori compound, is an aroma precursor that formed in the initial phase of the Maillard reaction (MR). Fructose-alanine can be isolated from tobacco, miso and white wine. Fructose-alanine significantly induces oxidative browning and correlates with Maillard product (furfuryl alcohol) with a roasted and sweet aroma. Fructose-alanine can be used for food industry and tobacco processing research [4].
Adipic acid- 13C6 (Hexanedioic acid- 13C6) is the 13C labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Octachlorodibenzo-p-dioxin- 13C12 is Octachlorodibenzo-p-dioxin- 13 C-labeled octachlorodibenzo-p-dioxin- 13C. Octachlorodibenzo-p-dioxin is a widespread environmental pollutant .
Metformin- 13C2 (1,1-Dimethylbiguanide- 13C2) hydrochloride is the 13C-labeled Metformin hydrochloride (HY-17471A). Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [4] .
Pyruvic acid-13C is isotype-labeled compound of Pyruvic acid. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats .
5'-Deoxy-5-fluorocytidine-d3 is deuterated labeled 5'-Deoxy-5-fluorocytidine (HY-W009538). 5'-Deoxy-5-fluorocytidine (5-Fluoro-5'-deoxycytidine) is a cytidine analog and metabolite of Capecitabine (HY-B0016). 5'-Deoxy-5-fluorocytidine is converted from Capecitabine by carboxylesterase in the liver. 5'-Deoxy-5-fluorocytidine is deaminated by cytidine deaminase to generate 5'-deoxy-5-fluorouridine, which is finally converted into 5-fluorouracil (HY-90006) by thymidine phosphorylase in tumor tissues to exert anti-tumor effects. 5'-Deoxy-5-fluorocytidine is used in the researches for solid tumors such as colorectal cancer, non-small cell lung cancer and breast cancer [4].
trans-Stilbene- 13C2 ((E)-Stilbene- 13C2) is the 13C labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
Eplerenone- 13C,d3 (Epoxymexrenone- 13C,d3) is 13C labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC50 value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV) .
Sulfamethoxazole- 13C6 (Ro 4-2130- 13C6) is a 13C labeled Sulfamethoxazole (HY-B0322). Sulfamethoxazole (Ro 4-2130) is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
N-Acetylglycine- 13C2, 15N (Aceturic acid- 13C2, 15N) is the 13C- and 15N-labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
Orotic acid- 13C, 15N2 (monohydrate) is the 13C and 15N labeled Orotic acid . Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats [4].
Salicylic acid- 13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity .
N-Lactoyl-Phenylalanine- 13C6 (Lac-Phe- 13C6) is 13C labeled N-Lactoyl-Phenylalanine. N-Lactoyl-Phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-Phenylalanine can reduce obesity and improve glucose tolerance .
Pemetrexed disodium- 13C5 (LY231514 disodium- 13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d62 (POPC-d64) is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for the preparation of liposomes and studying the properties of lipid bilayers .
3-Hydroxy Midostaurin- 13C6 (CGP52421- 13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
Zafirlukast- 13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
5,6-trans-Bimatoprost-d5 (5,6-trans-AGN 192024-d5) is the deuterium labeled 5,6-trans-Bimatoprost (HY-B0191A). 5,6-trans-Bimatoprost is the isomer of Bimatoprost (HY-B0191), and can be used as an experimental control. Bimatoprost is a prostaglandin analogue that can be used in studies of ocular hypertension and glaucoma and also has anti-fat formation effects.
Selpercatinib- 13C,d3 (LOXO-292- 13C,d3) is 13C labeled Selpercatinib. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity .
5-Methylcytidine 5′-triphosphate-d3 trisodium is the deuterium labeled 5-Methylcytidine 5’-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5′-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5′-triphosphate trisodium can apply in replacing unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Sucrose- 13C6-1 is 13C labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose?can be applied in some animal models, including metabolic disease, obesity,?diet on preference,?and diabetes, et al .
Adenosine-d-2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Chlortetracycline-13C,d3 hydrochloride (7-Chlorotetracycline-13C,d3 hydrochloride) is the 13C- and deuterium labeled Chlortetracycline hydrochloride (HY-B1327). Chlortetracycline hydrochloride is an orally active, selective antibiotic, that inhibits methanogenic bacteria through inhibition of bacterial protein synthesis. Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, that inhibits binding of aminoacyl-tRNA to ribosomes [4] .
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Axitinib- 13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50 values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .
17β-Estradiol sulfate-d3 sodium (17β-Estradiol 3-sulfate-d3 sodium) is the deuterium labeled 17β-Estradiol sulfate sodium (HY-141672). 17β-Estradiol sulfate sodium, also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid .
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride . Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Sulfasalazine-d3, 15N is 15N and deuterated labeled Sulfasalazine (HY-14655). Sulfasalazine (NSC 667219) is an anti-rheumatic agent for the research of rheumatoid arthritis and ulcerative colitis. Sulfasalazine can suppress NF-κB activity. Sulfasalazine is a type 1 ferroptosis inducer [4].
Emtricitabine- 15N,d2 is a 15N-labeled and deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [4] .
Succinic acid- 13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
Moxonidine- 13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis [4] .
Adenosine-d-1 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib . Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Guanosine triphosphate- 15N5 (GTP- 15N5) dilithium is 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Fmoc-Gly-OH- 13C2 (Fmoc-glycine- 13C2) is a 13C-labeled Fmoc-Gly-OH (HY-Y1250). Fmoc-Gly-OH (Fmoc glycine) is a Fmoc-protected glycine derivative, can be used for the synthesis of compounds .
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively .
Triclocarban- 13C6 is the 13C labeled isotope of Triclocarban (HY-B1805). Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
3-Phenoxybenzoic acid- 13C6 is the 13C6 labeled 3-Phenoxybenzoic acid. 3-Phenoxybenzoic acid is the metabolite of pyrethroid insecticides. 3-Phenoxybenzoic acid induces immunotoxicity and oxidative stress, and inhibits the phagocytic ability of macrophages .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d31 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
Linagliptin- 13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levomefolic acid- 13C5 is the 13C labeled Levomefolic acid . Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid (HY-B0172A). Isoallolithocholic acid is a T cell regulator and enhances regulatory T cells (Tregs) differentiation .
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base . Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ [4].
Saxagliptin-15N,d2 Hydrochloride (BMS-477118-15N,d2 Hydrochloride) is the 15N and deuterium labeled isotope of Saxagliptin (HY-10285). Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4(DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
Raltegravir- 13C,d3 potassium is 13C labeled Raltegravir potassium (HY-10353A). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
Pravastatin- 13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
L-Alanine-1,2- 13C2 (Alanine- 13C2) is 13C labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
2'-Deoxy-N-ethylguanosine-d6 (N2-Ethyl-2'-deoxyguanosine-d6) is the deuterium labeled 2-(Ethylamino)-9-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1H-purin-6(9H)-one (HY-W013267).
Guanosine triphosphate- 13C10 (GTP- 13C10) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Cholestenone- 13C2 is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells .
D-α-Hydroxyglutaric acid-d5 disodium (Disodium (R)-2-hydroxyglutarate-d5) is the deuterium labeled D-α-Hydroxyglutaric acid disodium (HY-100542). D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling [4] .
rac-1-Linoleoyl-3-chloropropanediol-d5 is deuterium labeled 1-Linoleoyl-3-chloropropanediolte. 1-Linoleoyl-3-chloropropanediolte (3-Chloro-2-hydroxypropyl (9Z,12Z)-octadeca-9,12-dienoate) is an ester product .
Flurbiprofen- 13C,d3 is the 13C- and deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d82 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
MTSSL- 15N,d15-1 (Otmpmms- 15N,d15) is the deuterium and 15N-labeled MTSSL (HY-130509). MTSSL (Otmpmms) is highly reactive thiol-specific spin label, which is used to label protein thiol residues for protein structure and dynamics determination and protein-protein interaction studies .
Thiabendazole- 13C6 is the 13C6 labeled Thiabendazole. Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
2,2-Dibromomalonamide- 13C3 (Dibromo Malonamide- 13C3) is the 13C-labeled 2,2-Dibromomalonamide (HY-W324382). 2,2-Dibromomalonamide is a biochemical agent .
Fluvoxamine- 13C, d3 maleate is 13C and deuterated labeled Fluvoxamine maleate (HY-B0103A). Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
Butanedioic acid- 13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Velpatasvir- 13C,d3 (GS-5816- 13C,d3) is 13C and deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
Riociguat- 13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
Benzyl 4-hydroxybenzoate- 13C6 (Benzyl Paraben- 13C6) is the 13C-labeled Benzyl 4-hydroxybenzoate (HY-W013482). Benzyl 4-hydroxybenzoate is a prominent material. Benzyl 4-hydroxybenzoate can be used as an excipient, such as bacteriostatic agent, preservative. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Zafirlukast- 13C,d3 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Norflurazon- 13C,d3 (SAN 9789- 13C,d3) is the deuterium and 13C-labeled Norflurazon (HY-114849). Norflurazon (SAN 9789) is a bleaching herbicide. Norflurazon can block carotenoid biosynthesis by inhibiting phytoene desaturase activity .
Benoxaprofen- 13C,d3 (LRCL 3794- 13C,d3) is the deuterium and 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a potent and long-acting anti-inflammatory and antipyretic compound. Benoxaprofen is a relatively weak inhibitor of cyclooxygenase in in vitro systems, inhibits lipoxygenase in other systems, and inhibits monocyte migration in some animal models of inflammation .
Rabeprazole- 13C,d3 (sodium) (LY307640- 13C,d3 (sodium)) is 13C labeled Rabeprazole (sodium). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
L-Histidine- 15N3 hydrochloride hydrate is the 15N-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Acetyl-L-carnitine-d3-1 (O-Acetyl-L-carnitine-d3-1) hydrochloride is the deuterium labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression .
5-Methylcytidine 5'-triphosphate-d8 trisodium is the deuterium-labeled form of 5-Methylcytidine 5'-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5'-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5'-triphosphate trisodium can be used to replace unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Asenapine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
Trelagliptin-13C,d3 is a deuterated labeled Trelagliptin . Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) .
Lamivudine- 15N,d2 is 15N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
Methyl arachidonate- 13C5 (Arachidonic acid methyl ester- 13C5) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
Acetophenone- 13C8 (1-Phenylethan-1-One- 13C8) is the 13C-labeled Acetophenone (HY-Y0989). Acetophenone (1-Phenylethan-1-One) is an organic compound with simple structure. Acetophenone can be bioreduced to phenylethanol (PEA) .
Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
4-Methyl-2-oxopentanoic acid-d7 (α-Ketoisocaproic acid-d7) sodium is the deuterium labeled 4-Methyl-2-oxopentanoic acid (HY-W012722).4-Methyl-2-oxopentanoic acid is a metabolite of L-leucine and is involved in energy metabolism. 4-Methyl-2-oxopentanoic acid increases endoplasmic reticulum stress, promotes lipid accumulation in preadipocytes and insulin resistance by impairing mTOR and autophagy signaling pathways .
Argininic acid- 13C6 (L-Argininic Acid- 13C6) is the 13C-labeled Argininic acid (HY-113079). Argininic acid is an α-amino acid that is used in the biosynthesis of proteins.
1-(4-Chlorophenyl)cyclobutanecarbonitrile-d6(1-(4-Chlorophenyl)-1-cyclobutanecarbonitrile-d6) is the deuterium labeled 1-(4-Chlorophenyl)cyclobutanecarbonitrile (HY-W010002).
2-Methyl-3-(trifluoromethyl)aniline-d3 (3-Trifluoromethyl-2-methylaniline-d3) is deuterium labeled 2-Methyl-3-(trifluoromethyl)aniline. 2-Methyl-3-(trifluoromethyl)aniline is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Butenafine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled. Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Triclocarban- 13C13 (3,4,4'-Trichlorocarbanilide- 13C13) is 13C labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes [4].
Adenosine monophosphate- 13C10 (AMP- 13C10) dilithium is 13C-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Asenapine- 13C,d3 Maleate is the deuterium labeled and 13C-Asenapine Maleate (HY-11100). Asenapine (Org 5222) Maleate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine Maleate can be used in the research of schizophrenia and bipolar disorder .
Sumatriptan-d6 (formate) (GR 43175 free base-d6 (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [4] .
L-Histidine- 13C6 (hydrochloride hydrate) is the 13C-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Methyl Paraben- 13C6 (Methyl 4-hydroxybenzoate- 13C6) is a 13C labeled Methyl Paraben (HY-N0349) . Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity .
Rabeprazole-13C,d3 is a deuterated labeled Rabeprazole . Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux [4].
2,3-Diphosphoglyceric acid-d3 ammonium (2,3-DPG-d3 ammonium) is the deuterium labeled 2,3-Diphosphoglyceric acid (HY-113050). 2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2, 3-diphosphoglyceric acid has antiparasitic activity. 2,3-Diphosphoglyceric acid can be used in the study of Alzheimer's disease (AD) [4].
Ketoprofen- 13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively .
Carisbamate-d2,- 15N (RWJ-333369-d2,- 15N) is the deuterium labeled Carisbamate (HY-14948). Carisbamate (RWJ-333369) is an orally active neuromodulator. Carisbamate prevents the development and production of epilep-like discharges and has a neuroprotective effect after in vitro epilepticus-like injury. Carisbamate has good antiepileptic activity in genetic models of generalized and nonconvulsive epilepsy .
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Oseltamivir- 13C,d3 (phosphate) (GS 4104- 13C,d3 (phosphate)) is 13C labeled Oseltamivir (phosphate). Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Asenapine-d3, 13C (Org 5222-d3, 13C) is deuterium and 13C labeled Asenapine. Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder .
Fmoc-Gly-OH-2,2-d2 (Fmoc-glycine-2,2-d2) is the deuterium labeled Fmoc-Gly-OH (HY-Y1250). Fmoc-Gly-OH (Fmoc glycine) is a Fmoc-protected glycine derivative, can be used for the synthesis of compounds .
Lactic acid-d3 (DL-Lactic acid-d3) sodium (60% in water) is the deuterium labeled Lactic acid sodium (60% in water) (HY-B2227B) . Lactic acid (DL-Lactic acid) sodium (60% w/w in water) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium (60% w/w in water) is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium (60% w/w in water) is an oncometabolite and has immune protective role of lactate in anti-tumor immunity . Lactic acid sodium (60% w/w in water) also has antimicrobial activity, which can be used as a food preservative .
Tecarfarin- 13C,d3 (ATI-5923- 13C,d3) is 13C labeled Tecarfarin. Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X . Tecarfarin has the antithrombotic activity .
Hypoxanthine- 13C2, 15N-1 is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
β-Alanine- 13C3, 15N is the 13C- and 15N-labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
(1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide-d4 is deuterated labeled (1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide.
2′,2′-Difluorodeoxyuridine- 13C, 15N2 (dFdU- 13C, 15N2) is a 13C- and 15N-labeled compound. 2’,2’-Difluorodeoxyuridine (dFdU) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells [4].
O-Phospho-L-serine- 13C3, 15N is the 13C- and 15N-labeled O-Phospho-L-serine. O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2 .
L-Valine- 15N,d8 ((S)-Valine- 15N,d8) is the deuterium and 15N labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
(2R)-Octyl-α-hydroxyglutarate-d17 ((2R)-Octyl-2-HG-d17) is deuterium labeled (2R)-Octyl-α-hydroxyglutarate (HY-103641). (2R)-Octyl-α-hydroxyglutarate is a modified form of S-isomer 2-Hydroxyglutarate .
1-Palmitoyl-sn-glycero-3-phosphocholine-d31 (16:0 Lyso PC-d31) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Indole-3-carboxaldehyde- 13C8 (3-Formylindole- 13C8) is the 13C-labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde, a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin. Indole-3-carboxaldehyde also enhances the epithelial barrier and anti-inflammatory activity in the intestinal tract .
L-Glutamine- 13C5 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Apixaban- 13C,d3 (BMS-562247-01- 13C,d3) is a deuterium and 13C labeled Apixaban (HY-50667). Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively .
ATP- 13C2 (Adenosine 5'-triphosphate- 13C2) dilithium is 13C-labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
(Z)-Aconitic acid- 13C6 is the 13C-labeled (Z)-Aconitic acid (HY-W016814). (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is the cis-isomer of Aconitic acid. (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is an intermediate in the tricarboxylic acid cycle produced by the dehydration of citric acid.
Calcifediol- 13C5 monohydrate is the 13C-labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels .
Deoxythymidine-5'-triphosphate- 15N2 (dTTP- 15N2) dilithium is 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin . Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
ATP- 13C10 (Adenosine 5'-triphosphate- 13C10) dilithium is 13C-labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Glycidyl palmitate- 13C16 (Oxiran-2-ylmethyl palmitate- 13C16) is the 13C-labeled Glycidyl palmitate (HY-W127578). Glycidyl Palmitate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
L-Alanine- 13C3 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
MCPA- 13C8 is the 13C-labeled MCPA (HY-B0859). MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds [4] .
1-Palmitoyl-sn-glycero-3-phosphocholine-d9 (16:0 Lyso PC-d9) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Flavin adenine dinucleotide- 13C5 (FAD- 13C5) ammonium is 13C labeled Flavin adenine dinucleotide (HY-B1654). Flavin adenine dinucleotide (FAD) is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.
2,3’-Anhydrothymidine-d3 (2’-Deoxy-3’,2-anhydro-5-methyluridine-d3) is the deuterium labeled 2,3’-Anhydrothymidine (HY-154340). 2,3’-Anhydrothymidine; 2’-Deoxy-3’,2-anhydro-5-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
1-Palmitoyl-sn-glycero-3-phosphocholine-d49 (16:0 Lyso PC-d49) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Guanosine 5'-diphosphate- 13C10 (GDP- 13C10) dilithium is 13C-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
1-Acetyl-4-(4-hydroxyphenyl)piperazine-d8 (Tetraethoxy C methyl propane-d8) is the deuterium labeled 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone (HY-W014037).
DL-Lysine- 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 15N2 hydrochloride) is 15N labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
2-(3,4-Dimethoxyphenyl)-3-methylbutanenitrile-d7 (alpha-Isopropyl homoveratronitrile-d7) is the deuterium labeled 2-(3,4-Dimethoxyphenyl)-3-methylbutanenitrile (HY-W101691).
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
Uridine 5'-monophosphate- 15N2 (5'-Uridylic acid- 15N2) is the 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Caffeic acid- 13C3 is an 13C labeled caffeic acid. Caffeic acid is a phytonutrient belonging to the flavonoids. Caffeic acid and its derivatives, are potential antimicrobial agents, chronic infection induced by microbes such as bacteria, fungi, and viruses .
L-Alanine- 13C2 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
2-Methyl-2-[(trimethylsilyl)oxy]propanenitrile-d6 (2-methyl-2-trimethylsilyloxypropanenitrile-d6) is the deuterium labeled 2-Methyl-2-[(trimethylsilyl)oxy]propanenitrile (HY-W176004).
AChE-IN-23-d10 (4-Amino-Alpha-diethyl amino-o-cresol-d10 (dihydrochloride)) is the deuterium labeled AChE-IN-23 (HY-W077226). AChE-IN-23 (compound 3h) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 48.3 μM .
Homovanillic acid- 13C,d3 (Vanilacetic acid- 13C,d3) is 13C and deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
Guanosine 5'-diphosphate- 15N5 (GDP- 15N5) dilithium is 15N labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI) .
5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) [4].
DL-Lysine- 13C6 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6 hydrochloride) is 13C-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
L-Glutamine- 15N2 is the 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
N,N-Di-(beta-carboethoxyethyl)methylamine-d8 (Di-Beta-carbethoxyethyl-methylamine-d8) is the deuterium labeled N,N-Di-(beta-carboethoxyethyl)methylamine (HY-76097).
Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
ATP- 15N5 (Adenosine 5'-triphosphate- 15N5) dilithium is 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Moxifloxacin- 13C,d3 hydrochloride (BAY 12-8039- 13C,d3) is 13C and deuterated labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
Tempol-d17, 15N is the deuterium labeled Tempol . Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS) .
D-Glutamic acid- 13C5 ((R)-Glutamic acid- 13C5) is 13C labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
Deoxythymidine-5'-triphosphate- 13C10 (dTTP- 13C10) dilithium is 13C-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
(Rac)-Folic acid- 13C5, 15N is the 13C-labeled and 15N-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
L-Glutathione reduced- 13C2, 15N is the 13C- and 15N-labeled L-Glutathione reduced. L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
dGTP- 13C10 (2'-Deoxyguanosine-5'-triphosphate- 13C10) dilithium is 13C-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
D-(+)-Glucono-1,5-lactone- 13C6 (Gluconic acid lactone- 13C6) is the 13C-labeled D-(+)-Glucono-1,5-lactone (HY-I0301). D-(+)-Glucono-1,5-lactone is a polyhydroxy (PHA) that is capable of metal chelating, moisturizing and antioxidant activity.
L-Gulono-1,4-lactone- 13C6 (L-Gulonolactone- 13C6) is the 13C-labeled L-Gulono-1,4-lactone (HY-W016628). L-Gulono-1,4-lactone is a substrate of L-gulono-1,4-lactone oxidoreductase, which catalyzes the last step of the biosynthesis of L-ascorbic (Vatamin) C. In other words, L-Gulono-1,4-lactone is a direct precursor of vitamin C in animals, in plants and in some protists.
2-Naphthoic acid- 13C6 (Naphthalene-2-carboxylic acid- 13C6) is the 13C-labeled 2-Naphthoic acid (HY-W007437). 2-Naphthoic acid is an organic compound commonly used as a raw material for dyes and the production of other chemicals. It can form dyes with other organic substances and is widely used in textile, printing and manufacturing fields. In addition, the compound is also used as a photosensitive material and a lubricant.
3-?Bromo-?L-?tyrosine- 13C6 (3-Bromo-Tyr- 13C6) is a 13C-labeled 3-?Bromo-?L-?tyrosine (HY-W018386). 3- Bromo- L- tyrosine (3-Bromo-Tyr) is a tyrosine derivative .
11-Beta-hydroxyandrostenedione-d7 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor
Lamotrigine- 13C (LTG- 13C) is 13C labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
4-Octyl itaconate- 13C5-1 is 13C-labeled 4-Octyl itaconate (HY-112675). Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
N4-Acetylsulfamethazine- 13C6 (Sulfamethazine-n4-acetyl- 13C6) is the 13C-labeled N4-Acetylsulfamethazine (HY-W290839). N4-Acetylsulfamethazine is a metabolite of Sulfamethazine (HY-B0035). Sulfamethazine is one of the most frequently used sulfonamides in the poultry farming industry .
2'-Deoxyadenosine-5'-triphosphate- 13C10 (dATP- 13C10) dilithium is 13C-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
DMT-dA(bz) Phosphoramidite- 15N5 is the 15N labeled DMT-dA(bz) Phosphoramidite . DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA .
Lysophosphatidylcholine 18:2-d9 is deuterium labeled Lysophosphatidylcholine 18:2. Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary
Topiramate- 13C (McN 4853- 13C) is 13C labeled Topiramate. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
Dehydro Nifedipine-13C,d3 is a deuterated labeled Dehydro Nifedipine . Dehydro nifedipine (BAY-b 4759) is a metabolite of Nifedipine (HY-B0284). Nifedipine (BAY-a-1040) is a potent calcium channel blocker and an agent of choice for cardiac insufficiencies .
(Rac)-Nebivolol-d2, 15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
Ethyl 3,4-Dihydroxybenzoate- 13C3 (Protocatechuic acid ethyl ester- 13C3) is the 13C-labeled Ethyl 3,4-dihydroxybenzoate (HY-W016409). Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema [4].
5-(Hydroxymethyl)-1-phenylpyridin-2(1H)-one-d5 (Pirfenidone Impurity 6-d5) is the deuterium labeled 5-(Hydroxymethyl)-1-phenylpyridin-2(1H)-one (HY-W349458).
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase .
PhIP-d3(2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine-d3) is the deuterium labeled PhIP (HY-118716). PhIP (2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine) is the most abundant of generation of heterocyclic amines (HCA), resulted in the cooking of meat . DNA damaging and mutagenic activities. PhIP also has oestrogenic activity that could contribute to its tissue specific carcinogenicity .
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
9(S)-HODE- 13C18 ((+)-α-Dimophecolic acid- 13C18) is 13C labeled 9S-HODE. 9S-HODE (Alpha-dimorphecolic acid) is an octadecadienoic acid and the main active derivative of linoleic acid, which can reduce the viability of HL-60 cells and induce apoptosis. 9S-HODE is rich in lipid peroxidation (LPO) products and is almost an ideal marker for LPO .
3-Hydroxybutyric acid- 13C2 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids .
2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development .
Oleoyl coenzyme A- 13C18 (lithium) is the 13C labeled Oleoyl Coenzyme A lithium . Oleoyl coenzyme A (Oleoyl-CoA) is a thioester of oleic acid and coenzyme A. Oleoyl coenzyme A has a role as an Escherichia coli metabolite and a mouse metabolite .
Acetyl coenzyme A- 13C2 lithium is the 13C-labeled Acetyl coenzyme A (HY-114293). Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ethyl maltol-d5 is the deuterium labeled Ethyl maltol. Ethyl maltol (2-Ethyl-3-hydroxy-4H-pyran-4-one) is an orally active and important food additive and flavor enhancer. Ethyl maltol is less toxic to rats and dogs. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells .
Levomefolic acid- 13C,d3 is the deuterium labeled Levomefolic acid (HY-14781) . Levomefolic acid (5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .
3,5,6-Trichloro-2-pyridinol- 13C3 (TCPy- 13C3) is the 13C-labeled 3,5,6-Trichloro-2-pyridinol (HY-W018171). 3,5,6-Trichloro-2-pyridinol (TCPy) is the main degradation product of the herbicide Triclopyr and the insecticides Chlorpyrifos and Chlorpyrifos-methyl .
2-Ketoglutaric acid- 13C2 (Alpha-Ketoglutaric acid- 13C2) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
Varenicline- 13C 15N (CP 526555- 13C 15N) is 13C and 15N labeled Varenicline. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation [4] .
(1S,2R)-Tranylcypromine-d5 (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride . Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression [4].
2'-Deoxyadenosine-5'-triphosphate- 15N5 (dATP- 15N5) dilithium is 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Dibenzo[a,c]anthracene- 13C6 (2,3-Benzotriphenylene- 13C6) is 13C labeled Benzo[f]tetraphene. Benzo[f]tetraphene (Dibenz[a,c]anthracene) is a polycyclic aromatic hydrocarbon with significant antitumor activity. Benzo[f]tetraphene is used as a luminescent probe in cell biology research and can effectively detect reactive oxygen species in biological systems. Benzo[f]tetraphene can also be used as a potential photosensitizer and shows good application prospects in photodynamic inhibition.
(S)-Velpatasvir- 13C,d3 ((S)-GS-5816- 13C,d3) is 13C labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
Prostaglandin E2-1-glyceryl ester-d5 (PGE2-1-glyceyl ester-d5) is deuterium labeled Prostaglandin E2-1-glyceryl ester. Prostaglandin E2-1-glyceryl ester, a Prostaglandin Glycerol Ester, is an endocannabinoid ligand for the CB1 receptor. Prostaglandin E2-1-glyceryl ester induces rapid, transient elevation of intracellular free Ca 2+ .
2-Ketoglutaric acid- 13C5 (Alpha-Ketoglutaric acid- 13C5) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
1,2-Dioctanoyl-3-chloropropanediol-d5 is deuterium labeled 1,2-Dioctanoyl-3-chloropropanediol. 1,2-Dioctanoyl-3-chloropropanediol (3-Chloropropane-1,2-diyl dioctanoate) is an ester product .
L-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
VD3-d6 (Vitamin D3-26,26,26,27,27,27-d6) is deuterated VD3. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action [4].
2-Amino-6-hydroxypyrimidin-4(1H)-one- 13C2 (2-Amino-6-hydroxy-1H-pyrimidin-4-one- 13C2) is the 13C-labeled 2-Amino-6-hydroxypyrimidin-4(1H)-one (HY-Y0559).
1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE-d11 (15(S)-HETE-SAPE-d11) is deuterium labeled 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE. 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 (HY-N6687) by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE (SAPE) by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes .
1-beta-D-Arabinofuranosyluracil- 13C, 15N2 (1-b-D-Arabinofuranosyluracil- 13C, 15N2; Uracil 1-β-D-arabinofuranoside- 13C, 15N2) is the 13C- and 15N-labeled labeled 1-beta-D-Arabinofuranosyluracil (HY-N6652). 1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties . 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells .
2-Chloro-5-methylpyrimidin-4-amine- 15N2, 13C (4-Amino-2-chloro-5-methylpyrimidine- 15N2, 13C) is the 13C- and 15N-labeled 2-Chloro-5-methylpyrimidin-4-amine (HY-W002966).
L-Arginine-1,2- 13C2 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
L-Valine-d8 is a deuterated form of L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Cefazolin- 13C2, 15N (Cephazolin- 13C2, 15N) is 13C and 15N labeled Cefazolin. Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
Gimeracil- 13C3, 15N (Gimestat- 13C3, 15N) is 13C and 15N labeled Gimeracil. Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD) .
L-Lactic acid-2- 13C1 is the 13C-labeled L-Lactic acid (HY-Y0479). L-Lactic acid is a buildiing block which can be used as a precursor for the production of the bioplastic polymer poly-lactic acid .
Emtricitabine- 13C, 15N2 (BW1592- 13C, 15N2) is a 13C- and 15N-labeled Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Uridine 5'-monophosphate- 15N2 (5'- Uridylic acid- 15N2) dilithium is 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
rU Phosphoramidite- 13C9 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9) is 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
1-Palmitoyl-sn-glycero-3-phosphocholine-d9-1 (16:0 Lyso PC-d9-1) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Phenyl-boronic acid-d5 (Boronic acid,B-(phenyl-2,3,4,5,6)-d5) is the deuterium labeled Phenylboronic acid (HY-W001090). Phenylboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Nitrofurazone- 13C, 15N2 (Nitrofural- 13C, 15N2) is the 13C and 15N labled Nitrofurazone (HY-B0226) . Nitrofurazone is a potential antibiotic that can be used topically to treat wounds, burns, ulcers and skin infections to combat various microorganisms and to prepare surfactants . Nitrofurazone may affect the ecosystem function in Marine environment and affect the functional processes of epiphytic fauna .
[1,1'-Biphenyl]-3-amine-13C6 hydrochloride (Biphenyl-3-amine-13C6 hydrochloride) is the 13C labeled isotope of [1,1'-Biphenyl]-3-amine hydrochloride (HY-W106014) .
N-Acetyl-D-glucosamine-d3 (N-Acetyl-2-amino-2-deoxy-D-glucose-d3) is deuterium labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose), the D isomer of N-acetylglucosamine, is an orally active monosaccharide derivative of glucose with anti-tumor and anti-inflammation properties. N-Acetyl-D-Glucosamine is also a bacterial metabolite, which is found in Escherichia coli. N-Acetyl-D-Glucosamine can induce yeast-mycelial conversion in Candida albicans. N-Acetyl-D-Glucosamine also enhances healing of cartilaginous injuries in rabbits .
Uridine 5′-diphosphoglucose- 13C6 (UDP-D-Glucose- 13C6) disodium is the 13C labeled Uridine 5′-diphosphoglucose disodium (HY-N7032) . Uridine 5’-diphosphoglucose (UDP-glucose) disodium, secreted by cardiomyocytes during ischemia and reperfu, is a potent agonist of the proinflammatory P2Y14 receptor. It acts an important role in the regulation of inflammation and neutrophil polarization in neutrophils. Uridine 5’-diphosphoglucose disodium is also the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine 5’-diphosphoglucose disodium is promising for research in counteracting myocardial infarction/reperfusion (MIR)-induced inflammation in the heart tissue [4] .
L-Alanine- 13C,d is the 13C- and deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N,N'-Dimethyl-3,3'-dithiodipropionamide-d6 (Propanamide, 3,3'-dithiobis[n-methyl-d6) is the deuterium labeled N,N'-Dimethyl-3,3'-Dithiodipropionamide (HY-W045680).
2,6-Dichlorodiphenylamine- 13C6 (2,6-Dichloro-N-phenylaniline- 13C6) is the 13C-labeled 2,6-Dichlorodiphenylamine (HY-W012126). 2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a?COX?inhibitor, with?IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
2-Amino-2-deoxyglucose hydrochloride- 13C6 (D-Glucosamine Hydrochloride- 13C6) is the 13C-labeled 2-Amino-2-deoxyglucose hydrochloride (HY-N9459). 2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc .
Mannosan,95%- 13C6 (1,6-Anhydro-β-D-mannopyranose- 13C6) is the 13C-labeled Mannosan,95% (HY-124095). Mannosan,95% (1,6-Anhydro-β-D-mannopyranose,95%) is a class of biochemical reagents used in glycobiology research. Glycobiology studies the structure, synthesis, biology, and evolution of sugars. It involves carbohydrate chemistry, enzymology of glycan formation and degradation, protein-glycan recognition, and the role of glycans in biological systems. This field is closely related to basic research, biomedicine, and biotechnology .
5'-Deoxy-5-fluorocytidine-13C5 is the 13C labeled isotope of 5'-Deoxy-5-fluorocytidine (HY-W009538). 5'-Deoxy-5-fluorocytidine (5-Fluoro-5'-deoxycytidine) is a cytidine analog and metabolite of Capecitabine (HY-B0016). 5'-Deoxy-5-fluorocytidine is converted from Capecitabine by carboxylesterase in the liver. 5'-Deoxy-5-fluorocytidine is deaminated by cytidine deaminase to generate 5'-deoxy-5-fluorouridine, which is finally converted into 5-fluorouracil (HY-90006) by thymidine phosphorylase in tumor tissues to exert anti-tumor effects. 5'-Deoxy-5-fluorocytidine is used in the researches for solid tumors such as colorectal cancer, non-small cell lung cancer and breast cancer [4].
1,5-Anhydrosorbitol- 13C6 (1,5-Anhydro-D-glucitol- 13C6) is the 13C-labeled 1,5-Anhydrosorbitol (HY-113075). 1,5-Anhydrosorbitol is a short-term marker for glycemic control.
L-Phenylalanine- 13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
L-Phenylalanine- 13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
(3S,5R)-Fluvastatin-d6 (sodium)?is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
rU Phosphoramidite- 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 15N2) is 15N labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
trans-2,cis-6-Nonadienal- 13C2 is 13C labeled trans-2,cis-6-Nonadienal (HY-W127515). Trans-2, cis-6-NonadienalIt is an organic compound belonging to aldehydes. It has a strong, pungent smell and is commonly found in a variety of foods, including fruits and vegetables. Trans-2, cis-6-NonadienalIt has a variety of applications in the flavor and fragrance industry, especially as a fragrance agent in products such as perfume, cologne and air fresheners. In addition, it can also be used as an intermediate in the synthesis of various chemicals and drugs.
Uridine 5'-monophosphate- 13C9 (5'- Uridylic acid- 13C9) dilithium is 13C-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
(E)-3-Methyl-2-hexenoic acid-d5 ((2E)-3-Methyl-2-hexenoic acid-d5) is a deuterium labeled (E)-3-Methyl-2-hexenoic acid. (E)-3-Methyl-2-hexenoic acid is an axillary odor-related compound .
2-Thiouracil- 13C, 15N2 is the 13C, 15N labeled 2-Thiouracil. 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
(E)-3,4-Dimethoxycinnamic acid- 13C3 ((E)-O-Methylferulic acid- 13C3) is the 13C-labeled (E)-3,4-Dimethoxycinnamic acid (HY-N1778A). (E)-3,4-Dimethoxycinnamic acid is the less active isomer of 3,4-Dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway . Anti-apoptotic effects .
DL-Phenylmercapturic Acid- 13C6 (N-Acetyl-S-phenyl-L-cysteine- 13C6) is the 13C-labeled DL-Phenylmercapturic Acid (HY-W141770). DL-Phenylmercapturic Acid is a cysteine derivative .
Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Ethyl linoleate-d5 (Linoleic Acid ethyl ester-d5) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators . .
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole . Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC- 13C16 (POPC- 13C16) is 13C labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for the preparation of liposomes and studying the properties of lipid bilayers .
Urea- 13C, 15N2 is the 13C and 15N labeled Urea . Urea is a powerful protein denaturant via both direct and indirect mechanisms . A potent emollient and keratolytic agent . Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function . Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Fluconazole-13C2,15N (UK-49858-13C2,15N) is the 13C and 15N labeled isotope of Fluconazole (HY-B0101). Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL .
1,2-Dilauroyl-3-chloropropanediol-d5 (1,1′-[1-(Chloromethyl)-1,2-ethanediyl] didodecanoate-d5) is the deuterium labeled 1,2-Dilauroyl-3-chloropropanediol (HY-W587507). 1,2-Dilauroyl-3-chloropropanediol (1,1′-[1-(Chloromethyl)-1,2-ethanediyl] didodecanoate) is an ester product.
3,3'-Diiodo-L-thyronine- 13C6 is the 13C labeled 3,3'-Diiodo-L-thyronine . 3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity .
Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled Gemcitabine hydrochloride . Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
Zidovudine O-β-D-glucuronide-d3 (sodium) (3'-Azido-3'-deoxythymidine β-D-glucuronide-d3 (sodium)) is a deuterium labeled Zidovudine O-β-D-glucuronide (sodium) (HY-137522). Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection .
L-Lactic acid- 13C3 ((S)-2-hydroxypropanoic- 13C3) sodium (20% in water) is the 13C labeled L-Lactic acid. L-Lactic acid- 13C3 sodium (20% in water) can be used for lactate metabolism research .
Captopril- 13C5, 15N (SQ 14225- 13C5, 15N) is 13C and 15N labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
1-(4,4-Dimethylthiochroman-6-yl)ethanone-d8(6-Acetyl-4,4-dimethylthio-chroman-d8) is the deuterium labeled 1-(4,4-Dimethylthiochroman-6-yl)ethanone (HY-I0187).
Laninamivir- 13C, 15N2 (R 125489- 13C, 15N2) is 13C and 15N labeled Laninamivir. Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively .
1-Oleoyl-2-linoleoyl-rac-glycerol-d5 (DG(18:1/0:0/18:2)-d5) is the deuterium labeled 1-Oleoyl-2-linoleoyl-rac-glycerol (HY-W777107). 1-Oleoyl-2-linoleoyl-rac-glycerol (DG(18:1/0:0/18:2)) is a diacylglycerol, which is composed of a linoleic acid and an oleic acid. 1-Oleoyl-2-linoleoyl-rac-glycerol can be found in dry-cured ham, and acts as the food additive .
Lisinopril- 13C5, 15N (MK-521- 13C5, 15N) is 13C and 15N labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
Pomalidomide- 15N, 13C5 is 15N and 13C labeled Pomalidomide (HY-10984). Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Lamivudine- 13C, 15N3 (BCH-189- 13C, 15N3) is 13C and 15N labeled Lamivudine. Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
((2R,3S,4R,5R)-5-(4-Amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate- 13C9, 15N3 (sodium) is the 13C and 15N labeled Sodium ((2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate .
PSI-6206-d1, 13C, 15N2 is 15N and 13C labeled PSI-6206 (HY-15236). PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Nonanoic acid-d2 is the deuterium labeled Nonanoic acid . Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
L-Glutamine-1,2- 13C2 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
(9S,13R)-12-OPDA-d5 ((9S,13R)-12-OPDA-d5) is an isotopic label of (9S,13R)-12-oxyphytodienoic acid. (9S,13R)-12-Oxophytodienoic acid is an isomer of 12-oxoPDA (HY-118828). (9S,13R)-12-Oxo phytodienoic Acid is a lipoxygenase metabolite in green plant leaves .
1-(4-Chlorophenyl)-2-methylpropan-2-ol-d6(1-(4-Chlorophenyl)-2-methyl-2-propanol-d6) is the deuterium labeled 1-(4-Chlorophenyl)-2-methylpropan-2-ol (HY-W101971).
L-Ascorbic acid- 13C6-1 (L-Ascorbate-1; Vitamin C- 13C6-1) is a 13C labeled L-Ascorbic acid (HY-B0166) . L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor [4]. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells .
Zidovudine Glucuronide- 13C6 (3'-Azido-3'-deoxythymidine β-D-glucuronide- 13C6) is 13C labeled Zidovudine O-β-D-glucuronide. Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection .
LacCer (d18:1/16:0)-d3 (C16 Lactosylceramide (d18:1/16:0)-d3) is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
5-Fluorouracil- 13C, 15N2 is the 13C and 15N labeled 5-Fluorouracil . 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer . 5-Fluorouracil also inhibits HIV [4].
2-Amino-2-deoxyglucose hydrochloride- 13C2 (D-Glucosamine Hydrochloride-1,2- 13C2) is the 13C-labeled 2-Amino-2-deoxyglucose hydrochloride (HY-N9459). 2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc .
N-Phthaloylglycine- 13C2, 15N (Phthaloyl glycine- 13C2, 15N) is the 13C- and 15N-labeled N-Phthaloylglycine (HY-W014665). N-Phthaloylglycine (Phthaloyl glycine) is an FX-type hapten that attaches to free amine groups of proteins .
1-(Adamantan-1-yl)ethan-1-one-d3 (N-Benzyl-3-carboethoxy-4-piperidone hydrochloride-d3) is the deuterium labeled 1-(Adamantan-1-yl)ethan-1-one (HY-W067624).
Diacetone-β-D-fructose-d12(2,3:4,5-Di-O-isopropylidene-β-D-fructopyranose-d12) is the deuterium labeled Diacetone-β-D-fructose (HY-W011792). Diacetone-β-D-fructose is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Homovanillic acid- 13C6, 18O (Vanilacetic acid- 13C6, 18O) is the 13C- and 18O-labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
L-Valine- 13C5, 15N ((S)-Valine- 13C5, 15) is the 13C- and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
(S)-2-Hydroxy-3-phenylpropanoic acid- 13C9 (L-(-)-3-Phenyllactic Acid- 13C9) is the 13C-labeled (S)-2-Hydroxy-3-phenylpropanoic acid (HY-30220). (S)-2-Hydroxy-3-phenylpropanoic acid is the L-configuration of 2-Hydroxy-3-phenylpropanoic acid, and its level is closely related to some diseases, such as phenylketonuria .
Octreotide- 13C9, 15N (SMS 201-995- 13C9, 15N) is 13C and 15N labeled Octreotide. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
Taurine- 13C2, 15N is the 13C- and 15N- labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
Dihydrouracil- 13C, 15N2 (5,6-Dihydrouracil- 13C, 15N2) is the 13C- and 15N-labeled Dihydrouracil (HY-W012926). Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient .
2-(4-Bromophenoxy)-N,N-dimethylethanamine-d6 (2-(N,N-Dimethylamino)ethyl 4-bromophenyl ether-d6) is the deuterium labeled 2-(4-Bromophenoxy)-N,N-dimethylethanamine (HY-W013927).
Oxypurinol- 13C, 15N2-1 (Oxipurinol- 13C, 15N2-1) is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol, the major active metabolite of Allopurinoll (HY-B0219), is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
Betrixaban-d4(PRT054021-d4) is deuterium labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
Floxuridine- 13C, 15N2 (5-Fluorouracil 2'-deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled Floxuridine (HY-B0097). Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
Benzyl alcohol-α- 13C-α,α-d2 is the 13C-labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
N-Cyclohexyl-1,3-benzothiazol-2-amine- 13C6 (N-Cyclohexylbenzothiazole-2-amine- 13C6) is the 13C-labeled N-Cyclohexyl-1,3-benzothiazol-2-amine (HY-W200757).
1-Methyl-5-(3-pyridinyl)-2-pyrrolidinone- 13C,d3 (rac-Cotinine- 13C,d3) is the deuterium and 13C-labeled 1-Methyl-5-(3-pyridinyl)-2-pyrrolidinone (HY-W588192).
6-Amino-3-methylpyrimidine-2,4(1H,3H)-dione-d3 (6-Amino-3-methyluracil-d3) is the deuterium labeled 6-Amino-3-methylpyrimidine-2,4(1H,3H)-dione (HY-W038777).
H-N-Me-Ala-OH- 13C,d3 (N-Methyl-L-alanine- 13C,d3) is the deuterium and 13C labeled H-N-Me-Ala-OH (HY-W015926). H-N-Me-Ala-OH is an alanine derivative .
5,6-Diaminopyrimidine-2,4-diol hydrochloride- 13C3 (5,6-Diaminouracil hydrochloride- 13C3) is the 13C-labeled5,6-Diaminopyrimidine-2,4-diol (HY-W002107).
Fmoc-Gly-OH- 13C2, 15N (Fmoc glycine- 13C2, 15N) is a 15N-labeled and 13C-labled Fmoc-Gly-OH (HY-Y1250). Fmoc-Gly-OH (Fmoc glycine) is a Fmoc-protected glycine derivative, can be used for the synthesis of compounds .
Diethyl itaconate,98% (stabilized with TBC)- 13C5 (Itaconic Acid Diethyl Ester (stabilized with TBC)- 13C5) is the 13C-labeled Diethyl itaconate,98% (stabilized with TBC) (HY-W143131).
N-Ethyl-3,4-(methylenedioxy)aniline-d5 (N-Ethyl-3H-1,2-benzodioxol-6-amine-d5) is the deuterium labeled N-Ethylbenzo[d][1,3]dioxol-5-amine (HY-W015360).
2-Bromo-3'-methoxyacetophenone- 13C,d3 (α-Bromo-3'-methoxyacetophenone- 13C,d3) is the deuterium and 13C labeled 2-Bromo-3'-methoxyacetophenone (HY-W004800).
(R)-4-Benzyl-3-propionyloxazolidin-2-one-d3(N-3-propionyl-(4R)-benzyl-2-oxazolidinone-d3) is the deuterium labeled (R)-4-Benzyl-3-propionyloxazolidin-2-one (HY-W008773).
Meldrum's acid- 13C3 (2,2-Dimethyl-1,3-dioxane-4,6-dione- 13C3) is the 13C-labeled Meldrum's acid (HY-Y0232). Meldrum's acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Regorafenib N-oxide and N-desmethyl (M5)-d3-1 (N-Desmethyl regorafenib N-oxide-d3-1) is the deuterium labeled Regorafenib N-oxide and N-desmethyl (M5) (HY-108226). Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4 .
5-Bromo-2,4-di-tert-butoxypyrimidine- 13C, 15N2 (IFLAB-BB F1371-0151- 13C, 15N2) is the 13C- and 15N-labeled 5-Bromo-2,4-di-tert-butoxypyrimidine (HY-W128969).
5-Methyl cytosine- 13C, 15N2 hydrochloride (5-Methylcytosine hydrochloride- 13C, 15N2) is the 13C- and 15N-labeled 5-Methylcytosine hydrochloride (HY-W008091A). 5-Methylcytosine hydrochloride plays a crucial role in regulating gene expression, facilitating genomic imprinting, and suppressing transposable elements, while also being intricately linked to translational fidelity and tRNA recognition.
L-Alanine- 13C2, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Acetobromo-a-D-glucuronic acid- 13C6 methyl ester (Methyl acetobromo-α-D-glucuronate- 13C6 methyl ester) is 13C labeled Acetobromo-α-D-glucuronic acid methyl ester, 98% (HY-W008125). Acetobromo-α-D-glucuronic acid methyl ester, 98% is an intermediate. Acetobromo-α-D-glucuronic acid methyl ester, 98% can be used to synthesize HMR1098-S-Glucuronide Methyl Ester. HMR1098 is a novel KATP blocker that is metabolized to S-glucuronide in rat and dog bile. Acetobromo-α-D-glucuronic acid methyl ester, 98% can be used in the research of sudden cardiac death .
3-Hydroxykynurenine- 13C3, 15N (3-Hydroxy-DL-kynurenine- 13C3, 15N) is the 13C and 15N labeled 3-Hydroxykynurenine (HY-113294) . 3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis .
(S)-4-Benzyl-3-propionyloxazolidin-2-one-d3 (2-Oxazolidinone, 3-(1-oxopropyl)-4-(phenylmethyl)-, (4S)-d3) is the deuterium labeled (S)-4-Benzyl-3-propionyloxazolidin-2-one (HY-W008304).
L-Alanine- 13C3, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N-Acetyl-D-glucosamine- 13C6 (N-Acetyl-2-amino-2-deoxy-D-glucose- 13C6) is the 13C labled N-Acetyl-D-glucosamine (HY-A0132) . N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of glucose.
Quinolinic acid- 13C3, 15N (2,3-Pyridinedicarboxylic Acid- 13C3, 15N) is the 13C- and 15N-labeled Quinolinic acid (HY-100807). Quinolinic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway and thereby has the potential of mediating N-methyl-D-aspartate neuronal damage and dysfunction .
3,4-Dihydronaphthalen-1-one- 13C6 (3,4-Dihydro-1(2H)-naphthalenon- 13C6) is the 13C-labeled 3,4-Dihydronaphthalen-1(2H)-one (HY-76194). 3,4-Dihydronaphthalen-1(2H)-one is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
D-Glutamic acid- 13C5, 15N ((R)-Glutamic acid- 13C5, 15N) is 13C and 15N labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
N2,9-Diacetylguanine- 13C2, 15N (N-(9-Acetyl-6,9-dihydro-6-oxo-1H-purin-2-yl)acetamide- 13C2, 15N) is the 13C- and 15N-labeled N2,N9-Diacetylguanine (HY-41619).
N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine-d3 (Methyl N-acetyl-S-(3-hydroxypropyl)-L-cysteinate-d3) is the deuterium labeled N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine.
D-Mannosamine-d2(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal-d2) hydrochloride is a deuterium labeled D-Mannosamine hydrochloride (HY-W021425). D-Mannosamine ((2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal) hydrochloride is a six-carbon amino sugar and an amino derivative of D-mannose. D-Mannosamine hydrochloride can block mannose receptors.
Dinoprost- 13C5 is 13C labeled Dinoprost (HY-12956). Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
Exendin-4 (Leu- 13C6, 15N) (Exenatide (Leu- 13C6, 15N)) TFA is the 13C- and 15N-labeled Exendin-4 TFA (HY-13443). Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM .
γ-Glu-(Phe- 13C9, 15N) is the 13C and 15N labeled isotope of γ-Glu-Phe(HY-101399).γ-Glu-Phe or the postenzymatic reaction mixture enhanced the umami intensity of commercial soy sauce and model chicken soup.
Cyclic GMP- 13C, 15N2 is 13C and 15N labeled Cyclic GMP (HY-113469). Cyclic GMP (cGMP), an important second messenger, is a major intracellular mediator of extracellular signals such as nitric oxide (NO) and natriuretic peptides (NPs). Effects of Cyclic GMP occur through three main groups of cellular targets: cGMP-dependent protein kinases (PKGs), cGMP-gated cation channels, and PDEs. Cyclic GMP can inhibit both platelet adhesion and aggregation. cGAMP (Cyclic-GMP-AMP) (HY-12512), a conjugate of Cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses [4].
L-Phenylalanine- 13C9, 15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
2-Chloropropane-1,3-diyl dioleate-d5 (1,1′-(2-Chloro-1,3-propanediyl) di-(9Z)-9-octadecenoate-d5) is the deuterium labeled 2-Chloropropane-1,3-diyl dioleate (HY-W705777). 2-Chloropropane-1,3-diyl dioleate (1,1′-(2-Chloro-1,3-propanediyl) di-(9Z)-9-octadecenoate) is an ester product.
1-(3,4-Dimethylphenyl)ethan-1-ol- 13C,d3 (1-(3,4-Dimethylphenyl)ethanol- 13C,d3) is the deuterium labeled and 13C-labeled 1-(3,4-Dimethylphenyl)ethan-1-ol (HY-W340128).
4-Amino-TEMPO-d17,15N (4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl-d17,15N) is the deuterium labeled 4-Amino-TEMPO-d17 (HY-W002004S1). 4-Amino-TEMPO (4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl) is a stable nitroxide radical and N-nucleophile based on TEMPO. 4-Amino-TEMPO has superoxide dismutase-mimetic activity, can protect cells from oxidative damage, and has radioprotective effects. 4-Amino-TEMPO is widely used in fields such as biomedicine, materials science, and industrial production. 4-Amino-TEMPO can be used as a spin label to detect free radicals, an oxidation catalyst in industrial production, and an antioxidant stabilizer for polymers, among others .
5'-Hydroxyphenyl carvedilol-d5(3-(2-((3-((9H-carbazol-4-yl)oxy)-2-hydroxypropyl)amino)ethoxy)-4-methoxyphenol-d5) is the deuterium labeled 3-(2-((3-((9H-carbazol-4-yl)oxy)-2-hydroxypropyl)amino)ethoxy)-4-methoxyphenol (HY-W334664).
8-Hydroxy-2'-deoxyguanosine- 13C, 15N2 is 13C and 15N labeled 8-Hydroxy-2'-deoxyguanosine. 8-Hydroxy-2'-deoxyguanosine is a critical biomarker of oxidative stress and carcinogenesis .
Ile-(Leu-13C6,15N)-OH (TFA) is 13C- and 15N-labeled L-Isoleucyl-L-leucine (HY-W269700). L-Isoleucyl-L-leucine has a role as a metabolite and can be used to inhibit movement-induced muscle damage and muscle defective condition.
(S)-2-Amino-3-(4-nitrophenyl)propan-1-ol-d6((2S)-2-Amino-3-(4-nitrophenyl)-1-propanol-d6) is the deuterium labeled (S)-2-amino-3-(4-nitrophenyl)propan-1-ol (HY-W270163).
Diacetone-β-D-fructose- 13C6 (2,3:4,5-Di-O-isopropylidene-β-D-fructopyranose- 13C6) is the 13C-labeled Diacetone-β-D-fructose (HY-W011792). Diacetone-β-D-fructose is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
(Leu-13C6,15N)-Ile-OH (L-Leucyl-13C6,15N-L-isoleucine) TFA is the deuterium labeled Leu-Ile-OH. Leu-Ile-OH protects against neuronal death by inducing brain-derived neurotrophic factor (BDNF) and glial cell line-derived neurotrophic factor (GDNF) synthesis .
1,3-Dipalmitin-d6 (Glyceryl 1,3-dipalmitate-d6) is deuterium labeled 1,3-Dipalmitin. 1,3-Dipalmitin (1,3-Dipalmitoylglycerol) is a cerebroside that can be found in Typhonium giganteum Engl .
(3S,6S)-3,6-Dimethyl-1,4-dioxane-2,5-dione- 13C2 (L-Lactide- 13C2) is the 13C-labeled L-Lactide (HY-W020691A). (3S,6S)-3,6-Dimethyl-1,4-dioxane-2,5-dione is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Uridine diphosphate glucuronic acid- 13C, 15N2 (UDP-α-D-glucuronic acid- 13C, 15N2) is the 13C- and 15N-labeled Uridine diphosphate glucuronic acid (HY-125954). Uridine diphosphate glucuronic acid (UDP-α-D-glucuronic acid) is a cofactor that is formed by the catalytic activity of UDP-glucose dehydrogenase. Uridine diphosphate glucuronic acid is a central precursor in sugar nucleotide biosynthesis and common substrate for C4-epimerases and decarboxylases releasing UDP-galacturonic acid (UDP-GalA) and UDP-pentose products, respectively. Uridine diphosphate glucuronic acid as a glucuronic acid donor, can be used for for the research of the conjugation of bilirubin in the endoplasmic recticulum .
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
3a,4,7,7a-Tetrahydro-1H-isoindole-1,3(2H)-dione-d6 (1,2,3,6-Tetrahydrophthalimide-d6) is the deuterium labeled 3a,4,7,7a-Tetrahydro-1H-isoindole-1,3(2H)-dione (HY-W068988).
3',5'-Di-O-benzyl Entecavir- 13C2, 15N (The intermediate of Entecavir hydrate- 13C2, 15N) is the 13C- and 15N-labeled 2-Amino-9-((1S,3R,4S)-4-(benzyloxy)-3-((benzyloxy)methyl)-2-methylenecyclopentyl)-1H-purin-6(9H)-one (HY-W105415).
2,4-Dichloro-5-methylpyrimidine- 15N2, 13C (Pyrimidine, 2,4-dichloro-5-methyl- 15N2, 13C) is the 13C- and 15N-labeled 2,4-Dichloro-5-methylpyrimidine (HY-W002132).
Eicosapentaenoic acid 1,2,3,4,5- 13C5 (EPA 1,2,3,4,5- 13C, FA 20:5- 13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation [4].
N-Acetyl-D-glucosamine- 13C3, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc .
N-Acetyl-D-glucosamine- 13C8, 15N is 13C and 15N labeled N-Acetyl-D-glucosamine (HY-A0132). N-Acetyl-D-glucosamine is a monosaccharide derivative of glucose.
N-Acetyl-D-glucosamine- 13C2, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc .
2-(5-tert-Butyl-2-hydroxyphenyl)benzotriazole-d9(2-(2H-Benzo[d][1,2,3]triazol-2-yl)-4-(tert-butyl)phenol-d9) is the deuterium labeled 2-(2H-Benzo[d][1,2,3]triazol-2-yl)-4-(tert-butyl)phenol (HY-W440436).
Citrinin- 13C13 (NSC 186- 13C13) is the 13C labeled Citrinin (HY-N6746). Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity [4] .
N2-Acetyl-O6-diphenylcarbamoylguanine- 13C2, 15N (2-Acetamido-9H-purin-6-yl diphenylcarbamate- 13C2, 15N) is the 13C- and 15N-labeled 2-Acetamido-9H-purin-6-yl diphenylcarbamate (HY-W143802).
2,5,6-Triaminopyrimidin-4(3H)-one- 13C2, 15N (6-Hydroxy-2,4,5-triaminopyrimidine- 13C2, 15N) is the 13C- and 15N-labeled 2,5,6-Triaminopyrimidin-4(3H)-one (HY-W018560).
N-Boc-S-Bzl-L-Cys-Gly-OBzl- 13C2, 15N (Benzyl S-benzyl-N-(tert-butoxycarbonyl)-L-cysteinylglycinate- 13C2, 15N) is the 13C- and 15N-labeled Benzyl S-benzyl-N-(tert-butoxycarbonyl)-L-cysteinylglycinate (HY-W699579).
1,2-Dioleoyl-3-lauroyl-rac-glycerol- 13C3 is the 13C-labeled 1,2-Dioleoyl-3-lauroyl-rac-glycerol (HY-165089), 1,2-Dioleoyl-3-lauroyl-rac-glycerol (1,2-Olein-3-laurin) is a triglyceride identified by specific analytical methods in human milk, infant formula, other mammalian milk, and vegetable oils, with specific structural and distribution characteristics.
Tenuazonic acid-(acetyl- 13C2) (mixture of diastereomers) in methanol (3-(Acetyl- 13C2)-5-((S)-sec-butyl)-4-hydroxy-1,5-dihydro-2H-pyrrol-2-one) is 13C labeled Tenuazonic acid-(acetyl) (mixture of diastereomers) in methanol .
((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methanol-d2 ((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizine-7a(5H)-methanol-d2) is the deuterium labeled ((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methanol.
Colfosceril miristate-d9 (DMPC-d9) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d67 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
Colfosceril miristate-d4(DMPC-d4) is deuterium labeled Colfosceril miristate. Colfosceril miristate is a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Stewart-Grubbs catalyst is an effective catalyst for the cross-metathesis of olefins with a large number of allylic substituents. In addition, ChemBeads are chemically coated glass beads that improve flowability and chemical homogeneity, making them ideal for automated solid dispensing and high-throughput experiments. Notably, the manufacture of ChemBeads does not require additional chemicals or surfactants, allowing for precise dispensing of sub-milligram amounts of catalyst.
Colfosceril miristate-d13 (DMPC-d13) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d58 (DMPC-d58) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d63 (DMPC-d63) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
Calcitonin- 13C6, 15N4 (salmon) (Salmon calcitonin- 13C6, 15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction [4].
Ac-{Cpg}-Thr-Ala-{Ala(CO)}-Asp-{Cpg}-NH2 (compound 40) is a potent Plasmodium subtilisin-like protease 1 (SUB1) inhibitor. SUB1-IN-1 shows IC50 values of 12 nM and 10 nM against P. vivax and P. falciparumSUB1 (Pv- and PfSUB1), respectively .
Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
Fibrinopeptide B, human-(Val- 13C5, 15N, Arg- 13C6, 154) TFA is the 13C- and 15N-labeled Fibrinopeptide B, human (HY-P1493). Fibrinopeptide B, human is a 14-aa peptide, released from the amino-terminus of β-chains of fibrinogen by thrombin .
d-KLA Peptide-d30 (D-(KLAKLAK)2-d30) is the deuterium labeled d-KLA Peptide (HY-P10285). d-KLA Peptide is a synthetic pro-apoptotic peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrial membrane. d-KLA Peptide activates biochemical pathways associated with apoptosis, including the activation of caspase family proteins and PARP (poly ADP ribose polymerase). d-KLA Peptide can be used to carry and deliver genes or small molecules to enhance anti-tumor effects .
Exendin-4 (Leu- 13C6, 15N) (Exenatide (Leu- 13C6, 15N)) TFA is the 13C- and 15N-labeled Exendin-4 TFA (HY-13443). Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM .
MCE Phenyl Agarose (Low Sub) 6FF is a low-substitution hydrophobic chromatography medium formed by covalently coupling phenyl ligands to agarose. It is suitable for laboratory-scale and industrial-scale purification of biomolecules with relatively weak hydrophobicity.
MCE Phenyl Agarose (High Sub) 6FF is a high-substitution hydrophobic chromatography medium formed by covalently coupling phenyl ligands to agarose. It is suitable for laboratory-scale and industrial-scale purification of biomolecules with relatively weak hydrophobicity.
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis[4].
Geranylgeraniol is an orally acitve vitamin K2sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [4].
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
Geranylgeraniol (Standard) is the analytical standard of Geranylgeraniol. This product is intended for research and analytical applications. Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [3][4].
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [4].
Pelargonidin chloride is an anthocyanidin and also is a scavenger of nitric oxide radical and has antioxidant activities. Pelargonidin inhibits cell viability and induces cell cycle arrest at sub-G1 phase. Pelargonidin chloride increases the mRNA and protein expression of HO-1, NQO1, Nrf2. Pelargonidin chloride improves Aβ-induced memory and learning impairment .
Alpha-Naphthoflavone (Standard) is the analytical standard of Alpha-Naphthoflavone. This product is intended for research and analytical applications. Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis [4].
Neochilenin (3-O-Methylquercetin 4 '-O-glucoside) is a glycoside of 3-O-methylquercetin, which can be isolated from the sub-family Cereoideae (Cactaceae). .
9-Oxooctadecanedioic acid is an α,ω-dicarboxylic fatty acid monomer found in the cork suberin of Quercus suber. It contributes to the formation of the hydrophobic barrier structure in plant cell walls and may play an important role in functions such as water resistance and protection against microbial penetration .
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitory activity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [4].
Procyanidin A3 (Cinnamtannin A3; Cinnamtannin II) is a sub class of Proanthocyanidins (HY-N0794). Proanthocyanidin are a class of polyphenolic that are widely distributed in higher plants, consisted of an electrophilic flavanyl unit. Proanthocyanidin can be used as antioxidant and anti-cancer agent. Proanthocyanidin also exhibit anti-inflammatory, cardioprotective, antibacterial and antifungal properties, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy .
The PC4/SUB1 protein acts as a multifunctional coactivator that cooperates with TAF to promote functional interactions between upstream activators and the general transcription machinery. Its role extends to the potential stability of multiprotein transcription complexes. PC4/SUB1 Protein, Human (His) is the recombinant human-derived PC4/SUB1 protein, expressed by E. coli , with N-His labeled tag.
ABC 29; ABC29; ABCC 1; ABCC; Abcc1; ATP binding cassette sub family C CFTR/MRP; member 1; ATP binding cassette sub-family C member 1; ATP binding cassette subfamily C member 1; ATP binding cassette transporter variant ABCC1delta ex13; ATP binding cassette transporter variant ABCC1delta ex13&14; ATP binding cassette transporter variant ABCC1delta ex25; ATP binding cassette transporter variant ABCC1delta ex25&26; ATP binding cassette, sub-family C CFTR/MRP; , member 1; ATP-binding cassette sub-family C member 1; DKFZp686N04233; DKFZp781G125; GS X; GSX; Leukotriene C4; transporter; LTC4 transporter; MRP 1; MRP; MRP1; MRP1_HUMAN; Multidrug resistance associated protein 1; Multidrug resistance protein; Multidrug resistance-associated protein 1; Multiple drug resistance associated protein; Multiple drug resistance protein 1
ABCC1, Human (His) is a multitasking ATP-binding cassette (ABC) transporter. ABCC1, Human plays a part in inflammatory and other immunological diseases, age-related macular degeneration, cardiovascular disease, and certain neurological disorders as well as tumor progression.
ABCB5, N-Trx Protein, Human is a plasma membrane-spanning protein that in humans is encoded by the ABCB5 gene. ABCB5 is an ABC transporter and P-glycoprotein family member principally expressed in physiological skin and human malignant melanoma.
The ABCC1 protein plays a key role in cellular physiology, mediating the ATP-dependent export of a variety of substrates, including drugs and organic anions. Notably, it confers resistance to anticancer drugs, actively reducing their intracellular accumulation. ABCC1 Protein, Bovine (HEK293, GFP, Strep, His) is the recombinant bovine-derived ABCC1 protein, expressed by HEK293 , with C-10*His, C-GFP, C-StrepII labeled tag.
Acetaminophen-d4 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
4-Aminobenzoic acid-d4 is the deuterium labeled 4-Aminobenzoic acid. 4-Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi.
N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine . N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection [4] .
Demethoxycurcumin-d4 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin (Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties .
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Zidovudine-d4 is deuterated labeled Zidovudine (HY-17413). Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
D-Glucose-d4 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Isoniazid-d4 is the deuterium labeled Isoniazid. Isoniazid (INH) is a proagent and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity [4].
Tiagabine-d4(NO050328-d4) is deuterium labeled Tiagabine. Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively .
Sulfameter-d4(Sulfametoxydiazine-d4) is the deuterium labeled Sulfameter (HY-B0213) . Sulfameter (Sulfametoxydiazine) is an orally active long-acting sulfonamide antibiotic. Sulfameter is active against both Gram-positive and Gram-negative bacteria. Sulfameter can be used for the research of diseases such as respiratory and urinary tract infections .
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Enclomiphene-d4((E)-Clomiphene-d4) hydrochloride?is a deuterium labeled Enclomiphene hydrochloride (HY-118861B). Enclomiphen hydrochloride?is a potent and orally active?estrogen receptor?antagonist with antioestrogenic property .
Enclomiphene-d4((E)-Clomiphene-d4) is a deuterium labeled Enclomiphene. Enclomiphen?is a potent and orally active?estrogen receptor?antagonist with antioestrogenic property .
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Phosphorylethanolamine-d4 (Monoaminoethyl phosphate-d4; NSC 254167-d4) is a deuterium labeled Phosphorylethanolamine (HY-N5034). Phosphorylethanolamine is an endogenous metabolite.
Telbivudine-d4 is deuterium labeled Telbivudine. Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication .
Binimetinib-d4(MEK162-d4) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
Cyclosporin A-d4 is the deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 ad
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Deracoxib-d4 (SC 046-d4; SC 59046--d4) is deuterium labeled Deracoxib (HY-17509). Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas.
Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
Erlotinib-d4(CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Valproic acid-d4 (sodium) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Vatalanib-d4(PTK787-d4;ZK-222584-d4;CGP-79787-d4) is the deuterium labeled Vatalanib (HY-10203). Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
Dihydromyricetin-d4(Ampelopsin-d4) is deuterium labeled Dihydromyricetin. Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination . Acyclovir prevents bacterial infections during induction therapy for acute leukaemia [4].
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
Bronopol-d4 is deuterium labeled Bronopol. Bronopol is an antibacterial agent with low toxicity (to mammals) and high activity (especially against Gram-negative bacteria). Bronopol oxidizes protein thiols, inhibits enzymatic activity, and exhibits antibacterial activity. Bronopol is also a formaldehyde releaser .
Sulfamethazine-d4(Sulfadimidine-d4) is a deuterium labeled Sulfamethazine (Sulfadimidine). Sulfamethazine is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections) .
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells .
Butylparaben-d4 is the deuterium labeled Butylparaben. Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
2-Phenylethanol-d4 is the deuterium labeled 2-Phenylethanol . 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans . It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Cladribine-d4(2-Chloro-2′-deoxyadenosine-d4) is deuterium labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis .
Hydroxytyrosol-d4 (DOPET-d4) is the deuterium labeled Hydroxytyrosol (HY-N0570). Hydroxytyrosol is a phenol found in the olive oil. Hydroxytyrosol can alleviate oxidative stress and improve mitochondrial function, thereby exerting neuroprotective effects. Hydroxytyrosol can induce cancer cells apoptosis via inducing ROS production. Hydroxytyrosol shows antibacterial and antiviral effect. Hydroxytyrosol can be used for the researches of cancer, infection, inflammation, immunology, metabolic, neurological and cardiovascular disease, such as colon cancer, diabetes, Alzheimer's Disease and atherosclerosis [4] .
D-Alanine-d4 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
(-)-(S)-Cibenzoline-d4(Escibenzoline-d4) is deuterium labeled (-)-(S)-Cibenzoline. (-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent .
Fosribnicotinamide-d4 (β-Nicotinamide mononucleotide-d4) is the deuterium labeled Fosribnicotinamide. Fosribnicotinamide is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD+ intermediate. The pharmacological activities of Fosribnicotinamide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity .
Thymidine-d4 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication .
Miltefosine-d4(HePC-d4) is deuterium labeled Miltefosine. Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity [4]. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT) .
Levamlodipine-d4 is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina .
Dropropizine-d4((±)-Dropropizine-d4) is deuterium labeled Dropropizine. Dropropizine ((±)-Dropropizine) belongs to the phenylpiperazine group of organic compounds. Dropropizine is a peripheral antitussive agent that acts by inhibiting cough reflex through its action on the peripheral receptors and their afferent conductors .
Carbamazepine-d4(CBZ-d4) is the deuterium labeled Carbamazepine (HY-B0246) . Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na +, Ca 2+, and K + channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.
Difethialone-d4(Baraki-d4; LM 2219-d4) is the deuterium labeled Difethialone (HY-113958). Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Adefovir-d4 is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses .
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Leriglitazone-d4(MIN-102-d4;Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
Rifampicin-d4 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Rebamipide-d4 is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner .
Exemestane-d4 (FCE 24304-d4) is deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Salbutamol-d4(Albuterol-d4;AH-3365-d4) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is a short-acting beta-2 adrenergic receptor agonist with oral activity. Salbutamol promotes tumorigenesis of gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol is used to study bronchospasms caused by asthma and chronic obstructive pulmonary disease (COPD) .
Sulfabrom-d4 (N 3517-d4) is is the deuterium labeled Sulfabrom (HY-U00131). Sulfabrom is a long-acting Sulfonamide that is used for the treatment of coccidiosis and various bacterial infections in the poultry, swine and cattle .
Aspirin-d4 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis [4] .
Estrone-d4 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Nicotinamide-d4 is the deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
4-Methylumbelliferone- 13C4 (Hymecromone- 13C4) is the 13C-labeled 4-Methylumbelliferone (HY-N0187). 4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects.
Corticosterone-d4 is the deuterium labeled Corticosterone. Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
Estradiol-d4 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
D-Glucose-d-44 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Etoricoxib-d4(MK-0663-d4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Vitamin K1-d4 is the deuterium labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism .
Fosamprenavir-d4 is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .
Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Lapatinib-d4(GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
D-Sorbitol-d4 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
Baloxavir-d4 (Baloxavir acid-d4;S-033447-d4) is the deuterium-labeled Baloxavir (HY-109025A). Baloxavir-d4(Baloxavir-d4 acid), derived from the proagent Baloxavir-d4 marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir-d4 inhibits viral RNA transcription and replication and has potently antiviral activity .
Serotonin-d4(5-Hydroxytryptamine-d4) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473) . Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Cibenzoline-d4(Cifenline-d4) is deuterium labeled Cibenzoline. Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a KATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC50 of 22.2 μM. Cibenzoline inhibits IKr and IKs currents with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia [4].
Procainamide-d4 hydrochloride is deuterated labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Entinostat-d4 is the deuterium labeled Entinostat . Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively .
Lornoxicam-d4 is the deuterium labeled Lornoxicam. Lornoxicam (Chlortenoxicam), a COX-1 and COX-2 inhibitor, is a new nonsteroidal anti-inflammatory agent (NSAID).
Penciclovir-d4 is the deuterium labeled Penciclovir. Penciclovir is reported to be potent against HSV types 1 and 2 with IC50 of 0.04-1.8 μg/mL and 0.06-4.4 μg/mL, respectively .
Lifitegrast-d4 (SAR 1118-d4) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Cysteamine-d4 (hydrochloride) is the deuterium labeled Cysteamine hydrochloride. Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
Isavuconazole-d4(BAL-4815-d4) is a deuterium labeled Isavuconazole (BAL-4815). Isavuconazole is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi .
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
Pantoprazole-d4(BY1023-d4) is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Lomitapide-d4(AEGR-733-d4) is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Palmitoylethanolamide-d4 is the deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.
Talazoparib-d4(BMN-673-d4) is deuterium labeled Talazoparib. Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity .
N4-Acetylsulfamerazine-d4(Acetylsulfamerazine-d4;Sulfamelazine-d4) is the deuterium labeled N4-Acetylsulfamerazine (HY-W031230). N4-Acetylsulfamerazine is a sulfonamides derivative .
Glimepiride-d4-1 is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
Darolutamide-d4(ODM-201-d4) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay .
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Caspofungin-d4 (acetate) is the deuterium labeled Caspofungin diacetate . Caspofungin (MK-0991) diacetate is a potent antifungal agent. Caspofungin diacetate inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan .
Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
(-)-Epigallocatechin Gallate-d4(EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma [4].
Dapivirine-d4(TMC120-d4) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities .
Revefenacin-d4(TD-4208-d4) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Secnidazole-d4 is the deuterium labeled Secnidazole . Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Serotonin-d4 is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
Caspofungin-d4(MK-0991-d4;L-743872-d4) is a deuterium labeled Caspofungin (HY-17006A). Caspofungin is a potent antifungal agent. Caspofungin inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan .
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
Irbesartan-d4(SR-47436-d4) is the deuterium labeled Irbesartan Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
Volinanserin-d4 (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity .
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
3-Nitrobenzoic acid-d4(m-Carboxynitrobenzene-d4; m-Nitrobenzenecarboxylic acid-d4; m-Nitrobenzoic acid-d4) is the deuterium labeled 3-Nitrobenzoic acid (HY-Y1313). 3-Nitrobenzoic acid is an antioxidant and antibacterial agent that can kill bacteria and fungi. 3-Nitrobenzoic acid can be degraded or reduced by certain bacteria (such as Pseudomonas) and fungi (such as white rot fungi) into aldehydes and alcohols.
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
Carvedilol metabolite 4-Hydroxyphenyl Carvedilol-d4 is deuterated labeled Carvedilol metabolite 4-Hydroxyphenyl Carvedilol (HY-12767). 4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol.
Acetaminophen-d7 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
Acetaminophen-d3 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
Acetaminophen-d5 is deuterated-labeled Acetaminophen (HY-66005). Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
NAD+-d4 is the deuterium-labeled NAD+ (HY-B0445). NAD+-d4 is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
Pimelic acid-d4 is the deuterium labeled Pimelic acid . Pimelic acid is the organic compound and its derivatives are involved in the biosynthesis of the amino acid called lysine.
Imatinib-d4(STI571-d4) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM) .
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .
Thiamine-d4 (hydrochloride) is deuterium labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
Pioglitazone-d4 hydrochloride (U 72107A-d4; AD 4833-d4) is the deuterium labeled Pioglitazone hydrochloride (HY-14601). Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
Valproic acid-d4 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
Etoposide-d4(VP-16-d4;VP-16-213-d4) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Clopidogrel carboxylic acid-d4 is a deuterated derivative of Clopidogrel carboxylic acid, which is an inactive metabolite of the antiplatelet agent Clopidogrel (HY-15283) in plasma. Clopidogrel carboxylic acid-d4 can be used to further explore the metabolic characteristics of Clopidogrel .
Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Octisalate-d4 (Octyl salicylate-d4; 2-Ethylhexyl salicylate-d4) is the deuterium labeled Octisalate (HY-B0929). Octisalate (Octyl salicylate) is an organic compound with high lipophilicity, which is used in sunscreens and cosmetics that absorbs UVB rays .
Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder .
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
Propylparaben-d4 is the deuterium labeled Propylparaben . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats [4].
4-Methylanisole-d4 is the deuterium labeled 4-Methylanisole . 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil .
4-Vinylphenol-d4 is deuterated labeled 4-Vinylphenol (HY-W005288). 4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
(-)-Epigallocatechin Gallate-d3/d4(EGCG-d3/d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma [4].
Higenamine-d4-1(Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [4] .
L-5-Hydroxytryptophan-d4(L-5-HTP-d4;Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [4] .
Retinyl acetate-d4 is the deuterium labeled Retinyl acetate . Retinyl acetate is a synthetic acetate ester form derived from retinol and has potential antineoplastic and chemo preventive activities .
Ticagrelor-d4(AZD6140-d4) is deuterium labeled Ticagrelor. Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.
Losartan-d4 carboxylic acid (E-3174-d4) is the deuterium labeled Losartan Carboxylic Acid (HY-12765). Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
Loratadine-d4-1(Loratidine-d4-1) is deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators .
Folic acid-d4 is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
Glimepiride-d4-2(GliAmperide-d4-2) is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
4-(Trifluoromethyl)aniline-d4(4-Aminobenzotrifluoride-d4) is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively .
L-Asparagine- 13C4 monohydrate is the 13C-labeled L-Asparagine monohydrate (HY-W017443). L-Asparagine monohydrate is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine monohydrate can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia [4] .
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Dinoprost-d4 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
N-(3-Indolylacetyl)-L-alanine-d4(Indoleacetylalanine-d4) is the deuterium labeled N-(3-Indolylacetyl)-L-alanine (HY-W141858). N-(3-Indolylacetyl)-L-alanine is an indoleacetylamino acid. N-(3-Indolylacetyl)-L-alanine appears to increase callus growth and reduces the ability of growths to differentiate into shoots of Phalaenopsis orchids .
p-Anisic acid-d4 is the deuterium labeled p-Anisic acid . p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties .
Folitixorin-d4(5,10-Methylenetetrafolate-d4; ANX-510 (free acid)-d4) is the deuterium labeled Folitixorin (HY-14769). Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research .
β-Alanine-d4 is the deuterium labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
Olaparib-d4-1(AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [4].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ～30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression .
Toxoflavin- 13C4 is the 13C-labeled Toxoflavin. Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity . Antibiotic properties.
5-Azacytidine- 15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy[4].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
Cyclosporin A- 13C2,d4 (Cyclosporine A- 13C2,d4; Ciclosporin A- 13C2,d4) is a 13C labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
Nitroxoline-d4 is the deuterium labeled Nitroxoline. Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe 2+ and Zn 2+ ions from the biofilm matrix .
Valproic acid-d4-1 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
3-Indoleacetic acid-d4 (Indole-3-acetic acid-d4;3-IAA-d4) is the deuterium labeled 3-Indoleacetic acid (HY-18569) . 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Lipoic acid-d4 ((R)-(+)-α-Lipoic acid-d4) is deuterium labeled Lipoic acid. Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid .
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD) .
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
Acotiamide-d4 (Z-338 (free base)-d4) is deuterium labeled Acotiamide. Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
4-Aminohippuric acid-d4 (p-Aminohippuric acid-d4) is the deuterium labeled 4-Aminohippuric acid (HY-B1306). 4-Aminohippuric acid (p-Aminohippuric acid) is a coordination ligand for metal ions (such as Cu 2+, Fe 3+, Hg 2+) and a functionalization reagent for nanomaterials. 4-Aminohippuric acid can coordinate with metal ions or modify the surface of materials such as carbon nanotubes and gold nanoparticles through amino and carboxyl groups. 4-Aminohippuric acid can form stable complexes with metal ions or participate in the synthesis of nanomaterials as a reducing agent/stabilizer, enriching metal ions or giving nanoparticles peroxidase-mimicking activity. 4-Aminohippuric acid can be used to construct highly sensitive electrochemical sensors or colorimetric sensors to detect and quantitatively analyze heavy metal ions such as copper, iron, and mercury in environmental water samples and biological samples. 4-Aminohippuric acid may also be a biomarker for attention-deficit/hyperactivity disorder (ADHD) [4].
4-Oxofenretinide-d4(4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
Sutezolid- 13C4 (PNU-100480- 13C4) is 13C labeled Sutezolid. Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis .
Ezetimibe phenoxy glucuronide-d4 is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity . Ezetimibe is a potent cholesterol absorption inhibitor .
Mono-(2-ethylhexyl) phthalate-d4 is a deuterium labeled Mono-(2-ethylhexyl) phthalate (HY-W018392). Mono-(2-ethylhexyl) phthalate (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP). Mono-(2-ethylhexyl) phthalate can promote fatty acid synthesis in hepatocytes by regulating the expression of relevant genes and proteins, contributing to non-alcoholic fatty liver disease (NAFLD) .
Leukotriene B4-d4 is the deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs .
Colfosceril miristate-d4(DMPC-d4) is deuterium labeled Colfosceril miristate. Colfosceril miristate is a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Tamsulosin-d4 ((R)-(-)-YM12617 (free base)-d4) is deuterium labeled Tamsulosin. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
Drospirenone-d4 is the deuterium labeled Drospirenone. Drospirenone (Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone .
Sulfatroxazole-d4(Isosulfafurazole-d4) is the deuterium labeled Sulfatroxazole (HY-105829) . Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50 of 0.26 μM) .
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Sulfacetamide-d4(Sulphacetamide-d4) is the deuterium labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
Ethambutol-d4 dihydrochloride is deuterated labeled Ethambutol dihydrochloride (HY-B0535A). Ethambutol dihydrochloride is an antimycobacterial compound that prevents cell wall formation by inhibiting arabinosyltransferase activity.
Sulfadimethoxine-d4 is a deuterium labeled Sulfadimethoxine (Sulphadimethoxine). Sulfadimethoxine is a sulfonamide antibiotic used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections .
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
Salcaprozate-d4 (sodium) is a deuterated labeled Salcaprozate (sodium) . Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation .
Tetrahydrozoline-d4 (hydrochloride) is the deuterium labeled Tetrahydrozoline hydrochloride. Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion .
Chlorpheniramine-d4(Chlorphenamine-d4) is deuterium labeled Chlorpheniramine. Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research .
Indomethacin-d4(Indometacin-d4) is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells . Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes .
Dicyclomine-d4 is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Sulfachloropyridazine-d4 is the deuterium labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria .
Sulfisomidin-d4(Sulfaisodimidine-d4) is deuterium labeled Sulfisomidin. Sulfisomidin (Sulfaisodimidine) is an orally active short-acting sulfonamide antibacterial. Sulfisomidin can be used for the research of lower urinary tract infections .
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
Nefopam-d4 (hydrochloride) is deuterium labeled Nefopam (hydrochloride). Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo .
Histamine-d4(Ergamine-d4) is deuterium labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
Ethambutol-d4 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Dibenzylamine-d4(Bisbenzylamine-d4) is the deuterium labeled Dibenzylamine (HY-Y1067). Dibenzylamine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Hydrocortisone-d4 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Sulfadoxine-d4 is the deuterium labeled Sulfadoxine. Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
(±)-Lisofylline-d4((±)-Lisophylline-d4) is deuterium labeled (±)-Lisofylline. (±)-Lisofylline ((±)-Lisophylline) is the racemate of Lisofylline. Lisofylline inhibits the generation of phosphatidic acid and free fatty acids. Lisofylline also blocks the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline can be used for Type 1 diabetes research .
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
Desmethylcitalopram-d4 hydrochloride is deuterated labeled Desmethylcitalopram hydrochloride (HY-113739). Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6, -2C19 with IC50s of 39.5 and 53.5 μM .
Dicyclomine-d4 hydrochloride (Dicycloverine-d4 hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
Cabozantinib-d4 (S-malate) (XL184-d4 (S-malate); BMS-907351-d4 (S-malate)) is the deuterium labeled Cabozantinib (S-malate) (HY-12044). Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
D-Glucose- 13C2-4 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Everolimus- 13C2,d4 (RAD001- 13C2,d4) is 13C labeled Everolimus. Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities .
Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties [4] .
Sacubitrilat- 13C4 (Desethyl Sacubitril- 13C4) is 13C labeled Sacubitrilat. Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
Hypoxanthine- 15N4 is the 15N labeled Hypoxanthine . Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia .
Pyridoxine- 13C4 (hydrochloride) is the 13C-labeled Pyridoxine (hydrochloride). Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
4'-Fluoroacetophenone-d4(1-(4-Fluorophenyl)ethan-1-one-d4) is deuterium labeled 4'-Fluoroacetophenone. 4'-Fluoroacetophenone (1-(4-Fluorophenyl)ethan-1-one) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Lenalidomide-d4(CC-5013-d4) is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Lesinurad-d4(RDEA594-d4) is deuterium labeled Lesinurad. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 μM, respectively.
Ketoprofen-d4 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively .
Homosalate-d4 is the deuterium labeled Homosalate. Homosalate is an organic compound used in some sunscreens, it is used as a chemical UV filter, protecting the skin from sun damage.
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
Evocalcet-d4(KHK7580-d4) is deuterium labeled Evocalcet. Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism .
Carboplatin-d4 is the deuterium labeled Carboplatin. Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
Oxcarbazepine-d4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Anti-cancer and anticonvulsant effects .
Diisopropyl phthalate-d4(DiPP-d4) is the deuterium labeled Diisopropyl Phthalate (HY-W011926). Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM .
Ertapenem-d4(MK-0826-d4) is deuterium labeled Ertapenem. Ertapenem (MK-0826) is a broad spectrum and long acting β-lactam antibiotic. Ertapenem has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract .
Etodolac-d4(AY-24236-d4) is deuterium labeled Etodolac. Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM)
Terconazole-d4 is the deuterium labeled Terconazole. Terconazole is a broad-spectrum antifungal medication for the treatment of vaginal yeast infection.
4-Hydroxytolbutamide-d9 is the deuterium labeled 4-Hydroxytolbutamide. 4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic .
Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Darifenacin-d4 is the deuterium labeled Darifenacin . Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) .
Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant .
Granisetron-d4 (BRL 43694-d4) is deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
Equilin-d4 is the deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism .
Ropinirole-d4 (SKF 101468-d4) hydrochloride is the deuterium labeled Ropinirole hydrochloride. Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Kiof 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Sulfabenzamide-d4 is the deuterium labeled Sulfabenzamide (HY-B0960). Sulfabenzamide (N-Sulfanilylbenzamide) is an antimicrobial agent and usually consumed in combination with Sulfathiazole and Sulfacetamide. Sulfabenzamide is effective against Gram-positive and negative bacterial strains .
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
Azaperone-d4 is the deuterium labeled Azaperone. Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic agent with antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM .
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Acalabrutinib-d4(ACP-196-d4) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
Posaconazole-d4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity .
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Risedronic acid-d4(Risedronate-d4) is the deuterium labeled Risedronic acid (HY-B0148). Risedronic acid (Risedronate) is a bisphosphonate and potent antiresorptive agent. Risedronic acid induces Apoptosis. Risedronic acid inhibits the transfer of farnesyl pyrophosphate groups to parasite proteins. Risedronic acid inhibits osteoclast-mediated bone resorption and alters bone metabolism. Risedronic acid inhibits blood-stage Plasmodium falciparum (IC50 of 20.3 μM) [4].
Azilsartan-d4 is the deuterium labeled Azilsartan . Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research [4] .
Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Paroxetine-d4(BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches [4] .
Lansoprazole-d4(AG-1749-d4) is a deuterium labeled Lansoprazole. Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid .
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities [4].
Mirogabalin-d4(DS5565-d4) is a deuterated compound of Mirogabalin (HY-12650), a ligand that selectively targets the voltage-sensitive calcium channel complex α2δ-1 .
Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
Mequinol-d4 is the deuterium labeled Mequinol[1]. Mequinol (4-Methoxyphenol) is one of bioactive components in Mercurialis. Mequinol is used for skin depigmentation[2].
Efinaconazole-d4 is the deuterium labeled Efinaconazole. Efinaconazole (KP-103) is a triazole antifungal agent and againsts T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 μg/mL and 0.00098 μg/mL, respectively . Efinaconazole has a potent in vitro activity against fungal pathogens including dermatophytes, Candida and Malassezia species .
Gusacitinib-d4(ASN-002-d4) is the deuterium labeled Gusacitinib (HY-103018). Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5 .
Cinacalcet-d4(AMG-073-d4) hydrochlorideis deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment .
Vanzacaftor-d4(VX-121-d4) is the deuterium labeled Vanzacaftor (HY-145603). Vanzacaftor is an orally active noval corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves processing and trafficking of CFTR protein as well as increases chloride transport in triple combined with Tezacaftor (HY-15448) and Deutivacaftor. Vanzacaftor-Tezacaftor-Deutivacaftor is safe and well tolerated, improving lung function, respiratory symptoms, and CFTR function with cystic fibrosis, which is promising for research in the field of cystic fibrosis diseases .
Acipimox-d4 is the deuterium labeled Acipimox. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Hydroxymetronidazole-d4 is the deuterium labeled Hydroxymetronidazole. Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle .
(R)-Lansoprazole-d4 is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Rabeprazole-d4 potassium is deuterated labeled Rabeprazole potassium. Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an b>IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux .
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
Sarpogrelate-d4(MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis [4].
Famotidine-d4(MK-208-d4) is deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion .
Famciclovir-d4 is the deuterium labeled Famciclovir. Famciclovir (BRL 42810) is a guanine analogue antiviral agent used for the treatment of various herpesvirus infections .
Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
Latanoprost-d4 is the deuterium labeled Latanoprost. Latanoprost (PHXA41) is a prostaglandin F2α analogue and an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).
Sitagliptin-d4(MK-0431-d4) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
Sacubitril-d4 is the deuterium labeled Sacubitril. Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively .
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer [4] .
2-Mercaptoethanesulfonate-d4 sodium (Mesnum-d4 sodium) is the deuterium labeled Sodium 2-mercaptoethanesulfonate (HY-13679). Mesna (Sodium 2-mercaptoethanesulfonate) is an antioxidant which has cytoprotective effects. Mesna is widely used as a systemic protective agent against chemotherapy toxicity. Mesna is also used to reduce hemorrhagic cystitis induced by cyclophosphamide .
Raltegravir-d4 (potassium) (MK 0518-d4 (potassium)) is deuterium labeled Raltegravir (potassium). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CLpro activity [4].
Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
Remdesivir-d4(GS-5734-d4) is deuterium labeled Remdesivir (HY-104077). Remdesivir (GS-5734) is a nucleoside analogue with effective antiviral activity. Remdesivir can inhibit the synthesis of viral DNA or RNA. Remdesivir can be used for the research of infection, such as SARS-CoV and MHV infection .
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K .
Sitagliptin-d4 (hydrochloride) is the deuterium labeled Sitagliptin . Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Losartan-d4 is the deuterium labeled Losartan. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure .
2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide . 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics .
Quinapril-d4(CI-906-d4) is deuterium labeled Quinapril. Quinapril is a potent, orally active, non-peptide and nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE). Quinapril specifically interrupts the conversion of angiotensin I to angiotensin II in both plasma and tissue. Quinapril is enzymatically hydrolyzed to a pharmacologically active diacid form quinaprilat. Quinapril is efficacious in hypertensive models .
Rabeprazole-d4 is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux .
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors [4] .
Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively .
Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Ponesimod-d4(ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation [4].
Flecainide-d4 (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential .
Glycochenodeoxycholic acid-d4 is the deuterium labeled Glycochenodeoxycholic acid. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) induces hepatocyte apoptosis .
Prasugrel-d4 is the deuterium labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Cilnidipine-d4(FRC-8653-d4) is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca 2+-channel blocker on L and N-type Ca 2+ channel [4]. Antihypertensive effects .
Delamanid-d4 is the deuterium labeled Delamanid. Delamanid, a newer?mycobacterial cell wall synthesis ?inhibitor, inhibits the synthesisi of mucolic acids .
Prothioconazole-d4(JAU-6476-d4) is the deuterium labeled Prothioconazole (HY-116568). Prothioconazole is a triazolinthione fungicide. Prothioconazole is a CYP51 inhibitor .
Glasdegib-d4(PF-04449913-d4) is deuterium labeled Glasdegib. Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
Candesartan-d4(CV-11974-d4) is the deuterium labeled Candesartan (HY-B0205). Candesartan (CV 11974) is an orally active angiotensin II AT1-Receptor blocker and PPAR-γ agonist. Candesartan has potent and long-lasting antihypertensive effects. Candesartan can be used for the research of hypertension, chronic heart failure (CHF) and Traumatic brain injury (TBI).
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
Tecovirimat-d4(ST-246-d4) is a deuterium-labelled Tecovirimat (HY-14805). Tecovirimat is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat could be used in the study for orthopoxvirus-induced diseases [4] .
Eliglustat-d4 is the deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM .
Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levocetirizine-d4((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
Erdosteine-d4 is a deuterium labeled Erdosteine (HY-B0289). Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects .
Momelotinib-d4(CYT387-d4) dihydrochloride hydrate is a deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50s of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3 .
Diclazuril-d4 is deuterium labeled Diclazuril. Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. Diclazuril can be used for the research of certain infectious and parasitic diseases, including coccidiosis, acute toxoplasmosis, equine protozoal pyoencephalitis (EPM) et.al .
(R)-Pantetheine-d4(Pantetheine-d4) is the deuterium labeled (R)-Pantetheine (HY-126050). (R)-Pantetheine is the biosynthetic precursor to CoA. (R)-Pantetheine and its corresponding disulfide pantethine, play a key role in metabolism as a building block of coenzyme A (CoA). (R)-Pantetheine has high toxicity .
Meclofenamic acid-d4 is the deuterium labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker .
Ezetimibe-d4 (SCH 58235-d4) is the deuterium labeled Ezetimibe (HY-17376). Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Butenafine-d4 (KP363-d4) is the deuterium labeled Butenafine (HY-114518). Butenafine (KP363) is a potent and broad spectrum benzylamine antifungal agent . Butenafine inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation, leading to a deficiency of the fungal cell membranes. Butenafine is effective against dermatophytes infections, such as ?tinea pedis, ?tinea cruris, tinea versicolor .
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
Dapagliflozin-d4(BMS-512148-d4) is deuterium labeled Dapagliflozin. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction . Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
Elacestrant-d4(RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Methylprednisolone-d4 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels .
Dasatinib-d4(BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Rabeprazole-d4 (sodium) is the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
Olmesartan-d4(RNH-6270-d4) is the deuterium labeled Olmesartan (HY-17004). Olmesartan is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma [4].
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
Pazufloxacin-d4 is deuterium labeled Pazufloxacin (HY-B0724B). Pazufloxacin is an orally active fluoroquinolone antimicrobial agent. Pazufloxacin inhibits DNA gyrase with IC50 values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). Pazufloxacin exhibits broad-spectrum antimicrobial activity, with MIC90 values ranging from 0.025 to 100 μg/mL against Gram-positive and Gram-negative bacteria, non-fermenting bacteria, Legionella spp., and anaerobic bacteria. Pazufloxacin is indicated for research on systemic infections, lung infections, urinary tract infections, and Legionella pneumonia [4] .
Glycoursodeoxycholic acid-d4(Ursodeoxycholylglycine-d4) is the deuterium labeled Glycoursodeoxycholic acid. Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid .
Lumateperone-d4(ITI-007-d4) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .
Fluconazole-d4 is the deuterium labeled Fluconazole. Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL .
Nemonoxacin-d4 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
Piroxicam-d4 is the deuterium labeled Piroxicam. Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
Didesethyl chloroquine-d4 is the deuterium labeled Didesethyl chloroquine. Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial agent Chloroquine. Didesethyl chloroquine is a potent myocardial depressant .
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Estragole-d4 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity [4] [10] .
Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
Empagliflozin-d4 is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2 .
Ciprofloxacin-d4(Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity [4].
Bimatoprost-d4 is the deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface .
Flurbiprofen-d4 is deuterated labeled Flurbiprofen (HY-10582). Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma [4] .
Urea-d4 is the deuterium labeled Urea . Urea is a powerful protein denaturant via both direct and indirect mechanisms . A potent emollient and keratolytic agent . Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function [4]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic .
Glutathione oxidized- 13C4, 15N2 is the 13C and 15N labeled Glutathione oxidized (HY-D0844). Glutathione oxidized is produced by the oxidation of glutathione. Detoxification of reactive oxygen species is accompanied by production of glutathione oxidized. Glutathione oxidized can be used for the research of sickle cells and erythrocytes .
Inosinic acid- 15N4 dilithium (5'-IMP-15N4 (dilithium); IMP-15N4 (dilithium); Inosine 5'-(dihydrogen phosphate)-15N4 (dilithium)) is 15N-labeled Inosinic acid (HY-108213). Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant, or as the dietary supplement to improve the yield and meat quality of pigs .
Ceftolozane- 15N2,d4 (CXA-101- 15N2,d4) TFA is the 15N- and deuterium-labeled Ceftolozane TFA (HY-106257A). Ceftolozane TFA is a cephalosporin antibiotic that can be used to inhibit Gram-negative bacterial infections. Ceftolozane TFA can be used to synthesize new antibiotic that are more potent and safer .
Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent . Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor [4].
N6-Methyladenosine- 13C4 (6-Methyladenosine- 13C4; N-Methyladenosine- 13C4) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
Rivaroxaban-d4 (BAY 59-7939-d4) is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM) .
N-Acetylsulfanilamide-d4(4-Acetamidobenzenesulfonamide-d4) is a deuterium labeled N-Acetylsulfanilamide (HY-W069721). N-Acetylsulfanilamide is a compound with potential anti-infective activity .
Sulfamethoxazole-d4 (Ro 4-2130-d4) is a deuterium labeled Sulfamethoxazole (HY-B0322). Sulfamethoxazole (Ro 4-2130) is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
Diethyl succinate-d4 is the deuterium labeled Diethyl succinate . Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring .
Eslicarbazepine-d4 (BIA 2-194-d4) is deuterium labeled Eslicarbazepine. Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
Dihydrouracil-d4 is the deuterium labeled Dihydrouracil . Dihydrouracil (HY-W012926), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient .
Fenofibric acid-d4 (FNF acid-d4) is deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
cis-Atovaquone-d4 is deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Nonanoic acid-d4 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
Minodronic acid-d4 is deuterium labeled Minodronic acid. Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain .
Suberic acid-d4 is the deuterium labeled Suberic acid . Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency .
Taurine-d4 is the deuterium labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
Hydroxychloroquine-d4 (sulfate) is the deuterium labeled Hydroxychloroquine sulfate. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro .
Isobutylparaben-d4 is the deuterium labeled Isobutylparaben. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics .
Tenoxicam-d4(Ro-12-0068-d4) is the deuterium labeled Tenoxicam (HY-B0440). Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
Lansoprazole sulfone-d4(AG-1813-d4) is the deuterium labeled Lansoprazole sulfone. Lansoprazole sulfone-d4 is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone-d4 can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone-d4 has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease .
Moxifloxacin-d4 hydrochloride (BAY 12-8039-d4) is the hydrochloride salt form of deuterium labeled Moxifloxacin (Moxifloxacin). Moxifloxacin is an orally active antimicrobial, that can be used in the research of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Climbazole-d4 is the deuterium labeled Climbazole. Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450 .
Benzyl salicylate-d4 (NSC 6647-d4) is the deuterium labeled Benzyl salicylate (HY-B1556). Benzyl salicylate (NSC 6647)?is a salicylic acid benzyl ester. It can be used as a fragrance additive or UV light absorber .
Taurocholic acid-d4 (sodium) is the deuterium labeled Taurocholic acid. Taurocholic acid (N-Choloyltaurine) is a bile acid involved in the emulsification of fats.
Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
SAH-d4 is the deuterium labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine . SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 μM .
Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects .
21-Desacetyldeflazacort-d4(21-desDFZ-d4) is the deuterium labeled 21-Desacetyldeflazacort (HY-100085). 21-Desacetyldeflazacort (21-desDFZ) is the active metabolite of Deflazacort (HY-13609). Deflazacort is an anti-inflammatory and immunosuppressant. Deflazacort is an inactive pro-drug which can be rapidly converted by esterases to the active metabolite 21-desacetyldeflazacort after oral administration .
Cefadroxil-d4 (hydrate) is the deuterium labeled Cefadroxil hydrate (HY-B1190A). Cefadroxil hydrate is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil hydrate inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil hydrate is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil hydrate has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain [4] .
4-Methylanisole-d7 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
4-Hydroxynonenal-d3 is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria .
Succinic-2,2,3,3-d4 acid is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
Glycohyocholic acid-d4 is the deuterium labeled Glycohyocholic acid (HY-122141). Glycohyocholic acid (GHCA) is a primary conjugated bile acid formed by the conjugation of Cholic acid (HY-N0324) and Glycine (HY-Y0966). Glycohyocholic acid can be used in the study of hepatitis C-related cirrhosis and diabetes mellitus [4].
Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
Tolcapone-d4 (Ro 40-7592-d4) is the deuterium labeled Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4].
Nifedipine-d4 is the deuterium labeled Nifedipine. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
DSG Crosslinker-d4 is the deuterium labeled DSG Crosslinker. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Acarbose-d4 (BAY g 5421-d4) is deuterium labeled Acarbose. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate . Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products . A systemic acquired resistance (SAR) signal in tobacco . A topical nonsteroidal anti-inflammatory agent (NSAID). Methyl salicylate lactoside is a COX inhibitor .
1-Undecanol-d4 (Undecyl alcohol-d4) is the deuterium labeled 1-Undecanol (HY-W004292). 1-Undecanol (Undecyl alcohol) is the main product generated from the degradation of 2-tridecanone by Pseudomonas bacteria isolated from the soil. 1-Undecanol can enhance the attraction of Grapholita molesta to sex pheromone traps .
5-Methoxytryptamine-d4 (O-Methylserotonin-d4) is the deuterium labeled 5-Methoxytryptamine (HY-W015169). 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .
Vortioxetine-d4 (Lu AA 21004-d4) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
Sitafloxacin-d4(DU6859a-d4) is deuterium labeled Sitafloxacin. Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection .
Taurochenodeoxycholic acid-d4 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
Veratrole-d4 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment .
Ramatroban-d4 is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
Arachidic acid-d4 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Adipic acid-d4 (Hexanedioic acid-d4) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Docosanoic acid-d4 (Behenic acid-4) is deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Sorafenib-d4 (Bay 43-9006-d4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
Lansoprazole sulfide-d4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacterium tuberculosis) agent with IC50 values of 0.59 μM intracellularly and 0.46 μM in broth .
Tryptophol-d4(Indole-3-ethanol-d4) is the deuterium labeled Tryptophol (HY-W010155). Tryptophol is an aromatic alcohol and secondary metabolite produced by microorganisms. Tryptophol induces apoptosis and cleavage of caspase-8. Tryptophol inhibits Cunninghamella blakesleeana biofilm. Tryptophol has anti-phage infection, biofilm formation regulation, anti-inflammatory, hemolytic, sleep induction, temperature change, seizure susceptibility and immune regulation activities. Tryptophol is used in the research of African trypanosomiasis, sleep disorders, epilepsy [4] .
Clofibric acid-d4 is the deuterium labeled Clofibric acid (HY-B1415). Clofibric acid also is an herbicideClofibric acid (Chlorofibrinic acid) is an orally active PPARα agonist. Clofibric acid inhibits the fimbriation of Escherichia coli. Clofibric acid increases SOD activity. Clofibric acid lowers blood lipids and prevents experimental pyelonephritis. Clofibric acid has anticancer activity against ovarian cancer. Clofibric acid is also a herbicide. Clofibric acid is used in ovarian cancer, liver cancer, obesity, and urinary tract infection research [4] .
Alendronate-d4 (sodium) (Alendronic acid-d4 (monosodium salt)) is deuterium labeled Alendronate sodium. Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis .
Asoxime-d4 (dichloride) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system .
N4-Acetylsulfamethoxazole-d4 is the deuterium labeled N4-Acetylsulfamethoxazole. N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of?Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections .
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease [4] .
4-Methylanisole-d3 is the deuterium labeled 4-Methylanisole . 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil .
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis .
Deruxtecan-d4 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
DPPC-d4 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in m
4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Antipyrine in the brain .
13,14-Dihydro-15-keto prostaglandin D2-d4(DK-PGD2-d4) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
Serotonin- 13C,D4(5-Hydroxytryptamine-13C,D4) is a 13C- and deuterated labeled Serotonin (HY-B1473A). Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
DSPC-d4(1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid . 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
4-Phenylbutyric acid-d11 is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid . 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research [4].
Inosinic acid- 13C10, 15N4 dilithium (5'-IMP-13C10,15N4 (dilithium); IMP-13C10,15N4 (dilithium); Inosine 5'-(dihydrogen phosphate)-13C10,15N4 (dilithium)) is 13C- and 15N-labeled Inosinic acid (HY-108213). Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant, or as the dietary supplement to improve the yield and meat quality of pigs .
1,2-Dihydropyridazine-3,6-dione-3,4,5,6- 13C4 (1,2-Dihydro-3,6-pyridazine- 13C4-dione) is 13C labeled Maleic hydrazide. Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins .
Hypoxanthine- 13C5, 15N4 is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Donepezil-d4(E2020-d4 (free base)) is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Dimethyl adipate-d4 (Hexanedioic acid dimethyl ester-d4) is the deuterium labeled Dimethyl adipate (HY-W015301). Dimethyl adipate is an aliphatic dicarboxylate compound. Dimethyl adipate is mainly used as a plasticizer and an intermediate in organic synthesis.
3-Amino-2-oxazolidinone-d4(AOZ-d4) is a deuterium labeled 3-Amino-2-oxazolidinone (HY-W012982). 3-Amino-2-oxazolidinone (AOZ) is the metabolite of Furazolidone (HY-B1336). 3-Amino-2-oxazolidinone is always be detected as a indicator of furazolidone residues in vivo. 3-Amino-2-oxazolidinone is orally active .
Pitavastatin-d4-1(NK-104-d4-1) sodium is the deuterium labeled Pitavastatin sodium (HY-B0144B). Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects [4].
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Anti-cancer and anticonvulsant effects .
Melatonin-d4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties . Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation [4].
(S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX) .
Vilanterol-d4 (trifenatate) is deuterium labeled Vilanterol (trifenatate).Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research.
Folinic acid-d4-1(Leucovorin-d4-1) calcium hydrate is deuterated labeled Folinic acid (HY-17556). Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (HY-14519) as a rescue agent to decrease Methotrexate-induced toxicity.
Mono(3-carboxypropyl) phthalate-d4(MCPP-d4) is a deuterium labeled Mono(3-carboxypropyl) phthalate (HY-133673). Mono(3-carboxypropyl) phthalate (MCPP) is a metabolite of Di-n-octyl phthalate. Di-n-octyl phthalate (DnOP) is a plasticizer used in polyvinyl chloride plastics, cellulose esters, and polystyrene resins .
Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
1,4-Dibromobenzene-d4 is a deuterium labeled 1,4-Dibromobenzene. 1,4-Dibromobenzene is used as a fumigant and as a chemical intermediate for pharmaceuticals. Inhalation exposure gives rise to dizziness and chokingwhereas contact with skin or eye produces inflammation and burning in humans .
Methyl paraben-d4 is the deuterium labeled Methyl Paraben . Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity .
4-Hydroxypropranolol-d7 is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .
Pimozide-d4-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5 [4].
Indole-3-acetyl glutamate-d4(IAGlu-d4) is deuterium labeled Indole-3-acetyl glutamate. Indole-3-acetyl glutamate (IAGlu) is a derivative of the plant hormone indole-3-acetic acid (IAA). As a conjugated form of IAA, Indole-3-acetyl glutamate involves in the transport, storage, and homeostatic regulation of IAA within the plant. Indole-3-acetyl glutamate can be used for research into the effects of plant hormones on the growth and development of plants .
Triclocarban-d4 is the deuterium labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
Latanoprost ethyl amide-d4(Lat-NEt-d4) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .
Bendamustine-d4 is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
Paliperidone palmitate-d4 (9-Hydroxyrisperidone palmitate-d4) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .
4-Methylanisole-d7-1 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
4-Methylpentanoic acid-d12 is the deuterium labeled 4-Methylpentanoic acid. 4-Methylpentanoic acid (Isocaproic Acid) is a Short chain fatty acid (SCFA) .
Prostaglandin D2-d4 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals . Prostaglandin D2 is one of the most potent endogenous sleep promoting substances . PGD2 plays a protective role by suppressing inflammation .
Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Delamanid-d4-1 is deuterated labeled Delamanid.Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids .
Sacubitril-d4 hemicalcium salt is the deuterium labeled Sacubitril hemicalcium salt (HY-15407A). Sacubitril hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM [4].
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
(R)-Carvedilol-d4 is deuterium labeled (R)-Carvedilol (HY-B0006C). (R)-Carvedilol ((R)-BM 14190) is the orally active R-isomer of Carvedilol (HY-B0006). (R)-Carvedilol has α-receptor blocking activity but no β-receptor blocking activity. (R)-Carvedilol inhibits spontaneous Ca 2+ waves. (R)-Carvedilol inhibits stress-induced ventricular tachycardia and delays the development of UV-induced skin tumors and reduces their malignancy [4].
Creosol-d4(2-Methoxy-4-methylphenol-d4) is the deuterium labeled Creosol (HY-W040971). Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable .
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Dimethyl phthalate (Ring-d4) is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins .
Desloratadine-d4 hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Prostaglandin D1-d4(PGD1-d4) is deuterium labeled Prostaglandin D1. Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
4-Methyl-1-pentanol-d7 (Isohexanol-d7) is the deuterium labeled 4-Methyl-1-pentanol (HY-W007511). 4-Methyl-1-pentanol is a volatile aroma component of red wine, which is often used in the production and blending of wine. 4-Methyl-1-pentanol can also be used as an alcohol antagonist to antagonize the effects of ethanol and 1-butanol on cell-cell adhesion, and is used in the study of fetal alcohol syndrome [4] .
Riboflavin- 13C4, 15N2is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Raspberry ketone-d5 (Frambione-d5; 4-(4-Hydroxyphenyl)-2-butanone-d5) is the deuterium labeled Raspberry ketone (HY-N1426). Raspberry ketone is a major aromatic compound of red raspberry, widely used as a fragrance in cosmetics and as a flavoring agent in foodstuff; also shows PPAR-α agonistic activity.
DL-Arginine- 15N4,d7 hydrochloride is deuterium and 15N labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Dimethyl phthalate- 13C6,d4 (DMP- 13C6,d4) is the deuterium labeled and 13C-labeled Dimethyl phthalate (HY-N7106). Dimethyl phthalate (DMP) can be used as a plasticizer to impart flexibility to rigid polyvinyl chloride (PVC) resin. Additionally, Dimethyl phthalate is an oral active endocrine disruptor that can cause ovarian dysfunction in mice. Dimethyl phthalate can also induce oxidative stress and apoptosis in cells, thereby affecting blood and red blood cell function in rats .
Inosine-5'-diphosphate- 15N4 dilithium (IDP- 15N4 dilithium) is 15N labeled Inosine-5'-diphosphate dilithium. Inosine-5'-diphosphate (IDP) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research [4].
p-Toluic acid-d4 is the deuterium labeled p-Toluic acid . p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Taurochenodeoxycholic acid-d4-1 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) sodium is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
4-Acetamidobutanoic acid-d3 is the deuterated analog of 4-Acetamidobutanoic acid (HY-101411). 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities .
Lignoceric acid-d4-2 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research .
Docosanoic acid-d4-1 (Behenic acid-d4-1) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Moxifloxacin-d4 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Pyridoxine- 13C4 (Pyridoxol- 13C4) is 13C labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
3-Methoxytyramine-d4 (hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride. 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1) .
Deruxtecan-d4-1 is the deuterium labeled Adenosine Deruxtecan (HY-13631E) . Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
L-Alanine-d4 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N-Nitrosonornicotine-d4((2S)-N'-Nitrosonornicotine-d4) is deuterium labeled N-Nitrosonornicotine. N-Nitrosonornicotine is a tobacco-specific nitrosamine that has carcinogenic and mutagenic activity, and it can induce micronuclei in C3A cells. N-Nitrosonornicotine can form DNA adducts .
Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
Docosanoic acid-d4-2 (Behenic acid-d4-2) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
DL-Lysine-4,4,5,5-d4 (dihydrochloride) is the deuterium labeled DL-Lysine. DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins .
L-Glutamine-d4 (L-Glutamic acid 5-amide-d4) is the deuterium labeled L-Glutamine (HY-N0390). L-Glutamine is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
p-Cresol sulfate-d4 (potassium) is deuterium labeled p-Cresyl sulfate (potassium). p-Cresyl sulfate potassium is a uremic toxin that binds to a prototype protein. p-Cresyl sulfate potassium activates the JNK and p38 MAPK signaling pathways. p-Cresyl sulfate potassium has pro-inflammatory activity .
Dimethyl adipate-d4-1 (Hexanedioic acid dimethyl ester-d4-1) is the deuterium labeled Dimethyl adipate (HY-W015301). Dimethyl adipate is an aliphatic dicarboxylate compound. Dimethyl adipate is mainly used as a plasticizer and an intermediate in organic synthesis.
Adipic acid-d4-1 (Hexanedioic acid-d4-1) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
3-Methyl-2-quinoxalinecarboxylic acid-d4 is the deuterium labeled 3-Methyl-2-quinoxalinecarboxylic acid. 3-Methyl-2-quinoxalinecarboxylic acid (MQCA), an important N-oxide reductive metabolite of Quinocetone or Olaquindox, potently inhibits the growth of Chang liver cells through S phase arrest of the cell cycle .
3-O-Methyltolcapone-d4 (Ro 40-7591 d4) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4] .
Monomethyl phthalate-d4 (2-(Methoxycarbonyl)benzoic acid-d4) is the deuterium labeled Monomethyl phthalate. Monomethyl phthalate is a phthalate metabolite. Monomethyl phthalate acts as a urinary biomarker of phthalates exposure and can be used as a standard for the determination of thyroid cancer and benign nodule .
Monooctyl phthalate-d4 (Mono-n-octyl phthalate-d4) is a deuterium labeled Monooctyl phthalate (HY-133671). Monooctyl phthalate (Mono-n-octyl phthalate) exhibits antimycobacterial activity with a MIC of 20 μg/mL .
Clindamycin-d3 (hydrochloride) is the deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 μM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM .
(R)-3-Hydroxybutanoic acid- 13C4 sodium is a 13C labeled (R)-3-Hydroxybutanoic acid (HY-W051723). (R)-3-Hydroxybutanoic acid is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones .
Riboflavin-5-Phosphate- 13C4, 15N2-1 is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
L-Arginine- 15N4,d7 (hydrochloride) is the deuterium and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
4-[[(4-Fluorophenyl)imino]methyl]phenol-d4(4-{(E)-[(4-Fluorophenyl)imino]methyl}phenol-d4) is the deuterium labeled 4-[[(4-Fluorophenyl)imino]methyl]phenol (HY-W014178).
Bexarotene- 13C4 (LGD1069- 13C4) is the 13C-labeled Bexarotene (HY-14171). Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
Resolvin E1-d4-1 is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production .
Ethylenediaminetetraacetic acid- 13C4 (EDTA- 13C4) is the 13C-labeled Ethylenediaminetetraacetic acid (HY-Y0682). Ethylenediaminetetraacetic acid (EDTA) is a kind of metal chelating agent (binds to bivalent and trivalent metal cations, including calcium). Ethylenediaminetetraacetic acid has antibacterial, anti-inflammatory, antioxidant, anti-hypercalcemia and anticoagulant activities. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can alleviate the liver fibrosis. Ethylenediaminetetraacetic acid can be used for coronary artery disease and neural system disease research [4] .
Coproporphyrin III- 15N4 (Zincphyrin- 15N4) is the 15N-labeled Coproporphyrin III (HY-101398). Coproporphyrin III (Zincphyrin) is a naturally occurring porphyrin derivative that is mainly found in urine .
Timonacic-d4 (1,3-Thiazolidine-4-carboxylicacid-d4) is deuterium labeled Timonacic. Timonacic (1,3-Thiazolidine-4-carboxylic acid) is a thiol antioxidant. Timonacic has anti-aging and anti-hepatotoxic effects, and it can be used to study acute illnesses and liver diseases, by inducing reversal, it is also used in research on certain cancer cases .
Mono(7-carboxy-2-methyloctyl) phthalate-d4(MCNP-d4) is the deuterium labeled Mono(7-carboxy-2-methyloctyl) phthalate (HY-133679). Mono(7-carboxy-2-methyloctyl) phthalate (MCNP) is a metabolite of Di-decyl phthalate (DDP) .
3-Hydroxybutyric acid-d4 (sodium) is the deuterium labeled 3-Hydroxybutyric acid. 3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids .
Sacubitril-13C4 (AHU-377-13C4) is a 13C-labeled version of Sacubitril (HY-15407). Sacubitril is an orally active inhibitor of neprilysin NEP (IC50=5 nM). Sacubitril is used in research on heart failure, hypertension and COVID-19 [4] .
2-Ketoglutaric acid-d4 (Alpha-Ketoglutaric acid-d4) is the deuterium labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid Sodium is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM) .
8-Isoprostaglandin E2-d4(iPE2-III-d4) is deuterium labeled 8-Isoprostaglandin E2. 8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway .
Arachidonic acid- 13C4 (Immunocytophyt- 13C4) is 13C labeled Arachidonic acid. Arachidonic acid (Immunocytophyt) is a polyunsaturated omega-6 fatty acid and a major constituent of biomembranes. Arachidonic acid also acts as the substrate for various lipid mediators, such as prostaglandins (PGs). Arachidonic acid improves cognitive response and cardiovascular function .
Estradiol valerianate-d4 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
Mono(5-carboxy-2-ethylpentyl) phthalate-d4(MECPP-d4) is a deuterium labeled Mono(5-carboxy-2-ethylpentyl) phthalate (HY-133675). Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking .
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells [4] .
N-Heptyl 4-hydroxybenzoate-d4 is the deuterium labeled N-Heptyl 4-hydroxybenzoate (HY-W150903) . N-Heptyl 4-hydroxybenzoate (p-Oxybenzoesaureheptylester) is an antimicrobial agent that inhibits S. aureus with MIC of 12.5 μg/mL. N-Heptyl 4-hydroxybenzoate also against plant pathogenic fungi, such as Alternaria brassicicola, F. solani, C. dematium and C. acutatum .
Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4(MEHHP-d4) is a deuterium labeled Mono(2-ethyl-5-hydroxyhexyl) phthalate (HY-133677). Mono(2-ethyl-5-hydroxyhexyl) phthalate (MEHHP) is an oxidative metabolite of Di(2-ethylhexyl) phthalate (DEHP). Mono(2-ethyl-5-hydroxyhexyl) phthalate may protective sperm DNA damage. Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking .
Monobenzyl phthalate-d4 is the deuterium labeled Monobenzyl phthalate. Monobenzyl phthalate (2-((Benzyloxy)carbonyl)benzoic acid) is the urinary metabolite exposuring to phthalates, such as, diethylhexyl phthalate (DEHP) .
Clindamycin- 13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
4-(4-Fluorobenzylamino)-1-methylpiperidine-d2(N-[(4-Fluorophenyl)methyl]-1-methyl-4-piperidinamine-d2) is the deuterium labeled 4-(4-Fluorobenzylamino)-1-methylpiperidine.
1-Methylpiperidin-4-ol-d4(N-Methyl-4-piperidinol-d4) is the deuterium labeled 1-Methylpiperidin-4-ol (HY-W018626). 1-Methylpiperidin-4-ol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Butyric acid-13C4 sodium (Butanoic acid-13C4 sodium) is a stable isotope labeled compound with the activity of promoting cell proliferation and regulating gene expression. Butyric acid-13C4 sodium can be used in metabolic research and compound development to help scientists gain a deeper understanding of the role of short-chain fatty acids in organisms. Butyric acid-13C4 sodium also plays an important role in nutrition and intestinal health research, especially in the regulation of probiotic function and intestinal microbiota.
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
4,4'-Sulfonyldiphenol-d8 (Bisphenol S (4,4'-Sulfonyldiphenol)-d8) is the deuterium labeled 4,4'-Sulfonyldiphenol (HY-W011927).4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone), a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
(S)-2-Aminohexanedioic acid-d4 is the deuterium labeled (S)-2-Aminohexanedioic acid. (S)-2-Aminohexanedioic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Docosanoic acid- 13C4 (Behenic acid- 13C4) is the 13C-labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in vivo .
Pseudane IX-d4(2-Nonylquinolin-4(1H)-one-d4) is deuterium labeled Pseudane IX. Pseudane IX, a compound isolated from the leaves of Ruta angustifolia, has strong anti-HCV activity with an IC50 value of 1.4 μg/mL. Pseudane IX reduces HCV RNA replication and viral protein synthesis levels .
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
L-Arginine- 15N4 (hydrochloride) is the 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis .
(Rac)-Moxifloxacin-d4 ((Rac)-BAY 12-8039-d4 (free base)) is deuterium labeled (Rac)-Moxifloxacin. (Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Octanoic acid- 13C4 is the 13C labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
rac cis-Moxifloxacin-d4 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin Hydrochloride (BAY 12-8039) is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Succinic acid- 13C4 is the 13C labeled Succinic acid . Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries .
Methyl arachidonate- 13C4 (Arachidonic acid methyl ester- 13C4) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
DL-Arginine- 13C6, 15N4,d7 hydrochloride is 13C and 15N-labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Allantoin- 13C2, 15N4 is the 13C and 15N labeled Allantoin . Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth .
DL-Arginine- 13C6, 15N4 hydrochloride is 13C and 15N-labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
DL-α-Tocopherol acetate- 13C4,d6 is the deuterium and 13C labeled DL-α-Tocopherol acetate . DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition .
Bisphenol F- 13C12 is the 13C labeled Bisphenol F (HY-W014901). Bisphenol F is an orally active endocrine disruptor. Bisphenol F promotes ROS generation, upregulates p-AKT/p-GSK3β, and induces Apoptosis. Bisphenol F interferes with glucose metabolism, affects neurodevelopment and reproductive function. Bisphenol F reduces social novelty preference in mouse offspring. Bisphenol F can be used in bone, blood, and fat-related studies. Bisphenol F is used as a substitute for Bisphenol A (HY-18260) [4] .
Bisphenol F- 13C6 is the 13C labeled Bisphenol F (HY-W014901). Bisphenol F is an orally active endocrine disruptor. Bisphenol F promotes ROS generation, upregulates p-AKT/p-GSK3β, and induces Apoptosis. Bisphenol F interferes with glucose metabolism, affects neurodevelopment and reproductive function. Bisphenol F reduces social novelty preference in mouse offspring. Bisphenol F can be used in bone, blood, and fat-related studies. Bisphenol F is used as a substitute for Bisphenol A (HY-18260) [4] .
L-Arginine- 13C6, 15N4,d7 (hydrochloride) is the deuterium, 13C-, and 15-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
13-cis-4-Oxoretinoic acid-d6 (4-Keto 13-cis-retinoic acid-d6; 4-Oxoisotretinoin-d6; Ro 22-6595-d6) is the deuterium labeled 13-cis-4-Oxoretinoic acid (HY-107494). 13-cis-4-Oxoretinoic acid (4-Keto 13-cis-retinoic acid) is a metabolite of vitamin A in human plasma .
4-Hydroxy-1-(pyridin-3-yl)butan-1-one-d4(4-Hydroxy-1-(3-pyridyl)-1-butanone-d4) is the deuterium labeled 4-Hydroxy-1-(pyridin-3-yl)butan-1-one (HY-W270498).
Lactic acid-d4 (DL-Lactic acid-d4) sodium (60% in water) is the deuterium labeled Lactic acid sodium (60% in water) (HY-B2227B) . Lactic acid (DL-Lactic acid) sodium (60% w/w in water) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium (60% w/w in water) is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium (60% w/w in water) is an oncometabolite and has immune protective role of lactate in anti-tumor immunity . Lactic acid sodium (60% w/w in water) also has antimicrobial activity, which can be used as a food preservative .
Oxaloacetic acid- 13C4 is the 13C-labeled Oxaloacetic acid. Oxaloacetic acid (2-Oxosuccinic acid) is a metabolic intermediate involved in several ways, such as citric acid cycle, gluconeogenesis, the urea cycle, the glyoxylate cycle, amino acid synthesis, and fatty acid synthesis .
Isoallolithocholic acid-d4 (3β-Hydroxy-5α-cholanic acid-d4) is deuterium labeled Isoallolithocholic acid. Isoallolithocholic acid (3β-Hydroxy-5α-cholanic acid), a derivative of Lithocholic acid (HY-10219), is a T cell regulator. Isoallolithocholic acid enhances regulatory T cells (Tregs) differentiation .
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
NH2-C2-NH-Boc-d4 is the deuterium labeled NH2-C2-NH-Boc . NH2-C2-NH-Boc (PROTAC Linker 22) is a alkyl chain-based PROTAC linker can be used in the synthesis of PROTACs .
4-Trifluoromethylsalicylic acid- 13C6 is the 13C labeled 4-Trifluoromethylsalicylic acid . 4-Trifluoromethylsalicylic acid is a platelet aggregation inhibitor .
S 8849-1-d4 (free base) (Tianeptine metabolite MC5-d4) is deuterium labeled S 8849-1 (free base). S 8849-1 (free base) (Tianeptine metabolite MC5) is a Tianeptine (HY-90003) metabolite that is found in plasma. The mean elimination half-lives of S 8849-1 (free base) is 7.53 h in rats. S 8849-1 (free base) is promising for research of antidepressants .
Succinyladenosine- 13C4 (N6-Succinyl adenosine- 13C4) is the 13C-labeled Succinyladenosine (HY-113284). Succinyladenosine, the metabolic product of dephosphorylation of intracellular adenylosuccinic acid (S-AMP) by cytosolic 5-nucleotidase, is a biochemical marker of adenylosuccinase (ASL) deficiency .
17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid .
2-Nonyl-3-hydroxy-4-quinolone-d4(C9-PQS-d4) is deuterium labeled 2-Nonyl-3-hydroxy-4-quinolone. 2-nonyl-3-hydroxy-4-Quinolone (C9-PQS) is a quinolone compound produced by P. aeruginosa and other related bacterias. 2-nonyl-3-hydroxy-4-Quinolone is a quorum sensing (QS) signal molecule that controls the expression of many virulence genes as a function of cell population density .
2,5-Deoxyfructosazine- 13C4 (NSC 270912- 13C4) is the 13C-labeled 2,5-Deoxyfructosazine (HY-135078). 2,5-Deoxyfructosazine is a pyrazine derivative that can be found in cured tobacco and is used as a flavoring agent in the food and tobacco industry. Pyrazines, including 2,5-deoxyfructosazine, can be produced either by pyrolytic decomposition of natural compounds or by the reaction of sugars with alcoholic ammonia. 2,5-Deoxyfructosazine is also formed by the breakdown of D-glucosamine at neutral pH. Like glucosamine, 2,5-deoxyfructosazine has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC50=~1.25 mM).
Sacubitril- 13C4 (hemicalcium salt) is a 13C-labeled and deuterium labeled Sacubitril hemicalcium salt. Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696 .
N-(2-Iodophenyl)-4-methylbenzenesulfonamide-d4(N-Tosyl-2-iodoaniline-d4) is the deuterium labeled N-(2-Iodophenyl)-4-methylbenzenesulfonamide (HY-W024801).
4-Hydroxyestrone- 13C6 is a 13C-labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone (4-OHE1), an estrone metabolite, has strong neuroprotective effect against oxidative neurotoxicity. 4-Hydroxyestrone increases cytoplasmic translocation of p53 resulting from SIRT1-mediated deacetylation of p53. 4-Hydroxyestrone has little estrogenic activity .
Dihydrouracil- 13C4, 15N2 is the 13C and 15N labeled Dihydrouracil . Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient .
5-Fluorouracil- 13C4, 15N2 is the 13C and 15N labeled 5-Fluorouracil . 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer . 5-Fluorouracil also inhibits HIV [4].
L-Arginine- 13C6, 15N4 (hydrochloride) is the 13C- and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Talaporfin- 13C4, 15N (ME2906 (free acid)- 13C4, 15N) is the 13C- and 15N-labeled Talaporfin (HY-16477A). Talaporfin sodium, can be used in intraoperative photodynamic therapy (PDT) with a 664-nm semiconductor laser, was evaluated for efficacy and safety in treating primary malignant parenchymal brain tumors .
4-(2-(5-Ethylpyridin-2-yl)ethoxy)benzaldehyde-d4(4-[2-(5-ethyl-pyridin-2-yl)-ethoxy]-benzaldehyde-d4) is the deuterium labeled 4-(2-(5-Ethylpyridin-2-yl)ethoxy)benzaldehyde (HY-W329684).
Indinavir- 13C4, 15N (MK-639 (free base)- 13C4, 15N) is 13C and 15N labeled Indinavir. Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL pro inhibitor [4].
4-Nonylphenol-d5 is the deuterium labeled 4-Nonylphenol. 4-Nonylphenol, a major degradation product of Nonylphenol ethoxylates (NPEOs), is a persistent organic pollutant with endocrine-disrupting properties and exerts estrogenic activity .
Pyruvic acid- 13C,d4 is the deuterium and 13C labeled Pyruvic acid . Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats .
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Histamine-α,α,β,β-d4 (dihydrochloride) is the deuterium labeled Histamine. Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
Pyridinium bisretinoid A2E-d4 TFA is the deuterium-labeled Pyridinium bisretinoid A2E (HY-134928). Pyridinium bisretinoid A2E (A2E)is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E mediates autophagy and the production of reactive oxygen species [4].
Azetidine-2-carboxylic acid-d4 (D,L-Azetidine-2-carboxylic acid-d4) is the deuterium labeled Azetidine-2-carboxylic acid (HY-75308). Azetidine-2-carboxylic acid is a non proteinogenic amino acid homologue of proline. Found in common beets. Azetidine-2-carboxylic acid can be misincorporated into proteins in place of proline in many species, including humans. Toxic and teratogenic agent .
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
4-Hydroxy-5-methylfuran-3(2H)-one-d3 is deuterated labeled 4-Hydroxy-5-methylfuran-3(2H)-one (HY-W012927). 4-Hydroxy-5-methylfuran-3(2H)-one (Chicory furaneol) can be used to assay oxidoreductase activity. 4-Hydroxy-5-methylfuran-3(2H)-one is a kind of biological materials or organic compounds that are widely used in life science research .
Geranylgeraniol-d5 is the deuterium labeled Geranylgeraniol (HY-W011474). Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [4].
4,4'-Sulfonyldiphenol- 13C12 (Bisphenol S- 13C12) is 13C labeled 4,4'-Sulfonyldiphenol. 4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Calcitonin- 13C6, 15N4 (salmon) (Salmon calcitonin- 13C6, 15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
Bisphenol AF- 13C12 is an isotopic label of Bisphenol AF. Bisphenol AF is used in polycarbonate plastic and epoxy resin manufacturing. Bisphenol AF can significantly increase intracellular ROS levels .
3-Hydroxybutyric acid- 13C4 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids .
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .
L-Hydroxyproline-d4 is deuterium labeled L-Hydroxyproline. L-Hydroxyproline, one of the hydroxyproline (Hyp) isomers, is a useful chiral building block in the production of many pharmaceuticals .
11-Beta-hydroxyandrostenedione-d4 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor .
L-Alanine- 13C3, 15N,d4 is the deuterium, 13C-, and 15-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
4-Amino-TEMPO-d17(4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl-d17) is the deuterium labeled 4-Amino-TEMPO (HY-W002004). 4-Amino-TEMPO (4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl) is a stable nitroxide radical and N-nucleophile based on TEMPO. 4-Amino-TEMPO has superoxide dismutase-mimetic activity, can protect cells from oxidative damage, and has radioprotective effects. 4-Amino-TEMPO is widely used in fields such as biomedicine, materials science, and industrial production. 4-Amino-TEMPO can be used as a spin label to detect free radicals, an oxidation catalyst in industrial production, and an antioxidant stabilizer for polymers, among others .
L-Alanine- 15N,d4 is the deuterium and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4,allo-LCA-d4) is deuterium labeled Allolithocholic acid. Allolithocholic acid is a steroid acid could found in normal serum and feces. Allolithocholic acid facilitates excretion, absorption, and transport of fats and sterols in the intestine and liver .
Diethyl succinate- 13C4 is the 13C labeled Diethyl succinate . Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring .
4,5,6,7-Tetrabromoisobenzofuran-1,3-dione- 13C6 (Tetrabromophthalic anhydride- 13C6) is the 13C-labeled 4,5,6,7-Tetrabromoisobenzofuran-1,3-dione (HY-W010833).
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
4-Acetyl-N-methylaniline-13C,d3 (1-(4-(Methylamino)phenyl)ethanone-13C,d3) is a 13C and deuterated isotope of 4-Acetyl-N-methylaniline. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL .
Fibrinopeptide B, human-(Val- 13C5, 15N, Arg- 13C6, 154) TFA is the 13C- and 15N-labeled Fibrinopeptide B, human (HY-P1493). Fibrinopeptide B, human is a 14-aa peptide, released from the amino-terminus of β-chains of fibrinogen by thrombin .
4-(Bromomethyl)-2,2-dimethyl-1,3-dioxolane-d5 (5-bromomethyl-2,2-dimethyl-1,3-dioxolane-d5) is the deuterium labeled 4-(Bromomethyl)-2,2-dimethyl-1,3-dioxolane (HY-W018073).
(1R,2S,7R)-Sitafloxacin-d4 hydrochloride is deuterium labeled (1R,2S,7R)-Sitafloxacin hydrochloride (HY-B0395D). (R)-Sitafloxacin (DU-6857), a stereoisomer of Sitafloxacin (DU-6859a), is also an inhibitor of topoisomerases, with an IC50 of 0.18 μg/mL of DNA gyrase .
9α,11β-Prostaglandin F2α-d4 is a deuterated labeled 9α,11β-Prostaglandin F2α . 9α,11β-Prostaglandin F2α is an endogenous metabolite present in Urine that can be used for the research of Asthma .
β-Carotene- 13C10 (Provitamin A- 13C10) is the 13C-labeled β-Carotene (HY-N0411). β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities [4] .
Felbamate-d5 is the deuterium labeled Felbamate . Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .
DHEA-d5 (Prasterone-d5; Dehydroisoandrosterone-d5; Dehydroepiandrosterone-d5) is the deuterium labeled DHEA (HY-14650). DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
Selegiline-d5 (Deprenyl-d5) is deuterium labeled Selegiline. Selegiline (Deprenyl) is a potent, selective and irreversible inhibitor of MAO-B, with an IC50 of 51 nM. Selegiline exhibits 450-flod selectivity for MAO-B over MAO-A (IC50=23 μM). Selegiline can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .
Nirvanol-d5 (Ethylphenylhydantoin-d5) is deuterium labeled Nirvanol (HY-W012481) . Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
Selegiline-d5 (hydrochloride) (Deprenyl-d5 (hydrochloride)) is deuterium labeled Selegiline (hydrochloride). Selegiline (Deprenyl) hydrochloride is a potent, selective and irreversible inhibitor of MAO-B, with an IC50 of 51 nM. Selegiline hydrochloride exhibits 450-flod selectivity for MAO-B over MAO-A (IC50=23 μM). Selegiline hydrochloride can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder .
Oxypurinol- 13C, 15N2 is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
Zidovudine-d3 is the deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Stepronin-d5 (Prostenoglycine-d5; TTPG-d5; Tiase-d5) is the deuterium labeled Stepronin (HY-A0234). Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands .
Daunorubicin- 13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor [4] .
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride . Tolterodine hydrochloride is a potent muscarinic receptor antagonist .
Tetradecyltrimethylammonium-d29 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide) . Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure .
Tetradecyltrimethylammonium-d38 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide) . Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure .
Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
TDHL-d10 (Tergurid-d10; Terguride-d10; trans-Dihydrolisuride-d10) is the deuterium labeled TDHL (HY-12714). TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.
Picropodophyllin-d3 (AXL1717-d3; Picropodophyllotoxin-d3; PPP-d3) is the deuterium labeled Picropodophyllin (HY-15494). Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist .
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
Carazolol-d7 is the deuterium labeled Carazolol (HY-107327). Carazolol is a highly potent antagonist of β1/β2 adrenoceptor. Carazolol is also a potent, selective β3-adrenoceptor agonist. Carazolol can be used in the research of hypertension .
N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine . N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
Nitisinone-d3 (NTBC-d3) is deuterium labeled Nitisinone. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase(4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism [4].
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
Moricizine-d8 Hydrochloride is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period .
Demethoxycurcumin-d7 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin(Curcumin II), a major active curcuminoid, possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
Travoprost-d7 (Fluprostenol isopropyl ester-d7) is deuterium labeled Travoprost. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
4-[[(4-Fluorophenyl)imino]methyl]phenol- 13C6 (4-{(E)-[(4-Fluorophenyl)imino]methyl}phenol- 13C6) is the 13C-labeled 4-[[(4-Fluorophenyl)imino]methyl]phenol (HY-W014178).
13,14-Dihydro-15-keto Prostaglandin F2α-d4 (13,14-Dihydro-15-keto-PGF2α-d4) is a deuterated labeled 13,14-Dihydro-15-keto Prostaglandin F2α (HY-113208). 13,14-Dihydro-15-keto Prostaglandin F2α-d4 is an endogenous metabolite present in Blood that can be used for the research of Pregnancy .
D-Glucose- 13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
Zoledronic acid-d5 is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects .
Tacrolimus-d3 (FK506-d3) is deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Alpha-Estradiol-d2 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia .
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
D-Glucose-d22 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
Squalene-d6 (Super Squalene-d6) is a deuterium labeled Squalene. Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity .
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
(Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
Tapinarof-d5 (WBI-1001-d5) is deuterium labeled Tapinarof. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice .
D-Glucose-d77 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Tiagabine-d6 (NO050328-d6) is deuterium labeled Tiagabine. Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
D-Glucose-d is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Indocyanine green-d7 (Foxgreen-d7) is the deuterium labeled Indocyanine green (HY-D0711). Indocyanine green is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography .
Normetanephrine-d3 (hydrochloride) is the deuterium labeled Normetanephrine hydrochloride. Normetanephrine ((±)-Normetanephrine) hydrochloride is the O-methylated metabolite of norepinephrine (NE) .
Clomipramine-d6 (hydrochloride) is the deuterium labeled Clomipramine hydrochloride. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD) .
Vitamin D2-d6 is the deuterium labeled Vitamin D2. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D .
Sudan IV-d6 (Solvent Red 24-d6) is the deuterium labeled Sudan IV(HY-D0932). Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections [4].
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
1-Cyclohexanol-d11 is the deuterium labeled 1-Cyclohexanol (HY-Y1217). 1-Cyclohexanol (Hydroxycyclohexane) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Tucatinib-d6 (Irbinitinib-d6) is deuterium labeled Tucatinib. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM .
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
1-Cyclohexanol-d12 is the deuterium labeled 1-Cyclohexanol (HY-Y1217). 1-Cyclohexanol (Hydroxycyclohexane) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Umbelliferone-d5 (7-Hydroxycoumarin-d5) is the deuterium labeled Umbelliferone (HY-N0573 ). Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in chronic alcohol-fed rats .
Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
Aprepitant- 13C2,d2 (Major) (MK-0869- 13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
Venetoclax-d6 (ABT-199-d6) is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
5-Aminosalicylic acid-d7 (5-ASA-d7; Mesalamie-d7; Mesalazie-d7) is deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN) .
Nevirapine-d5 (BI-RG 587-d5) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM .
Cetrimonium-d9 (bromide) is the deuterium labeled Cetrimonium bromide . Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR . Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Urethane-d5 is the deuterium labeled Urethane. Urethane (Ethyl carbamate), the ethyl ester of carbamic acid, is a byproduct of fermentation found in various food products. Urethane has the ability to suppress bacterial, protozoal, sea urchin egg, and plant tissue growth in vitro .
Amisulpride-d5 is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis[4].Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
Triapine-d3 (3-AP-d3) is deuterium labeled Triapine. Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer.
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Cetrimonium-d33 bromide is the deuterium labeled Cetrimonium bromide . Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Valproic acid-d7 (sodium) is the deuterium labeled Valproic acid (sodium salt). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Cyclosporin A-d12 (Cyclosporine A-d12) is deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion .
Cefpodoxime proxetil-d7 (U-76-d7,252-d7; CS-807-d7) is the deuterium labeled Cefpodoxime Proxetil (HY-N7101). Cefpodoxime Proxetil is an orally active broad spectrum third-generation cephalosporin with potent antibacterial activity against both Gram-positive and Gram-negative bacteria including staphylococci, streptococci, Haemophilus influenzae, Neisseria gonorrhoeae, Escherichia coli, Klebsiella pnuemoniae, Citrobacter spp, and Proteus spp. Cefpodoxime Proxetil binds to penicillin binding proteins (PBPs), which inhibits peptidoglycan synthesis, finally results in interfering bacterial cell wall biosynthesis. Cefpodoxime Proxetil can be used against skin structure infections, acute otitis media, pharyngitis, tonsillitis, upper respiratory tract infection, urinary tract infections and sexually transmitted diseases [4] .
Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan . Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura .
Elvitegravir-d6 (GS-9137-d6) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively .
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively [4]. Vemurafenib induces cell autophagy .
Erlotinib-d6 hydrochloride a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM . Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [4].
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
N,N-Dimethylglycine-d3 (Dimethylglycine-d3) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) hydrochloride, a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine hydrochloride is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine hydrochloride has antidepressant-like and surfactant effects .
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
Pipamperone-d10 (Floropipamide-d10) dihydrochloride is a deuterated Pipamperone dihydrochloride (HY-100703A). Pipamperone dihydrochloride (Floropipamide dihydrochloride) is a butyrophenone derivative and high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0). Pipamperone dihydrochloride is also a low-affinity antagonist of D2 receptor (pKi=6.7). Pipamperone dihydrochloride affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone dihydrochloride is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease [4].
Deracoxib-d3 (SC 046-d3; SC 59046-d3) is the deuterium labeled Deracoxib (HY-17509). Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas.
Guaifenesin-d3 is the deuterium labeled Guaifenesin. Guaifenesin (Guaiacol glyceryl ether), a constituent of guaiac resin from the wood of Guajacum officinale Linné, is an expectorant. Guaifenesin can alleviate cough discomfortby increasing sputum volume and decreasing its viscosity, thereby promoting effective cough .
Erlotinib-d8 (CP-358774-d8) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells [4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
Vitamin D2-d3 (Ergocalciferol-d3) is the deuterium labeled vitamin D2 (HY-76542), where the C-6 and C-19 protons are replaced by deuterium. Vitamin D2 can be produced by plants and mushrooms in the presence of sunlight .
Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
Miglustat-d9 is the deuterium labeled Miglustat. Miglustat (N-Butyldeoxynojirimycin) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1) .
Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Nevirapine-d8 (BI-RG 587-d8) is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM .
Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90 . Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression .
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
Benznidazole-d7 (Benznidazol-d7; Ro 07-1051-d7; Ro 71051-d7) is the deuterium labeled Benznidazole (HY-B1548). Benznidazole (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease .
Dimethoxycurcumin-d6 is the deuterium labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin is a derivative of Curcumin that has anti-inflammatory and antioxidant activities .
N,N-Dimethylglycine-d6 (Dimethylglycine-d6) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) hydrochloride, a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine hydrochloride is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine hydrochloride has antidepressant-like and surfactant effects [4].
Cortodoxone-d2 is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone) .
Delafloxacin-d5 is deuterium labeled Delafloxacin. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia .
Cortodoxone-d7 (11-Deoxycortisol-d7) is a deuterium labeled Cortodoxone (HY-77839). Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates T cell proliferation and activation .
Acoltremon-d3 (WS-12-d3) is the deuterium labeled Acoltremon (HY-108449). Acoltremon is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research .
Binimetinib-d3 (MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM .
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Miglustat-d9 hydrochloride is the deuterium labeled Miglustat hydrochloride. Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1) .
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
Fulvestrant-d5 (ICI 182780-d5) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
5-Aminosalicylic Acid-d3 (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
Cromolyn-d5 (Cromoglycate-d5) is the deuterium labeled Cromolyn (HY-B1619). Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
N6-Threonylcarbamoyladenosine- 13C4, 15N (N6-(N-Threonylcarbonyl)adenosine- 13C4, 15N) is the 13C- and 15N-labeled N6-Threonylcarbamoyladenosine (HY-18398). N6 - Threonylcarbamoyladenosine is a common nucleosides, which can decorate and become tRNA .
Nortriptyline-d3 (hydrochloride) is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression .
Ligustrazine-d12 (Chuanxiongzine-d12) is deuterium labeled Ligustrazine. Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats [4].
Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production .
Diacerein-d6 is the deuterium labeled Diacerein . Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases .
Thiamphenicol-d3 is a deuterium labeled Thiamphenicol. Thiamphenicol, a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative, Gram-positive aerobic and anaerobic bacteria) .
Physcion-d3 (Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects .
Guanidine-d5 (hydrochloride) is the deuterium labeled Guanidine hydrochloride . Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins .
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy .
Antipyrine-d3 is the deuterium labeled Antipyrine. Antipyrine (Phenazone) is an antipyretic and analgesic. Antipyrine can be used as a probe agent for oxidative agent metabolism. Antipyrine has been widely used in assessment of hepatic oxidative capacity .
Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research [4] .
Acepromazine-d6 (maleate) (Acetopromazine-d6 (maleate)) is deuterium labeled Acepromazine (maleate). Acepromazine (Acetopromazine) maleate is a phenothiazine tranquilizer and is alpha-adrenoceptor antagonist [2.
Metamizole-d3 sodium is the deuterium labeled Metamizole sodium. Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole sodium is a cyclooxygenase-3 (COX-3) inhibitor .
Domperidone- 13C6 (R33812- 13C6) is 13C labeled Domperidone. Domperidone (R33812) is an orally active and selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine .
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation?cephalosporin antibiotic. Cephalexin kills?gram-positive?and some?gram-negative bacteria?by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of?pneumonia,?strep throat, and bacterial endocarditis, et al .
D-erythro-Sphingosine-13C2,d2 is a deuterated labeled D-erythro-Sphingosine . D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator [4] .
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
Halobetasol propionate-d5 (BMY-30056-d5) is deuterium labeled Halobetasol propionate (HY-B0878). Halobetasol propionate (BMY-30056) is a synthetic glucocorticoid corticosteroid. Halobetasol propionate exhibits anti-inflammatory, antipruritic, and vasoconstrictive properties. Halobetasol propionate can be used for the study of psoriasis .
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
Epiandrosterone-d5 (3β-Androsterone-d5; trans-Androsterone-d5; iso-Androsterone-d5) is the deuterium labeled Epiandrosterone (HY-I0352). Epiandrosterone is a steroid hormone. Epiandrosterone activates BKCa. Epiandrosterone inhibits glucose transport and insulin release. Epiandrosterone has weak androgenic activity [4].
2-Phenylethanol-d9 is the deuterium labeled 2-Phenylethanol . 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans . It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
2-Phenylethanol-d5 is the deuterium labeled 2-Phenylethanol . 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans . It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Matrine-d3 (Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) [4] .
Hydroxytyrosol-d5 (DOPET-d5) is the deuterium labeled Hydroxytyrosol (HY-N0570). Hydroxytyrosol is a phenol found in the olive oil. Hydroxytyrosol can alleviate oxidative stress and improve mitochondrial function, thereby exerting neuroprotective effects. Hydroxytyrosol can induce cancer cells apoptosis via inducing ROS production. Hydroxytyrosol shows antibacterial and antiviral effect. Hydroxytyrosol can be used for the researches of cancer, infection, inflammation, immunology, metabolic, neurological and cardiovascular disease, such as colon cancer, diabetes, Alzheimer's Disease and atherosclerosis [4] .
Riboflavin phosphate-d3 sodium (Riboflavine phosphate-d3 sodium; Riboflavin 5'-phosphate-d3 sodium; Riboflavine 5'-phosphate-d3 sodium) is the deuterium labeled Riboflavin phosphate sodium (HY-B0964). Riboflavin phosphate sodium (FMN-Na) is a derivative of Riboflavin (vitamin B2) which is an essential nutrient for animals. Riboflavin phosphate sodium can be used for the research of progressive keratoconus, corneal ectasia and irregular astigmatism . Riboflavine phosphate sodium is a very effective NAD+-recycling agent .
Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research .
Acetylcysteine-d3 is the deuterium labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities. In addition, Acetylcysteine is the most stable form of cysteine during drug delivery and can be used in disulfidptosis studies [4] .
L-Tryptophan- 15N2,d8 is the deuterium and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
2,2-Dimethyl-1,3-dioxolane-4-methanol- 13C3 ((2,2-Dimethyl-[1,3] dioxane-4-yl)-methanol- 13C3) is the 13C-labeled 2,2-Dimethyl-1,3-dioxolane-4-methanol (HY-Y1372).
(R)-Pyrrolidine-2-carboxylic acid-d3 is the deuterium labeled (R)-pyrrolidine-2-carboxylic acid. (R)-pyrrolidine-2-carboxylic acid is an endogenous metabolite.
Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively [4].
Lamotrigine- 13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
Citicoline-d9 (Cytidine diphosphate-choline-d9) sodium is the deuterium labeled Citicoline sodium (HY-B0739A). Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study [4].
Cefditoren Pivoxil-d3 (Cefditoren pivoxyl-d3) is deuterium labeled Cefditoren Pivoxil. Cefditoren Pivoxil (ME 1207) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren Pivoxil has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren Pivoxil can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections .
D-Alanine-d7 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Propylthiouracil-d5 is the deuterium labeled Propylthiouracil. Propylthiouracil (6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor.
Cabazitaxel-d6 is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity .
Cabazitaxel-d9 is deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .
Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
D-Alanine-d3 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Glurate-d5 (4-Acetylbutyric acid-d5; 5-Oxohexanoic acid-d5; NSC-5281-d5) is the deuterium labeled Glurate (HY-W001957). Glurate (4-Acetylbutyric acid) is an acylating agent. Glurate can be used in the development of antiviral compounds, especially those targeting retroviruses such as herpes virus and HIV. Glurate can be used in the synthesis of acyclic nucleoside derivatives and 5-hydroxyhexanoic acid .
D-Alanine-d is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR .
Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses .
N-Acetyl-5-hydroxytryptamine-d3 is the deuterium labeled N-Acetyl-5-hydroxytryptamine. N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor .
Raloxifene-d10-1 is the deuterium labeled Raloxifene . Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) is the deuterated product of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research .
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
Benzoin-d10 (DL-Benzoin-d10) is the deuterium labeled Benzoin (HY-B1550). Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
5α-Cholestan-3β-ol-d7 (Dihydrocholesterol-d7; 5α-Cholestanol-d7; NSC 18188-d7) is the deuterium labeled 5α-Cholestan-3β-ol (HY-107819). 5α-Cholestan-3β-ol is a derivitized steroid compound.
Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Cefotaxime-d3 is the deuterium labeled Cefotaxime (HY-A0088A). Cefotaxime is the β-lactamase stable cephalosporin and the third-generation cephalosporin antibiotic. Cefotaxime possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria [4] .
L-Tryptophan-d8 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
Hexadecane-d34 (n-Hexadecane-d34) is the deuterium labeled Hexadecane (HY-W099580). Hexadecane (n-Hexadecane) is a saturated hydrocarbon of alkanes or paraffins and can be used as an organic solvent. Hexadecane is a component of petroleum, belongs to hydrophobic substrates, and is a model substance for studying bacterial degradation of hydrophobic compounds .
Rifampicin-d8 (Rifampin-d8) is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Tricaprilin-d50 (Trioctanoin-d50) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
Florfenicol-d3 ((-)-Florfenicol-d3)?is the deuterium labeled Florfenicol. Florfenicol, a commonly used veterinary antibiotic, is currently indicated for bovine respiratory disease, and also used in aquaculture for the control of enteric septicemia in catfish. Florfenicol can induce early embryonic death in eggs, with an LC50 of 1.07 μg/g.
Oxaprozin-d5 is deuterium labeled Oxaprozin. Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
Pyrazinamide-d3 is deuterium labeled Pyrazinamide. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis .
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .
Aspirin-d3 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis [4] .
Salbutamol-d3 (Albuterol-d3) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease .
D-Mannitol-d8 is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Tricaprilin-d15 (Trioctanoin-d15) is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
Esomeprazole-d3 potassium is deuterated labeled Esomeprazole (HY-17021). Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
L-Tryptophan-d3 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
Dexamethasone-d5 is the deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses .
Bisdemethoxycurcumin-d8 (Curcumin III-d8) is the deuterium labeled Bisdemethoxycurcumin (HY-N0007A). Bisdemethoxycucurmin (Curcumin III) is a curcuminoid compound and an inhibitor of P-glycoprotein and ferroptosis. Bisdemethoxycucurmin exhibits multiple activities such as anti-oxidation, anti-inflammation and anti-tumor.
Bisdemethoxycucurmin can be used for the research of tumors and inflammatory diseases [4] .
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine . Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .
Esomeprazole-d3 is deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
Estrone-d2 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human?DNA topoisomerase I?and?topoisomerase II?inhibitor with?IC50s of 0.8 μM and 2.67 μM, respectively.
Rifampicin-d3 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities .
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
D-Mannitol-d2 is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Piperin-d10 is deuterium labeled Piperine. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL [4].
Omadacycline-d9 (PTK 0796-d9; Amadacycline-d9) is the deuterium labeled Omadacycline (HY-14865) that can be used as the internal standard for the analysis of Omadacycline .
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
Glycochenodeoxycholic acid-d7 (sodium) is the deuterium labeled Glycochenodeoxycholic acid (sodium salt). Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) induces hepatocyte apoptosis .
Altrenogest-d5 is the deuterium labeled Altrenogest. Altrenogest (Allyltrenbolone) is a progestogen structurally related to veterinary steroid trenbolone.
Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
Stearoylethanolamide-d3 (Ceamid-d3) is deuterium labeled Stearoylethanolamide. Stearoylethanolamide is an endocannabinoid-like compound with pro-apoptotic activity .
Atomoxetine-d7 (Tomoxetine-d7) is deuterium labeled Atomoxetine. Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na + channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research .
(-)-Ketoconazole-d3 is deuterium labeled (-)-Ketoconazole. (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Sucralose-d6 is deuterium labeled Sucralose. Sucralose?(E955; Trichlorosucrose) is a?non-nutritive?artificial?sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents .
Spermine-d20 (NSC 268508-d20) is deuterium labeled Spermine. Spermine (NSC 268508) functions directly as a free radical scabenger to protect DNA from free radical attack. Spermine has antiviral effects .
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
Oxaprozin-d10 (Oxaprozinum-d10; Wy21743-d10) is the deuterium labeled Oxaprozin (HY-B0808). Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity [4]. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
Tofacitinib-d3 (Tasocitinib-d3) is deuterium labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
Rifabutin-d7 is the deuterium labeled Rifabutin. Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.
Nicotinamide-d3 (Niacinamide-d3) is deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity [4].
Salbutamol-d9 (Albuterol-d9) acetate is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease .
Thymidine-d3 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication .
(±)-Penbutolol-d9 (hydrochloride) is a deuterium labeled (±)-Penbutolol hydrochloride. (+)-Penbutolol hydrochloride is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM .
Cefotaxime-d3 (sodium) is the deuterium labeled Cefotaxime (sodium salt). Cefotaxime sodium salt, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria [4] .
L-Tryptophan-d5 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
Rifampicin-d11 (Rifampin-d11; Rifamycin AMP-d11) is the deuterium labeled Rifampicin (HY-B0272) . Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities. Rifampicin shows anti-orthopoxvirus activity .
Mecillinam-d12 is deuterium labeled Mecillinam. Mecillinam (Amdinocillin), the β-lactam antibiotic, has a broad spectrum of activity against gram-negative organisms .
Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Salbutamol-d9 (Albuterol-d9) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease .
Guanosine-d13 (DL-Guanosine-d13) is a deuterium of Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor .
Mitoxantrone-d8 (hydrochloride) (Mitozantrone-d8 (hydrochloride)) is deuterium labeled Mitoxantrone (dihydrochloride). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity [4]. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
Meldonium-d3 is the deuterated form of Meldonium. Meldonium is a cardiovascular protective agent that competitively inhibits BBOX1 and OCTN2. The IC50 value of Mildronate against human recombinant BBOX is 34-62 μM, and the EC50 value against human OCTN2 is 21 μM. Meldonium is a fatty acid oxidation inhibitor .
Cisapride-d6 (R51619-d6) is deuterium labeled Cisapride. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity [4] .
Nateglinide-d5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (?Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling .
Ritonavir-d8 is deuterated labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM.
Atomoxetine-d5 (Tomoxetine-d5) is deuterium labeled Atomoxetine. Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na + channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research .
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone . DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling .
Thymidine-d14 (DThyd-d14; NSC 21548-d14) is deuterium labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM .
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Formamide-d3 is the deuterium labeled Formamide (HY-Y0842). Formamide is an effective DNA denaturant that significantly reduces the stability of DNA in buffer solutions. Formamide can also be used as a decalcifying agent for rat cardiac cells. Additionally, formamide is widely used as a solvent or chemical raw material for ion compounds, resins, and plasticizers. [4]
D-Mannitol-d is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
Imidaprilate-d5 is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
Esomeprazole-d3 (sodium) is the deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research .
Pizotyline-d3 is deuterated labeled Pizotifen (HY-B0115). Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
Theophylline- 13C2,d6 (1,3-Dimethylxanthine- 13C2,d6) is the deuterium labeled and 13C-labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research [4] .
D-Glucose-d12-12 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
D-Glucose-d1-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Estradiol-d3 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
D-Glucose-d-33 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Methyl acetylacetate-d3 (Acetoacetate methyl ester-d3) is a deuterium labeled Methyl acetylacetate (HY-Y1298). Methyl acetylacetate is an endogenous metabolite .
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
Liothyronine-d3 is deuterated labeled Liothyronine (HY-A0070A). Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively .
Vincristine-d3 (sulfate)is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM .
Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
Vincristine-d6 (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
D-Glucose-d2-1 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidinesynthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs .
Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [4] .
Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
Doxifluridine-d2 is the deuterium labeled Doxifluridine . Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
Estradiol-d2 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
Vincristine-d3-ester (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM .
D-Glucose-d2-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
D-Glucose-d-11 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
Verapamil-d3 ((±)-Verapamil-d3) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
Adenosine-d13 (Adenine riboside-d13; D-Adenosine-d13) is deuterium labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
Duloxetine-d3 (hydrochloride) is a deuterium labeled Duloxetine hydrochloride. Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
Entecavir-d2 is the deuterium labeled Entecavir. Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
D-Sorbitol-d8 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement .
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
(±)-Leucine-d10 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08% .
Neohesperidin Dihydrochalcone-d3 (Neohesperidin DC-d3; NHDC-d3) is the deuterium labeled Neohesperidin dihydrochalcone (HY-N0154). Neohesperidin dihydrochalcone is a synthetic glycoside chalcone, is added to various foods and beverages as a low caloric artificial sweetener.
L-Carnitine-d9 (chloride)e is the deuterium labeled L-Carnitine chloride. L-Carnitine chloride, a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine chloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine chloride is an antioxidant. L-Carnitine chloride can ameliorate metabolic imbalances in many inborn errors of metabolism .
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Azeliragon-d9 (TTP488-d9) is the deuterium labeled Azeliragon (HY-50682). Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression with mild Alzheimer’s disease (AD) . Azeliragon also can cross the blood-brain barrier (BBB) .
Amantadine-d15 is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent .
L-Serine-d3 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Pantoprazole-d8 (BY1023-d8) sodium is a deuterium labeled Pantoprazole (HY-17507). Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Iopamidol-d3 (B-15000-d3; SQ-13396-d3) is the deuterium labeled Iopamidol (HY-B0684). Iopamidol is a nonionic, X-Ray iodinated contrast agent (CA) for a wide variety of diagnostic applications. Iopamidol contains amide and hydroxyl functionalities that can be exploited for the generation of the chemical exchange saturation transfer (CEST) contrast .
Dalbavancin-d6 is the deuterium labeled Dalbavancin . Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively .
Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy [4] .
Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
Mifepristone-d3 is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
Levosulpiride-d3 is the deuterium labeled Levosulpiride. Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class .
Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Tulathromycin A-d7 (Tulathromycin-d7) is deuterium labeled Tulathromycin A. Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 μM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects [4].
Molindone-d8 is the deuterium labeled Molindone. Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses .
Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
Etoricoxib-d3 is the deuterium labeled Etoricoxib . Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood [4].
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect .
Mirtazapine-d3 is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors .
Febuxostat-d3 (TEI 6720-d3) is deuterium labeled Febuxostat. Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout .
Amantadine-d6 is the deuterium labeled Amantadine . Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research [4] .
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Fluralaner-d3 (A1443-d3) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
(±)-Leucine-d7 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08% .
Lifitegrast-d6 (SAR 1118-d6) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Levodropropizine-d8 is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
Docosahexaenoic acid-d5 is the deuterium labeled Docosahexaenoic Acid. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
Dioxybenzone-d3 is deuterium labeled Dioxybenzone. Dioxybenzone (Benzophenone-8; UV-24) is an organic compound used to block UVB and short-wave UVA (ultraviolet) radiation. Dioxybenzone has orally activity. Dioxybenzone exhibits estrogenic disrupting effect. Dioxybenzone up-regulates inflammatory cytokines. Dioxybenzone can be used for cancer, reproductive system disease and inflammatory disease study [4].
Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
Cyclopropylcarboxylic acid-d5 (Carboxycyclopropane-d5) is a deuterium labeled Cyclopropylcarboxylic acid (HY-Y0001). Cyclopropylcarboxylic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Irbesartan-d7 is deuterated labeled Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM .
Fluralaner-d2 (A1443-d2) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Secnidazole-d3 (RP-14539-d3; PM-185184-d3) is the deuterium labeled Secnidazole (HY-B1118). Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
Pantoprazole-d8 (BY1023-d8) is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI) . Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142) [4].
Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
N-Benzylaniline-d2 (N-Phenylbenzylamine-d2) is the deuterium labeled N-Benzylaniline (HY-W016321). N-Benzylaniline is an N-alkyl-ated derivative of aniline .
Metopimazine-d6 (EXP999-d6; RP9965-d6) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks [4].
Molnupiravir-d7 is the deuterium labeled Molnupiravir. Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza .
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively .
Octacosane-d58 is the deuterium labeled Octacosane . Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l [4].
Fexofenadine-d10 (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years) .
Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .
Pocapavir-d3 (SCH-48973-d3; V-073-d3) is the deuterium labeled Pocapavir (HY-104074) . Pocapavir (SCH-48973) is an orally active capsid inhibitor. Pocapavir prevents virion uncoating upon entry into the cell. Pocapavir has antiviral activity against polioviruses. Pocapavir also inhibits enterovirus infections .
D-Sorbitol-d2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Pergolide-d7 (mesylate) is the deuterium labeled Pergolide mesylate. Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research .
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research .
Revefenacin-d9 (TD-4208-d9) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Revefenacin-d3 (TD-4208-d3) is deuterium labeled Revefenacin. Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Ondansetron-d6 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride . Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy [4] .
Chlorambucil-d8 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease [4].
Olaparib-d5 (AZD2281-d5) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [4].
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay [4] . Boceprevir inhibits SARS-CoV-2 3CLpro activity .
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
Fexofenadine-d3 is the deuterium labeled Fexofenadine . Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research [4].
Adenosine-d9 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio .
Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively .
Phenylglyoxylic acid-d5 (Benzoylformic acid-d5) sodium is the deuterium labeled Phenylglyoxylic acid sodium (HY-W010255A). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human. Phenylglyoxylic acid can be used as drug intermediate for synthesis of antineoplastic compounds .
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo [4].
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
Fluralaner-d5 (A1443-d5) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels .
Mavacamten-d7 (MYK461-d7) is deuterium labeled Mavacamten. Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Naftopidil-d7 (KT-611-d7 ) is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Elobixibat-d5 is the deuterium labeled Elobixibat (HY-15790). Elobixibat (A 3309; AZD 7806) is orally active, bile acid transporter (IBAT) inhibitor with IC50 values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to treat metabolic syndrome. Elobixibat can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly [4].
Dacomitinib-d10 dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively .
Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women .
Cephalexin-d5 (monohydrate) is the deuterium labeled Cephalexin monohydrate. Cephalexin monohydrate is a potent, orally active and the first-generation?cephalosporin antibiotic. Cephalexin monohydrate kills?gram-positive?and some?gram-negative bacteria?by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of?pneumonia,?strep throat, and bacterial endocarditis, et al .
Tivozanib-d6 (AV-951-d6) is deuterium labeled Tivozanib. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors .
Brequinar-d3 (DUP785-d3) is deuterium labeled Brequinar. Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity .
Midostaurin-d5 (PKC412-d5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM .
Actinine-d9 chloride is the deuterium labeled Actinine chloride. Actinine chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat .
6-Mercaptopurine-d2 is the deuterium labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent .
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
Verapamil-d6 ((±)-Verapamil-d6) is deuterium labeled Verapamil. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
Cyclamic acid-d11 (Sodium cyclamate-d11) sodiumis deuterium labeled Cyclamic acid (sodium). Cyclamic acid sodium (Sodium cyclamate) is a commonly used sweetener. Cyclamic acid sodium is toxic to osteoblasts and can inhibit cell proliferation, induce apoptosis and reduce cell mineralization. Cyclamic acid sodium causes focal necrosis of bladder organs in rats in vitro, which can promote bladder cancer, but some studies have shown that low doses of Cyclamic acid sodium have no carcinogenic effect. In addition, Cyclamic acid sodium has no effect on insulin and glucagon secretion induced by arginine [4] .
Undecanoic acid-d2 (Undecanoate-d2) is the deuterium labeled Undecanoic acid (HY-W004282). Undecanoic acid is a monocarboxylic acid with antifungal property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Aldox-d6 (Lexamine M-13-d6; MAPD-d6) is the deuterium labeled Myristamidopropyl dimethylamine (HY-W099582). Myristamidopropyl dimethylamine (MAPD) is an antimicrobial agent (including against bacteria and fungi) and an insecticide, exhibiting inhibitory activity against Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Fusarium solani, and Acanthamoeba polyphaga. Myristamidopropyl dimethylamine can be used in research on microbial-induced keratitis .
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive . Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Lubiprostone-d7 (RU-0211-d7) is the deuterium labeled Lubiprostone. Lubiprostone (SPI-0211) increases intestinal fluid secretion through generation of CIC-2/CFTR and activation of cAMP signaling pathway. Lubiprostone inhibits myeloperoxidase (MPO) activity, downregulates Indomethacin (HY-14397)-induced iNOS and TNFα expression. Lubiprostone can be used for chronic constipation research .
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
Duloxetine-d7 hydrochloride ((S)-Duloxetine-d7 hydrochloride) is the deuterium labeled Duloxetine hydrochloride (HY-B0161A). Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
N-Desmethyl clomipramine-d7 (Desmethylclomipramine-d7) is deuterium labeled N-Desmethyl clomipramine. Desmethylclomipramine (Norclomipramine) is a metabolite of Clomipramine (HY-B0457A) and can be used for neurological research .
Cefetamet-d3 (Ro 15-8074-d3; Deacetoxycefotaxime-d3) is the deuterium labeled Cefetamet (HY-A0111). Cefetamet (Ro 15-8074) is a cephalosporin antibiotic and the active metabolite of Cefetamet pivoxil (HY-B1894A). Cefetamet binds to bacterial penicillin-binding protein (PBP) (IC50 for PBP3 in Escherichia coli W3110 is 2.5 μg/mL). Cefetamet has significant activity against Gram-negative bacteria such as Enterobacteriaceae, Neisseria species, and Haemophilus influenzae, as well as Gram-positive bacteria such as Streptococcus. Cefetamet kills and lyses Treponema pallidum. Cefetamet can be used in the research of respiratory tract, urinary tract, ear, nose and throat infections, and syphilis [4] .
Oleanolic acid-d3 is the deuterium labeled Oleanolic Acid . Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities .
Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Resiquimod-d5 is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α .
Citronellol-d6 is deuterated labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis [4] .
Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy [4] .
Levodropropizine-d5 ((S)-(-)-Dropropizine-d5) is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
Fusidic acid-d6 is the deuterium labeled Fusidic acid. Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome .
Beraprost-d3 (TRK-100-d3) is deuterium labeled (Rac)-Beraprost. (Rac)-Beraprost ((Rac)-ML 1229) is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
L-Serine-d2 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively .
Irbesartan-d7 hydrochloride is deuterated labeled Irbesartan hydrochloride (HY-B0202A). Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Pregnanediol-d5 is the deuterium labeled Pregnanediol. Pregnanediol is the major metabolite of progesterone and can be excreted via urine. Pregnanediol offers an indirect way to measure progesterone levels in vivo .
Rucaparib-d8 (AG014699-d8 ) is deuterium labeled Rucaparib. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research [4].
Danegaptide-d5 (GAP-134-d5) is deuterium labeled Danegaptide. Danegaptide (GAP-134) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect .
Belumosudil-d7 (KD025-d7) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
Febuxostat-d5 (TEI 6720-d5) is deuterium labeled Febuxostat. Febuxostat (TEI 6720) is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat has the potential for the research of hyperuricemia and gout .
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
Cibenzoline-d5 (Cifenline-d5) is deuterium labeled Cibenzoline. Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a KATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC50 of 22.2 μM. Cibenzoline inhibits IKr and IKs currents with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia [4].
S-(+)-Ketoprofen-d3 ((S)-Ketoprofen-d3) is deuterium labeled S-(+)-Ketoprofen. S-(+)-Ketoprofen is a potent inhibitor of both COX-1 and COX-2 with IC50s of 1.9 and 27 nM, respectively.
Sparfloxacin-d5 is deuterium labeled Sparfloxacin (HY-B0308). Sparfloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity .
Methylmalonic acid-d3 is the deuterium labeled Methylmalonic acid. Methylmalonic acid (Methylmalonate) is an indicator of Vitamin B-12 deficiency in cancer .
Olaparib-d8 (AZD2281-d8) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [4].
Lamotrigine-d3 is the deuterium labeled Lamotrigine . Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors .Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Verapamil-d6 (CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research .
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride . Pyridoxine hydrochloride (Pyridoxol;Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol;Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway .
Brincidofovir-d6 (CMX001-d6) is the deuterium labeled Brincidofovir (HY-14532). Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. [4].
Verapamil-d7 is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research .
Pyridoxine-d2 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Safinamide-d5 (FCE 26743-d5) is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Undecanoic acid-d3 (Undecanoate-d3) is the deuterium labeled Undecanoic acid (HY-W004282). Undecanoic acid is a monocarboxylic acid with antifungal property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Albendazole sulfoxide-d7 is the deuterium labeled Albendazole sulfoxide. Albendazole sulfoxide (Ricobendazole), the main active metabolite of Albendazole, exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes .
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor .
Undecanoic acid-d21 (Undecanoate-d21) is the deuterium labeled Undecanoic acid (HY-W004282). Undecanoic acid is a monocarboxylic acid with antifungal property. Undecanoic acid inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum .
Aficamten-d3 (CK-274-d3) is deuterium labeled Aficamten. Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM) .
Dorzolamide-d3 hydrochloride is deuterated labeled Dorzolamide hydrochloride (HY-B0109A). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
L-Serine-d7 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Lapatinib-d7 (GW572016-d7) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
N-Desmethyl clomipramine-d6 (Desmethylclomipramine-d6) is deuterium labeled N-Desmethyl clomipramine. Desmethylclomipramine (Norclomipramine) is a metabolite of Clomipramine (HY-B0457A) and can be used for neurological research .
Pyridoxine-d3 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
Orlistat-d3 is a deuterated labeled Orlistat . Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity .?Anti-atherosclerotic?effect .
Diatrizoic acid-d6 (Diatrizoate-d6; Amidotrizoic acid-d6) is the deuterium labeled Diatrizoic acid (HY-B0926). Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium .
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations .
L-Carnitine-d9 is the deuterium labeled L-Carnitine. L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism .
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
Mavacamten-d5 (MYK461-d5; SAR439152-d5) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma .
Baloxavir-d5 is deuterium labeled Baloxavir. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity .
Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
Quizartinib-d8 (AC220-d8) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
Ribavirin- 15N, d2 is 15N and deuterated labeled Ribavirin (HY-B0434). Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.
Tildacerfont-d8 (SPR001-d8) is a deuterium labeled Tildacerfont (HY-113603). Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia .
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
2'-Deoxycytidine-5'-monophosphoric acid- 15N3,d12 dilithium is deuterium and 15N labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator [4].
Ibudilast-d7-1 is the deuterium labeled Ibudilast . Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia .
Crystal Violet-d6 is the deuterium labeled Crystal Violet (HY-B0324A). Crystal Violet, also known as Gentian violet, methyl violet 10B, is a triphenyl-methane, an alkaline dye that binds to DNA in the nucleus of a cell, staining it a deep purple. It is often used for Gram staining to classify bacteria, or for cell or histological staining .
Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway [4].
Hexacosanoic acid methyl ester-d3 (C26:0 methyl ester-d3) is deuterium labeled Methyl hexacosanoate. Methyl hexacosanoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
C6 Ceramide- 13C2,d2 (C6-Cer- 13C2,d2) is the deuterium labeled and 13C-labeled C6 Ceramide (HY-19542). C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects [4] .
N-(1-(Adamantan-1-yl)ethyl)hydroxylamine-d4(N-(1-((3r,5r,7r)-Adamantan-1-yl)ethyl)hydroxylamine-d4) is the deuterium labeled N-(1-(adamantan-1-yl)ethyl)hydroxylamine (HY-75864).
Zoledronic acid- 15N2, 13C2 (CGP 42446- 15N2, 13C2) is the 13C- and 15N-labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects .
Cladribine- 13C5, 15N2 (2-Chloro-2′-deoxyadenosine- 13C5, 15N2) is 13C and 15N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis .
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 μM and 2.6 μM, respectively .
(S)-Malic acid-d3 is the deuterium labeled (S)-Malic acid. (S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a dicarboxylic acid in naturally occurring form, contributes to the pleasantly sour taste of fruits and is used as a food additive .
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia .
Cisapride- 13C,d3 (R 51619- 13C,d3) is the deuteriumand 13C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity [4].
Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system .
Omeprazole metabolite Omeprazole sulfone-d3 is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Deoxycholic acid-d6 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
Betulinic acid-d3 (Lupatic acid-d3) is a deuterium labeled Betulinic acid (HY-10529). Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties [4].
Ethyl linoleate-d2 (Linoleic Acid ethyl ester-d2; Mandenol-d2) is the deuterium labeled Ethyl linoleate (HY-W013812). Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Malic acid-d3 is the deuterium labeled Malic acid. Malic acid (Hydroxybutanedioic acid) is a dicarboxylic acid that is naturally found in fruits such as apples and pears. It plays a role in many sour or tart foods .
Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
Labetalol hydrochloride-d6 (AH-5158 hydrochloride-d6) is deuterium labeled Labetalol hydrochloride (HY-B1108). Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy [4].
Vinorelbine-d3 (ditartrate) is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
Butylphthalide-d3 is the deuterium labeled Butylphthalide. Butylphthalide(3-n-Butylphthalide), an anti-cerebral-ischemia agent, is first isolated from the seeds of celery and showes efficacy in animal models of stroke.
Herniarin-d3 is the deuterium labeled Herniarin (HY-N1366). Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
Rivastigmine-d3 hydrochloride is deuterated labeled Rivastigmine (HY-17368). Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
Prostaglandin E1-d9 is deuterium labeled Prostaglandin E1.Prostaglandin E1 is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inh
Thiamine-d3 (hydrochloride) is the deuterium labeled Thiamine hydrochloride. Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
Ethyl linoleate-d11 (Linoleic Acid ethyl ester-d11) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Alvimopan-d7 (ADL 8-2698-d7) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
2'-Hydroxyacetophenone-d7 (o-Hydroxyacetophenone-d7; o-Acetylphenol-d7) is the deuterium labeled 2'-Hydroxyacetophenone (HY-Y1426). 2'-Hydroxyacetophenone is found in alcoholic beverages. 2'-Hydroxyacetophenone is present in tomato, cassia, fried beef, rum, whiskey, cocoa, coffee and black tea. 2'-Hydroxyacetophenone is a flavouring ingredient. Building block in chemical synthesis.
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research [4] .
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity .
Prostaglandin E2-d9 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
Phenylacetylglutamine-d5 (NSC 203800-d5) is the deuterium labeled Phenylacetylglutamine (HY-W050026). Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation .
Ethylparaben-d5 (Ethyl parahydroxybenzoate-d5) is deuterium labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Cabotegravir-d3 (sodium) is the deuterium labeled Cabotegravir sodium. Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltr
Enrofloxacin-d5 is the deuterium labeled Enrofloxacin. Enrofloxacin (BAY Vp 2674) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Valproic acid-d15 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity .
PF-06380101-d8 (Aur0101-d8) is a deuterium labeled PF-06380101 (HY-12522). PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue .
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease .
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor . Antianginal agent.
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice [4].
Dimebutic acid-d6 (NSC-16045-d6; NSC-741804-d6) is the deuterium labeled Dimebutic acid (HY-W015881). Dimebutic acid is a fatty acid derivative. Dimebutic acid is an orally active short-chain fatty acid. Dimebutic acid stimulates fetal globin production and alters the balance of Bcl family proteins. Dimebutic acid prolongs red blood cell survival. Dimebutic acid exhibits toxicity in rats. Dimebutic acid is used in the study of β-thalassemia and sickle cell disease .
Topotecan-d5 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87 .
Tamsulosin-d5 (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .
N-Acetylglycine-d2 (Aceturic acid-d2) is the deuterated labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity .
Chloroxylenol-d6 is the deuterium labeled Chloroxylenol. Chloroxylenol is a broad spectrum antimicrobial chemical compound used to control bacteria, algae, fungi and virus.
Adenine-d is the deuterium labeled Adenine. Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis .
Taurocholic acid-d8 (sodium) is deuterium labeled Taurocholic acid (sodium). Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect .
Butylphthalide-d9 (3-n-Butylphthalide-d9) is deuterium labeled Butylphthalide. Butylphthalide (3-n-Butylphthalide) is an active molecule against cerebral ischemia. It was originally isolated from celery species and has been shown to be effective in stroke animal models .
Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
Digitoxigenin-21,23,23-d3 (Cerberigenin-d3; Echujetin-d3) is the deuterium labeled Digitoxigenin (HY-B2151). Digitoxigenin is a steroid derivative commonly found in various plants, especially the foxglove plant (Digitalis purpurea). Digitoxigenin has unique chemical properties that make it an important precursor for the synthesis of cardiac glycosides, a group of drugs used to improve heart failure and certain types of arrhythmias. It works by inhibiting the sodium potassium ATPase pump, thereby increasing the force and efficiency of cardiac contractions.
Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs . Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs) .
Dexamethasone acetate-d5 (Dexamethasone 21-acetate-d5; Hexadecadrol acetate-d5) is the deuterium labeled Dexamethasone acetate (HY-14648A). Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively [4].
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
N-Acetylglycine-d5 (Aceturic acid-d5) is the deuterium labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
Enrofloxacin-d5 (hydrochloride) is deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Thiabendazole-d6 is a deuterated labeled Thiabendazole (HY-B0263). Thiabendazole is an orally available benzimidazole fungicide with repellent and anticancer activities. Thiabendazole can result in developmental malformations. Thiabendazole can be used for modeling [4] .
3-Methylanisole-d3 is the deuterium labeled 3-Methylanisole (HY-115127) .3-Methylanisole is an intermediate in drug synthesis, which has antiseptic, antibacterial and protein stabilizing effects .
Ulipristal-d3 (CDB-3236-d3) is deuterium labeled Ulipristal. Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system .
Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
Lomefloxacin-d5 (hydrochloride) is the deuterium labeled Lomefloxacin hydrochloride. Lomefloxacin (SC47111A) hydrochloride is a broad-spectrum quinolone antibiotic, with antimicrobial activity. Lomefloxacin hydrochloride is used for the research of respiratory tract infections, genitourinary infections, gastrointestinal infections, ENT infections, etc. .
Vildagliptin-d6 (LAF237-d6 ) is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
Riboflavin-d3 is the deuterium labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases [4] .
N-Desmethylolanzapine-d8 hydrochloride (N-Demethylolanzapine-d8 hydrochloride) is the deuterium labeled N-Desmethylolanzapine (HY-W009247). N-Desmethylolanzapine is an antipsychotic drug. The formation of N-Desmethylolanzapine correlates with the level and activity of human liver flavin-containing monooxygenase (FMO3). N-Desmethylolanzapine can be used in the study of antipsychotic drugs .
Riboflavin-d8 (Vitamin B2-d8 ) is deuterium labeled Riboflavin. Riboflavin, an orally active and easily absorbed micronutrient, is a precursor of flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD), which serve as coenzymes for numerous enzymatic reactions and perform key metabolic functions by mediating the transfer of electrons in biological oxidation-reduction reaction .
N-Desmethyl Clomipramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine
Thiamphenicol-d3-1 (Thiophenicol-d3-1; Dextrosulphenidol-d3-1) is the deuterium-labeled Thiamphenicol (HY-B0479) . Thiamphenicol (Thiophenicol)，a methyl-sulfonyl derivative of Chloramphenicol，is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit，leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative，Gram-positive aerobic and anaerobic bacteria) .
Propylparaben-d7 (Propyl parahydroxybenzoate-d7) is the deuterium labeled Propylparaben (HY-N2026) . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats [4].
Sofosbuvir-d6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Taurine- 15N (2-Aminoethanesulfonic acid- 15N) is 15N labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
Cytidine-5'-triphosphate- 15N3,d14 (Cytidine triphosphate- 15N3,d14 dilithium; 5'-CTP- 15N3,d14) dilithium is deuterium and 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
Thymidine- 13C10, 15N2 is the 13C and 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Deoxycytidine triphosphate- 15N3,d14 (dCTP- 15N3,d14 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3,d14) dilithium is deuterium and 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
(±)-1,2-Propanediol-d2 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
(±)-1,2-Propanediol-d8 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) methylbenzenesulfonate is the deuterium labeled S-Adenosyl-L-methionine methylbenzenesulfonate . S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research [4].
Menaquinone-7-d7 is the deuterium labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors . Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS) .
Naloxegol- 13C,d2 (NKTR-118- 13C,d2) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
6-Aminocaproic acid-d10 hydrochloride (EACA-d10 hydrochloride; Epsilon-Amino-n-caproic Acid-d10 hydrochloride; 6-Aminohexanoic acid-d10 hydrochloride) is the deuterium labeled 6-Aminocaproic acid hydrochloride (HY-B0236A). 6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
Hydrocinnamic acid-d9 is the deuterium labeled Hydrocinnamic acid . Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activitie s.
Naloxegol- 13C,d3 (NKTR-118- 13C,d3) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders .
Hydrocinnamic acid-d5 is the deuterium labeled Hydrocinnamic acid . Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities .
(±)-1,2-Propanediol-d6 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
L-Tryptophan- 13C11, 15N2 is the 13C- and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
5'-Guanylic acid- 15N5,d12 (5'-GMP- 15N5,d12 dilithium; 5'-guanosine monophosphate- 15N5,d12) dilithium is deuterium and 15N labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Kevetrin (hydrochloride)- 13C2, 15N3 is the 13C-labeled and 15N-labeled Kevetrin (hydrochloride). Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
Guanosine- 13C10, 15N5 is the 13C and 15N labeled Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Cytidine 5′-monophosphate- 15N3,d12 (5'-Cytidylic acid- 15N3,d12 dilithium; 5'-CMP- 15N3,d12) dilithium is deuterium and 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects .
Coenzyme Q10-d9 is the deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Diethyltoluamide-d7 is the deuterium labeled Diethyltoluamide . Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects .
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
(22R)-Budesonide-d6 (Dexbudesonide-d6) is deuterium labeled (22R)-Budesonide. (22R)-Budesonide ((22R)-BUD) is the (22R)-enantiomer of Budesonide (HY-13580). (22R)-Budesonide is a non-halogenated glucocorticoid with high local anti-inflammatory activity .
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Triacetin-d5 is the deuterium labeled Triacetin. Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Dorzolamide-d5(hydrochloride) (L671152 hydrochloride-d5) is deuterium labeled Dorzolamide (hydrochloride). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
N-Desmethyl Sildenafil-d8 is the deuterium labeled N-Desmethyl Sildenafil (HY-117605). N-Desmethyl Sildenafil is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor .
Levocarnitine propionate-d5 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
N6-Methyladenosine-d3 (6-Methyladenosine-d3; N-Methyladenosine-d3) is a deuterium labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
rel-Ritonavir-d6 (rel-ABT 538-d6) is the deuterium labeled rel-Ritonavir. rel-Ritonavir is a relative configuration of Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to study of HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
2-Linoleoyl glycerol-d5 (2-Monolinolein-d5; 2-Monolinoleoylglycerol-d5) is the deuterium labeled 2-Linoleoyl glycerol (HY-130311). 2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
Glyceryl Triacetate-d9 is the deuterium labeled Triacetin . Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Dexamethasone-d3-1 (Hexadecadrol-d3-1; Prednisolone F-d3-1) is a deuterium labeled Dexamethasone (HY-14648). Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Levocarnitine propionate-d3 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa [4] .
Ethyl phenylglyoxylate-d5 (Ethyl benzoylformate-d5; Phenylglyoxylic acid ethyl ester-d5) is the deuterium labeled Ethyl phenylglyoxylate (HY-W016618). Ethyl phenylglyoxylate (Ethyl benzoylformate), the ethyl ester of phenylglyoxylic acid, is used as a synthetic reagent. Ethyl phenylglyoxylate is also a poor substrate but a potent inhibitor of chicken liver carboxylesterase. Additionally, Ethyl phenylglyoxylate exhibits photoreactivity, where its excited triplet carbonyl can initiate intermolecular hydrogen abstraction, radical coupling and cross-linking reactions .
17α-Hydroxyprogesterone-d8 is the deuterium labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
N-Methylpyrrolidone-d9 (NMP-d9) is deuterium labeled N-Methylpyrrolidone. N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an orally active organic polar solvent with teratogenicity and toxicity. N-Methylpyrrolidone is low in acute toxicity with a LD50 value of 3914 mg/kg in rats and of 4050 mg/kg in mice. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals [4].
Folic acid-d2 (Vitamin B9-d2) is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
N-Methylpyrrolidone-d3 is the deuterium labeled N-Methylpyrrolidone . N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an organic polar solvent. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals .
N,N'-Dinitrosopiperazine-d8 is the deuterium labeled N,N'-Dinitrosopiperazine . N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568 .
Tolterodine tartrate-d14 (Kabi-2234-d14) is deuterium labeled Tolterodine (tartrate). Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine. Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease [4].
Diethyltoluamide-d10 is the deuterium labeled Diethyltoluamide . Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects .
Acetyl tributyl citrate-d33 is the deuterium labeled Acetyl tributyl citrate (HY-W010981). Acetyl tributyl citrate (Tributyl O-acetylcitrate; ATBC) is an alternative plasticizer .
Mitotane-d8 is the deuterium labeled Mitotane . Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [4] .
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Ganciclovir-d5 is the deuterium labeled Ganciclovir. Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) .
13-cis Acitretin-d3 is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis .
Loratadine-d5-1 is a deuterated labeled Loratadine (HY-17043). Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
L-5-Hydroxytryptophan-d3 is the deuterium labeled L-5-Hydroxytryptophan. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [4] .
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats [4].
Citalopram-d3 ((±)-Citalopram-d3) hydrobromide is deuterium labeled Citalopram (hydrobromide). Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
Dexamethasone-d5-1 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
13C20, 15N10-Cyclic di-GMP ( 13C20, 15N10-c-di-GMP) is 13C and 15N labeled Cyclic-di-GMP (disodium). Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research [4] .
Tazobactam- 15N,d2 (CL-298741- 15N,d2) is 15N and deuterium labeled Tazobactam. Tazobactam (CL-298741) is a potent β-lactamases inhibitor and penicillin antibiotic. Tazobactam has antibacterial activity. Tazobactam can be used for pneumonia research .
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells [4].
Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
Uridine triphosphate- 13C9, 15N2 (UTP- 13C9, 15N2) sodium is a labeled Uridine triphosphate sodium. Uridine triphosphate sodium can be used in nucleic acid synthesis.
Adenine- 13C5,15C5 (6-Aminopurine- 13C5,15C5; Vitamin B4- 13C5,15C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Clascoterone-d5 (Cortexolone 17 alpha-propionate-d5) is the deuterated analog of Clascoterone. Clascoterone is a topical and peripheral androgen antagonist .
(-)-Epicatechin- 13C3 ((-)-Epicatechol- 13C3) is 13C labeled (-)-Epicatechin. (-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.
Chlophedianol- 13C6 is the 13C labeled Chlophedianol (HY-A0161). Chlophedianol is an orally active and potent antitussive agent. Chlophedianol can be used for the research of acute cough due to upper respiratory tract infections (URIs) .
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
Maribavir-d6 TFA (1263W94-d6 TFA; BW1263W94-d6 TFA; GW257406X-d6 TFA) is a deuterium labeled Maribavir (HY-16305). Maribavir is an orally active antiviral agent for cytomegalovirus (CMV) through inhibition of protein kinase UL97 and the following CMV DNA replication .
L-Asparagine- 15N2 monohydrate is the 15N-labeled L-Asparagine monohydrate (HY-W017443). L-Asparagine monohydrate is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine monohydrate can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia [4] .
Acetyl-L-carnitine-d9 (O-Acetyl-L-carnitine-d9) is deuterium labeled Acetyl-L-carnitine. Acetyl-L-carnitine (O-Acetyl-L-carnitine) is a compound involved in human metabolic research. It has relevant applications in predicting metabolite biomarker changes using the Recon 2 metabolic reconstruction model and integrating and analyzing multiple data types, but its specific activity mechanism is not described in detail based on the existing information .
D-Sorbitol-d-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
Dinoprost-d9 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
Phenethicillin sodium-d5 (Pheneticillin sodium-d5; α-Phenoxyethylpenicillin sodium-d5) is the deuterium labeled Phenethicillin sodium (HY-137945). Phenethicillin (α-Phenoxyethylpenicillin) sodium is a Penicillin, and has antimicrobial activity .
Perindopril-d3 (erbumine) is deuterated labeled Perindopril (erbumine) (HY-B0130A). Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure [4].
Atomoxetine-d5 (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice .
Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
D-Sorbitol-d2-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
D-(+)-Trehalose-d2 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi .
D-Sorbitol-d2-1 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
(S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction .
L-Norleucine-d9 is the deuterium labeled L-Norleucine. L-Norleucine ((S)-2-Aminohexanoic acid) is an isomer of leucine, specifically affects protein synthesis in skeletal muscle, and has antivirus activity.
Meglutol-d3 is the deuterium labeled Meglutol . Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
Meta-Fexofenadine-d6 is the deuterium labeled meta-Fexofenadine. meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine . Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial .
(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
Skatole-d8 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38 .
Labetalol hydrochloride-d5 (AH-5158 hydrochloride-d5) is deuterium labeled Labetalol hydrochloride (HY-B1108). Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy [4].
Glycyl-Exatecan-d5 (Glycyl-DX-8951-d5) hydrochloride is deuterium labeled Glycyl-Exatecan (HY-128995A). Glycyl-Exatecan (Glycyl-DX-8951), a derivative of Exatecan (HY-13631), is an anticancer agent. Glycyl-Exatecan has significantly antitumor activity. Glycyl-Exatecan can be used for cancers like solid tumors research.
Ethyl 4-methylbenzenesulfonate-d5 (Ethyl p-toluenesulfonate-d5; Ethyl tosylate-d5) is deuterium labeled Ethyl 4-methylbenzenesulfonate (HY-W014895). Ethyl 4-methylbenzenesulfonate is a drug intermediate that can be used for the synthesis of alkyl and substituted alkyl fluorides.
Alfacalcidol-d7 is the deuterium labeled Alfacalcidol. Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis [4].
D-(+)-Trehalose-d14 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi .
Skatole-d3 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38 .
Cortisone-d2 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations [4] .
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
Duloxetine-d5 (oxalate) ((S)-Duloxetine-d5 (oxalate)) is deuterium labeled Duloxetine. Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
Palmitoylethanolamide-d5 (Palmidol-d5, PEA-15,15,16,16,16-d5) is deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract .
Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease [4].
Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research .
13-Methyltetradecanoic acid-d6 is a deuterated labeled 13-Methyltetradecanoic acid . 13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells .
Nonanoyl-CoA-d17 (Pelargonoyl-CoA-d17) is the deuterium labeled Nonanoyl-CoA (HY-E70246). Nonanoyl-CoA is a medium-chain fatty acyl-CoA that can be used as substrate for the medium-chain hydrolase .
Prednisone- 13C2,d2 (Dehydrocortisone- 13C2,d2) is 13C labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus .
C6 Ceramide-d11 is deuterated labeled C6 Ceramide (HY-19542). C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
2'-Deoxycytidine-5'-monophosphoric acid- 13C9, 15N3 dilithium is 13C and 15N-labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
Sulfameter- 13C6 (Sulfametoxydiazine- 13C6) is the 13C6 labeled Sulfameter (HY-B0213). Sulfameter (Sulfametoxydiazine) is an orally active long-acting sulfonamide antibiotic. Sulfameter is active against both Gram-positive and Gram-negative bacteria. Sulfameter can be used for the research of diseases such as respiratory and urinary tract infections .
D-Glucose- 13C2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Propane-1,2,3-triyl tritricosanoate-d5 (Glycerol Tritricosanoate-d5) is deuterium labeled Propane-1,2,3-triyl tritricosanoate. 1,2,3-Tritricosanoyl glycerol is a triacylglycerol that contains tricosanoic acid (HY-W009081) at the sn-1, sn-2, and sn-3 positions. It has been used as an internal standard for the quantification of fatty acids in the triglyceride component of human aortic endothelial cells (HAECs) grown in media supplemented with stearic and/or oleic acid.
Epeleuton-d5 (15(S)-HEPE-d5 ethyl ester) is deuterium labeled Epeleuton. Epeleuton is a second-generation synthetic N-3 fatty acid derivative with activity in patients with non-alcoholic fatty liver disease, although it did not reach the primary endpoints of alanine aminotransferase and liver stiffness, but it can significantly reduce triglycerides, glycated hemoglobin, plasma glucose and inflammatory markers .
Umbelliferone- 13C6 (7-Hydroxycoumarin- 13C6) is the 13C-labeled Umbelliferone (HY-N0573). Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in
chronic alcohol-fed rats [4].
Xylose- 13C5 (D-(+)-Xylose- 13C5) is 13C labeled Xylose. Xylose (D-(+)-Xylose) is a natural pentose sugar that is catalyzed by xylose isomerase to form xylulose, which is a key step in the anaerobic ethanol fermentation of Xylose. Xylose can be used by microorganisms to produce fuels, chemicals, and bulk industrial enzymes. Xylose provides the substances and energy for cells, as a carbon source for the biosynthesis of high-value chemicals and biofuel. Xylose can be used to fully explore lignocellulose resources and provide a new direction for microbia fermentation [4].
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM .
Droxidopa- 13C6 (L-DOPS- 13C6) is 13C labeled Droxidopa. Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder) [4].
Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture .
D-Glucose- 13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose- 13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard .
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine . 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis [4].
Indomethacin- 13C6 (Indometacin- 13C6) is 13C labeled Indomethacin. Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research .
Oxybenzone- 13C6 (Benzophenone 3- 13C6) is the 13C-labeled Oxybenzone (HY-A0067). Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells .
Sildenafil-d3-1 (UK-92480-d3-1) is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
Estradiol- 13C6 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
Estradiol- 13C2 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway .
L-Serine- 13C3, 15N,d3 is the deuterium, 13C-, and 15-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Fluralaner- 13C2, 15N,d3 is the deuterium, 13C-, and 15-labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia .
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE . p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Treprostinil- 13C2-d1 (Sodium) (UT-15- 13C2-d1(sodium)) is deuterium and 13C labeled Treprostinil (sodium). Treprostinil (UT-15) sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
Rufinamide-d2 (CGP 33101-d2) is the deuterium labeled Rufinamide (HY-A0042). Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome [4].
Dehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality [4] .
(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
3,4,5-Trimethoxybenzoic acid-d3 is the deuterium labeled 3,4,5-Trimethoxybenzoic acid[1]. 3,4,5-Trimethoxybenzoic acid (Eudesmic acid;Trimethylgallic Acid) is a benzoic acid derivative. A building block in medicine and organic synthesis. 3,4,5-Trimethoxybenzoic acid exhibits antibacterial activity against S. aureus with MIC of 0.97 μg/mL .
Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality [4] .
Enrofloxacin-d5 (hydriodide) is the deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
3-Indoleacetic acid-d7 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
1-Linoleoyl Glycerol-d5 (1-Linoleoyl-rac-glycerol-d5; 1-Monolinolein-d5) is the deuterium labeled 1-Linoleoyl Glycerol (HY-111346). 1-Linoleoyl glycerol is a LpPLA2 inhibitor. 1-Linoleoyl glycerol acts as a precursor for synthesizing various functional lipids, such as phospholipids. 1-Linoleoyl glycerol mitigates inflammation induced by Apolipoprotein CIII (reduction of IL-6) .
Uridine triphosphate-d13 (UTP-d13 dilithium; Uridine 5'-triphosphate-d13) dilithium is deuterium labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Treprostinil- 13C2,d is the 13C- and deuterium labeled Treprostinil. Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
3-Indoleacetic acid-d5 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid-d5 can be used as internal standard for assay of IAA releases by alkaline hydrolysis of ester and amide conjugates .
N-Decyl-N,N-dimethyldecan-1-aminium-d6 (chloride) is a deuterated labeled N-Decyl-N,N-dimethyldecan-1-aminium (chloride) . N-Decyl-N,N-dimethyldecan-1-aminium chloride (Didecyldimethylammonium chloride) is a dialkyl-quaternary ammonium compound that is used in numerous products for its bactericidal, virucidal and fungicidal properties .
Tadalafil- 13C2,d3-1 (IC-351- 13C2,d3-1) is the deuterium and 13C-labeled Tadalafil (HY-90009A). Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
Retinyl acetate-d3 (ALK-001) is a deuterated Vitamin A. Retinyl acetate-d3 can be used for research of geographic atrophy (GA) secondary to age-related macular degeneration (AMD) .
IDO-IN-7-d10 (NLG-919 analogue-d10; GDC-0919 analogue-d10) is the deuterium labeled IDO-IN-7 (HY-13983). IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Bzo-poxizid-d9 (5C-MDA-19-d9, Petyl MDA-19-d9) is deuterium labeled Bzo-poxizid. Bzo-poxizid is a synthetic cannabinoid that is a psychoactive substance .
O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism .
Tazarotene-13C2,d2 (AGN 190168-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotene (HY-15388). Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
Medroxyprogesterone-d3 is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity .
rac Timolol-d5 (maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction .
(S)-Indoximod-d3 is the deuterium labeled (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer .
Nitroxoline-d5 (8-Hydroxy-5-nitroquinoline-d5) is deuterium labeled Nitroxoline. Nitroxoline (8-Hydroxy-5-nitroquinoline), an antibiotic, is an orally active antibiofilm agent. Nitroxoline reduces the formation and induces the dispersal of Pseudomonas aeruginosa biofilms by chelation of iron and zinc. Nitroxoline can be used for the urinary tract infections and cancer research .
N1-Methylpseudouridine-d3 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
2'-Deoxycytidine- 15N3 is the 15N labeled 2'-Deoxycytidine . 2'-Deoxycytidine, a deoxyribonucleoside, could inhibit biological effects of Bromodeoxyuridine (Brdu) .
Erlotinib- 13C6 hydrochloride is the 13C labeled Erlotinib Hydrochloride . Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM . Erlotinib- 13C6 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2'-Deoxycytidine-5'-monophosphoric acid-d12 dilithium is deuterium labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid . 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [4].
Adenosine monophosphate- 13C10, 15N5,d12 (AMP- 13C10, 15N5,d12) dilithium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Leflunomide- 13C6 (HWA486- 13C6) is 13C labeled Leflunomide. Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.
Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis [4]. Tamoxifen also can induce gene knockout of CreER transgenic mouse .
L-Histidine- 13C6, 15N3,d5 hydrochloride hydrate is the deuterium, 13C-, and 15-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Elvitegravir- 13C6 (GS-9137- 13C6) is 13C labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
Rilpivirine- 13C6 (R278474- 13C6) is 13C labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV(EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
Deoxycytidine triphosphate- 13C9, 15N3 (dCTP- 13C9, 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9, 15N3) dilithium is 13C and 15N-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Cytidine 5′-monophosphate- 13C9, 15N3 (5'-Cytidylic acid- 13C9, 15N3 dilithium; 5'-CMP- 13C9, 15N3) dilithium is 13C and 15N-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Cytidine- 13C9, 15N3 is the 13C and 15N labeled Cytidine . Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [4].
5'-Guanylic acid- 13C10, 15N5 (5'-GMP- 13C10, 15N5 dilithium; 5'-guanosine monophosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
L-Glutamine- 13C5, 15N2,d5 is the deuterium, 13C-, and 15-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Biotin- 13C5 (Vitamin B7- 13C5) is 13C labeled Biotin. Biotin, vitamin B7 and serves as a coenzyme for five carboxylases in humans, involved in the synthesis of fatty acids, isoleucine, and valine, and in gluconeogenesis. Biotin is necessary for cell growth, the production of fatty acids, and the metabolism of fats and amino acids .
Glucosylsphingosine- 13C6 (Glucopsychosine- 13C6) is the 13C-labeled Glucosylsphingosine (HY-N7745). Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide with neurotoxicity and is also a noncompetitively inhibitor of glucocerebrosidase with a Ki value of 30 μM. Glucosylsphingosine is promising for research of Krabbe and Gaucher disease.
Fosfructose- 13C6 (tetrasodium hydrate) is the 13C labeled Fosfructose (HY-106950). Fosfructose is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma .
2-Phenylethanol- 13C2 is 13C labeled 2-Phenylethanol (HY-B1290). 2-Phenylethanol (Phenethyl alcohol) is an aromatic alcohol with a rose-like odour. 2-Phenylethanol is a flavour and fragrance compound, and can be used as a preservative and anti-microbial agent. 2-Phenylethanol has antityrosinase and antimicrobial activities .
Sulfamethazine- 13C6 is a 13C-labeled Sulfamethazine (HY-A0178). Sulfamethazine (Sulfadimidine) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections) .
Colfosceril miristate-d13 (DMPC-d13) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Hydroxyprogesterone Caproate-d11 (17α-Hydroxyprogesterone hexanoate-d11; 17α-Hydroxyprogesterone caproate-d11) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate is a synthetic progestin, a steroid.
Ribitol- 13C5 (Adonitol- 13C5) is the 13C-labeled Ribitol (HY-100582). Ribitol is a crystalline pentose alcohol formed by the reduction of ribose. Enhancing the flux of D-glucose to the pentose phosphate pathway in Saccharomyces cerevisiae for the production of D-ribose and ribitol.
VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc) .
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats [4] .
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
D-Fructose- 13C6,d7 is the deuterium and 13C labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants .
Menaquinone-4-d7 (Vitamin K2(MK-4)-d7) is the deuterium labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
Oleic acid-d9 is deuterium labeled Oleic acid (HY-N1446). Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activato .
α-Vitamin E-d11 ((+)-α-Tocopherol-d11) is the deuterium labeled α-Vitamin E (HY-N0683). α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant .
Colfosceril miristate-d9 (DMPC-d9) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Furagin- 13C3 (Furazidine- 13C3) is the 13C-labeled Furagin (HY-77036). Furagin (Furazidine), an analogue of Nitrofurantoin (HY-A0090), is an antibiotic with antibacterial activity against ESKAPE pathogens with MIC values of 0-32 μg/mL. Furagin inhibits human Carbonic anhydrases . Furagin is promising for research of cancer and urinary tract infections (UTIs) [4] .
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d67 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
1,3-Dipalmitin-d5 (1,3-Dipalmitoylglycerol-d5) is a deuterium labeled 1,3-Dipalmitin (HY-128792). 1,3-Dipalmitin (1,3-Dipalmitoylglycerol) is a cerebroside that can be found in Typhonium giganteum Engl .
Colfosceril miristate-d58 (DMPC-d58) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Tazarotenic acid-13C2,d2 (AGN 190299-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
Sapropterin-d3((6R)-BH4-d3) is deuterium labeled Sapropterin. Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU) .
Docosahexaenoic acid-d5 methyl ester is the deuterium labeled Docosahexaenoic Acid methyl ester. Docosahexaenoic Acid methyl ester is a methylated docosahexaenoic acid analog which can be intercalated into membrane phospholipids without being oxidized or hydrolyzed .
Oleic acid-d2) is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid ]. Oleic acid is a Na+/K+ ATPase activator .
Colfosceril miristate-d63 (DMPC-d63) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Deoxycytidine triphosphate-d14 (dCTP-d14 dilithium; 2′-Deoxycytidine-5′-triphosphate-d14) dilithium is deuterium labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
L-5-Hydroxytryptophan-d3-1 is the deuterium labeled L-5-Hydroxytryptophan . L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [4] .
(Rac)-Atomoxetine-d7 (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
Thymidine- 15N2 is the 15N labeled Thymidine . Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication [4].
Oleic acid-d17 is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate . Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor [4] .
Cytidine-5'-triphosphate-d14 (Cytidine triphosphate-d14 dilithium; 5'-CTP-d14) dilithium is deuterium labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist .
Levofloxacin-d3 ((-)-Ofloxacin-d3) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity [4] .
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning [4].
Carbocisteine-d3 (Carbocysteine-d3) is deuterium labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research [4] .
Phenformin-d5 (hydrochloride) is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity .
Digoxigenin-d3 (Lanadigenin-d3) is the deuterium labeled Digoxigenin (HY-B1025). Digoxigenin (DIG) is a steroid. DIG is used for situ hybridization as a labeling molecule probe due to long shelf life and fast detection and high sensitivity of DIG-labeled riboprobes .
Pyridoxine-d2 (Pyridoxol-d2) is deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Fenoverine-d8 is the deuterium labeled Fenoverine. Fenoverine (Spasmopriv) is an orally active and powerful anti-spasmodic drug. Fenoverine reduces calcium ion influx by suppressing voltage dependent calcium channels. Fenoverine has antiemetic, analgesic, and antidiarrheal effects. Fenoverine induces rhabdomyolysis. Fenoverine can be used to study smooth muscle overexcitation related conditions such as gastrointestinal spasms .
Dipivefrin-d6 (hydrochloride) is deuterium labeled Dipivefrin (hydrochloride). Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma proagent that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea .
Diphenylmethane-d2 (Benzylphenyl-d2) is the deuterium labeled Diphenylmethane (HY-W008814). Diphenylmethane (Benzylphenyl) is an aromatic compound used as a drug intermediate. Diphenylmethane in the fragrance industry is used as an oxidizing agent and in soaps; in pesticides, as a synergist; and in dyes, as a plasticizer.
Ibuprofen-d3 ((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [4].
Norethindrone-d8 (Norethisterone-d8) is deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Levofloxacin-d8 is the deuterium labeled Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
Desacetylcephapirin-d6 sodium (Deacetylcephapirin-d6 sodium) is the deuterium labeled Desacetylcephapirin sodium (HY-131989). Desacetylcephapirin (Deacetylcephapirin) sodium is an active metabolite of Cephapirin (HY-A0153A). Desacetylcephapirin sodium has antimicrobial against S. aureus and coagulase-negative staphylococci mastitis pathogen .
Deltamethrin-d5 is the deuterium labeled Deltamethrin. Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis .
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
Temephos-d12 is the deuterium labeled Temephos . Temefos is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage .
Betulin-d3 (Trochol-d3) is deuterium labeled Betulin. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line .
Pyridoxine-d5 (Pyridoxol-d5) is a deuterium labeled Pyridoxine (HY-B1328). Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence . Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor .
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine(HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections [4].
Nordoxepin-d3 (hydrochloride) is the deuterium labeled Nordoxepin hydrochloride. Nordoxepin hydrochloride is an active metabolite of Doxepin hydrochloride (HY-B0725), which is an orally active tricyclic antidepressant .
Salvigenin-d9 is the deuterium labeled Salvigenin. Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties .
Bendroflumethiazide-d5 (Bendrofluazide-d5) is the deuterium labeled Bendroflumethiazide (HY-B1363).Bendroflumethiazide (Bendrofluazide) is an orally available diuretic. Bendroflumethiazide inhibits the electroneutral sodium-chloride symporter located in the apical membrane of the early segment of the distal convoluted tubule and can effectively lower blood pressure. Bendroflumethiazide is used in the study of hypertension and edema. Bendroflumethiazide has an antidiuretic effect in diabetes insipidus .
Bestatin-d10 (Ubenimex-d10) is deuterium labeled Bestatin. Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
Edoxudine-d5 (EUDR-d5) is the deuterium labeled Edoxudine (HY-B1011). Edoxudine is an antiviral active molecule and thymidine analog. Edoxudine is effective against herpes simplex virus .
Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Dyclonine-d9 (hydrochloride) is deuterium labeled Dyclonine (hydrochloride). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an effective component of Runhou tablets. Dyclonine hydrochloride has significant bactericidal and fungicidal activity .
Chlorpheniramine-d6 (Chlorphenamine-d6) is deuterium labeled Chlorpheniramine. Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research .
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma [4] .
Hexadecanal-d5 (Palmitaldehyde-d5) is deuterium labeled Hexadecanal. Hexadecanal (Palmitaldehyde) , a volatile long-chain aliphatic aldehyde, is emitted from human feces, skin, and breath. The receptor for hexadecanal(OR37B) is highly conserved across mammals. Hexadecanal may exert its effects by modulating functional connectivity between the brain substrates of social appraisal and the brain substrates of aggressive execution. Also, Hexadecanal is confirmed to be highly deterrent to the ant Lasius niger. Hexadecanal is promising for the research of startle responses and aggression [4]
Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
Nefopam-d3 (hydrochloride) is the deuterium labeled Nefopam hydrochloride. Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo .
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria .
Levamisole-d5 (hydrochloride) is the deuterium labeled Levamisole hydrochloride. Levamisole ((-)-Tetramisole) hydrochloride is an anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives. Levamisole hydrochloride has antiviral effects against HSV .
Ethambutol-d10 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Norethindrone-d7 (Norethisterone-d7) is the deuterium labeled Norethindrone (HY-B0554). Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Hydrocortisone-d2 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Pyridoxine-d3 is a deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway .
Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex .
Lumefantrine-d9 is the deuterium labeled Lumefantrine. Lumefantrine is an antimalarial drug, used in combination with Artemether. The artemether-lumefantrine (AL) as the first- and second-line anti-malarial drugs.
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55) .
Deltamethrin-d6 (Decamethrin-d6) is deuterium labeled Deltamethrin. Deltamethrin (Decamethrin) is an orally active synthetic pyrethroid insecticide. Deltamethrin induces oxidative stress and results in inflammation and apoptosis via inhibiting Nrf2/HO-1 pathway. Deltamethrin has an anticancer effect by inducing apoptosis. Deltamethrin can be used extensively in pest control [4] .
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
Diphenylmethanol-d10 (Benzhydrol-d10) is the deuterium labeled Benzhydrol (HY-W004059). Diphenylmethanol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
Prednisone-d7 (Dehydrocortisone-d7) is deuterium labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus .
Desmethylmirtazapine-d6 hydrochloride (Normirtazapine-d6 hydrochloride) is the deuterium labeled Desmethylmirtazapine (HY-119223). Desmethylmirtazapine is an active metabolite of Mirtazapine that has antidepressant effects .
Pramocaine-d9 (hydrochloride) is deuterium labeled Pramocaine (hydrochloride). Pramocaine hydrochloride decreases the permeability of neuronal membranes to sodium ions, blocking both initiation and conduction of nerve impulses.
Anagliptin-d7 (SK-0403-d7) is deuterium labeled Anagliptin. Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4(DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively .
Ethotoin-d5 is the deuterium labeled Ethotoin . Ethotoin (Peganone) is an orally active anticonvulsant agent used in epilepsy research, Ethotoin is a hydantoin, similar to phenytoin .
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch .
Acenaphthylene-d8 is the deuterium labeled Acenaphthylene . Acenaphthylene is a polycyclic aromatic hydrocarbon (PAH). PAHs are derived naturally from coal and tar deposits, and produced by incomplete combustion of organic matter .
Econazole-d6 ((±)-Econazol-d6) is the deuterium labeled Econazole (HY-B0885). Econazole is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage [4] .
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent .
Torsemide-d7 is the deuterium labeled Torsemide. Torsemide (Torasemide) is an orally active loop diuretic. Torsemide has anti-aldosterone and vasodilatory effects. Torsemide also can be used for the research of heart failure, renal disease and hepatic cirrhosis .
Piperacillin-d5 is deuterium labeled Piperacillin. Piperacillin is kind of semisynthetic penicillins. Piperacillin has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Piperacillin has shown greater activity against β-lactamase-producing organisms than the other penicillins .
Lidocaine-d6 (Lignocaine-d6) is deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
Pitolisant-d6 (Tiprolisant-d6) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
Adrenosterone-d10 ((+)-Adrenosterone-d10) is the deuterium labeled Adrenosterone (HY-17462). Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells .
Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect [4].
Psychosine-d7 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell
Trigonelline-d3 (chloride) is the deuterium labeled Trigonelline chloride. Trigonelline chloride, an alkaloid with potential antidiabetic activity, is present in considerable amounts in coffee. Trigonelline chloride has anti-HSV-1 , antibacterial, and antifungal activities.
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Atovaquone-d5 is the deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome?bc1?complex. Atovaquone is against human and ?P. falciparum?cytochrome?bc1?activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia .
Dibucaine-d9 is the deuterium labeled Dibucaine(HY-B0552).Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor .
Pitolisant-d10 (Tiprolisant-d10) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Prednisone-d8 is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
Bendroflumethiazide-d7 (Bendrofluazide-d7) is deuterium labeled Bendroflumethiazide (HY-B1363). Bendroflumethiazide (Bendrofluazide) is an orally available diuretic. Bendroflumethiazide inhibits the electroneutral sodium-chloride symporter located in the apical membrane of the early segment of the distal convoluted tubule and can effectively lower blood pressure. Bendroflumethiazide is used in the study of hypertension and edema. Bendroflumethiazide has an antidiuretic effect in diabetes insipidus .
Amitriptylinoxide-d6 (Equilibrin-d6) is the deuterium labeled Amitriptylinoxide (HY-107032). Amitriptylinoxide (Equilibrin) is an analogue and metabolite of amitriptyline with similar antidepressant efficacy .
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
Ditiocarb-d10 sodium (Sodium diethyldithiocarbamate-d10) is the deuterium labeled Ditiocarb sodium (HY-B1637). Ditiocarb sodium (Sodium diethyldithiocarbamate) is an orally active copper reagent. Ditiocarb sodium exhibits activities such as antioxidation, chelation, anti-tumor effects, immunomodulation, and anti-HIV properties. Ditiocarb sodium can be used in the research of tumors, inflammatory, and immune-related diseases .
Pefloxacin-d3 (Pefloxacinium-d3) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies [4] .
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin? is a Histamine 1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant .
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis [4] .
Furaltadone-d5 is the deuterium labeled Furaltadone (HY-B1148A). Furaltadone, a nitrofuran agent, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci .
Psychosine-d5 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell.
Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium lepraeInhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy [4] .
Nefopam-d3 is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells .
Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies [4] .
Imidaprilat-d3 (6366A-d3) is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease .
DTAC-d3 (Dodecyltrimethylammonium-d3 chloride) is the deuterium labeled DTAC (HY-W096983). DTAC is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Bopindolol-d9 ((±)-Bopindolol-d9) is the deuterium labeled Bopindolol (HY-B1562). Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
Inosinic acid- 13C5 (5'-IMP- 13C5) is the 13C-labeled Inosinic acid (HY-108213). Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant, or as the dietary supplement to improve the yield and meat quality of pigs .
Chlorogenic acid- 13C3 (Heriguard- 13C3; NSC-407296- 13C3) is 13C- and 15N-labeled Chlorogenic acid (HY-N0055). Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb.. It plays several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension .
Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
L-Theanine- 13C2, 15N2 (L-Glutamic Acid γ-ethyl amide- 13C2, 15N2) is the 13C- and 15N-labeled L-Theanine (HY-15121). L-Theanine (L-Glutamic Acid γ-ethyl amide) is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective, anticancer and anti-oxidative activities. L-Theanine can pass through the blood–brain barrier and is orally active.
Cytidine-d13 (Cytosine β-D-riboside-d13) is deuterium labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function .
Thymidine- 13C10 (DThyd- 13C10; NSC 21548- 13C10) is 13C-labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Cytidine 5′-monophosphate-d12 (5'-Cytidylic acid-d12 dilithium; 5'-CMP-d12) dilithium is deuterium labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid-d12 (5'-GMP-d12 dilithium; 5'-guanosine monophosphate-d12) dilithium is deuterium labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Estrone- 13C3 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Ritonavir- 13C3 is 13C labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM .
D-Mannitol- 13C6 is the 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
L-Glutathione reduced-d5 (GSH-d5; γ-L-Glutamyl-L-cysteinyl-glycine-d5) is the deuterium labeled L-Glutathione reduced (HY-D0187). L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
Omeprazole metabolite Omeprazole sulfone (methoxy-d3) is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Sarcosine- 13C3 (N-Methylglycine- 13C3; Sarcosin- 13C3) is the 13C-labeled Sarcosine (HY-101037). Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia .
N-Acetyl mesalazine-d3 (N-Acetyl-5-aminosalicylic acid-d3) is the deuterium labeled N-Acetyl mesalazine (HY-66008). N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the primary intestinal metabolite of 5-Aminosalicylic Acid (HY-15027) and serves as a biomarker for evaluating the efficacy of 5-Aminosalicylic Acid (HY-15027). N-Acetyl mesalazine can scavenge free radicals, reduce DNA base hydroxylation, and ameliorate mucosal inflammation. N-Acetyl mesalazine can be used in the study of diseases such as colitis and colon cancer .
Guanosine- 15N5 is the 15N labeled Guanosine . Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Nicotinamide- 13C6 is the 13C-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Guanosine triphosphate- 15N5,d14 (GTP- 15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
L-Tryptophan- 13C11 is the 13C-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
6-(γ,γ-Dimethylallylamino)purine-d6 is the deuterium labeled 6-(γ,γ-Dimethylallylamino)purine (HY-112103). 6-(γ,γ-Dimethylallylamino)purine is a plant growth substance .
Cytidine-d2 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function .
Pyrroloquinoline quinone- 13C3 (PQQ- 13C3) sodium is an isotope of Pyrroloquinoline quinone. Pyrroloquinoline quinone (PQQ), a redox co-factor, is an anionic, redox-cycling orthoquinone. Pyrroloquinoline quinone is isolated from cultures of methylotropic bacteria and tissues of mammals. Pyrroloquinoline quinone is an essential nutrient for mammals and is important for immune function .
Desogestrel- 13C2,d2-1 (Org-2969- 13C2,d2-1) is the deuterium labeled and 13C-labeled Desogestrel (HY-12516). Desogestrel (Org-2969) is a third-generation progesterone analogue contained in many oral contraceptive preparations. Desogestrel is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups [4].
Estrone- 13C2 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells .
Glucosamine- 13C6 (D-Glucosamine- 13C6) is 13C labeled Glucosamine. Glucosamine (D-Glucosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes .
Cyromazine- 13C3 is the 13C3 labeled Cyromazine. Cyromazine is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects.
L-Tryptophan- 15N2 is the 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
(E,E)-Farnesol-d6 (trans,trans-Farnesol-d6) is deuterium labeled (E,E)-Farnesol (HY-Y0248). (E,E)-Farnesol (trans,trans-Farnesol) is a quorum-sensing molecule of Candida species. (E,E)-Farnesol can inhibit the growth, metabolism and biofilm formation of various Candida species, and affect their morphology and invasiveness .
(R,R)-Secoisolariciresinol diglucoside-d6 is deuterated labeled (R,R)-Secoisolariciresinol diglucoside (HY-N6937). (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells .
Guanosine- 13C10 is the 13C labeled Guanosine (HY-N0097). Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Adenosine monophosphate- 15N5,d12 (AMP- 15N5,d12) dilithium is deuterium and 15N labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Cytidine-d is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catechol
Tricaprilin- 13C3 (Trioctanoin- 13C3) is a 13C-labeled Tricaprilin (HY-B1804) . Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) .
Clomipramine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Clomipramine (hydrochloride). Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD) .
D-Glucose- 13C3-1 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Methoxsalen- 13C,d3 (8-Methoxypsoralen- 13C,d3) is the deuterium and 13C-labeled Methoxsalen (HY-30151). Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) .Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Dihydroartemisinin- 13C,d5 (Dihydroqinghaosu- 13C,d5) is the deuterium labeled and 13C-labeled Dihydroartemisinin (HY-N0176). Dihydroartemisinin is a potent anti-malaria agent.
D-Glucose- 13C,d is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C3-2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response .
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
Decitabine- 13C5 (5-Aza-2'-deoxycytidine- 13C5) is 13C labeled Decitabine. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity .
Tedizolid- 13C,d3 is the 13C- and deuterium labeled Tedizolid. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Lumateperone- 13C,d3 (ITI-007- 13C,d3) tosylate is 13C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia [4].
Vanillin- 13C6 is the 13C labeled Vanillin . Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine .
Rufinamide- 15N,d2 (CGP 33101- 15N,d2) is the deuterium and 15N labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome [4].
2-Methoxybenzoic acid- 13C6 is the 13C-labeled 2-Methoxybenzoic acid. 2-Methoxybenzoic acid (NSC 3778) is used as an internal standard of salicylic acid and its putative biosynthetic precursors in cucumber leaves. Another known use is in the synthesis of Benextramine.
Lamotrigine- 13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
3-O-Methyldopa-d3 (3-Methoxy-L-tyrosine-d3) is deuterium labeled 3-O-Methyldopa (HY-113468A). 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa has certain antidepressant and neuroprotective activities. 3-O-Methyldopa can be used in the research of nervous system diseases such as depression and Parkinson's disease .
L-Theanine-d5 is the deuterium labeled L-Theanine. L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake .
Hypoxanthine- 13C5 is a 13C-labeled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Vitamin D3- 13C5 is the 13C-labeled Vitamin D3 (HY-15398). Vitamin D3 (Cholecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells .
L-Glutamine- 15N2,d5 is the deuterium and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability [4].
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Vitamin K1- 13C6 is the 13C-labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism.
Adenosine- 13C10 (Adenine riboside- 13C10; D-Adenosine- 13C10) is 13C-labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis [4] .
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
Procainamide- 13C2 hydrochloride is 13C labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Vadadustat- 13C6 (PG-1016548- 13C6) is 13C labeled Vadadustat. Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor . Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo .
Dutasteride- 13C6 is the 13C labeled Dutasteride . Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
Fosamprenavir- 13C6 is the 13C-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .
Adrenosterone- 13C3 ((+)-Adrenosterone- 13C3) is the 13C-labeled Adrenosterone (HY-17462). Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells .
D-Sorbitol- 13C6 is the 13C labeled D-Sorbitol . D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement .
3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) hydrate is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa hydrate inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa hydrate has certain antidepressant and neuroprotective activities. 3-O-Methyldopa hydrate can be used in the research of nervous system diseases such as depression and Parkinson's disease .
Lodoxamide- 15N2,d2 (U-42585E (free acid)- 15N2,d2) is the deuterium and 15N-labeled Lodoxamide (HY-14270). Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
Adenosine- 13C5 is the 13C labeled Adenosine . Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
Pentetic acid- 13C5 (Diethylenetriaminepentaacetic acid- 13C5) is the 13C-labeled Pentetic acid (HY-B1335). Pentetic acid (Diethylenetriaminepentaacetic acid) is an orally active compound with biodegradability used to construct magnetic adsorbent, which can simultaneously remove heavy metal and dye from complex wastewater. Pentetic acid can form strong metal complexes, which prevents metal ions from catalysing the decomposition of peroxygen chemicals, especially hydrogen peroxide [4].
Pantethine- 15N2 is the 15N2 labeled Pantethine. Pantethine is an orally active lipid-lowering agent. Pantethine has anti-tumor, anti-inflammatory and anti-SARS-COV virus activities. Pantethine is also a neuroprotective agent. Pantethine can be used in the study of Alzheimer's disease, Parkinson's disease, major depression, systemic sclerosis and pantothenate kinase-related neurodegeneration [4] .
L-Serine- 13C3 is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Histamine- 13C5, 15N3 (Ergamine- 13C5, 15N3) is the 13C and 15N labeled isotope of Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
Deoxythymidine-5'-triphosphate- 15N2,d15 (dTTP- 15N2,d15) dilithium is deuterium and 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Vitamin D3- 13C3 is the 13C-labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Topiramate-13C6 (McN 4853-13C6) is the 13C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
Thyroxine hydrochloride- 13C6 is the 13C-labeled L-Thyroxine. L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4) .
ATP- 15N5,d14 (Adenosine 5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Etravirine- 13C3 (R165335- 13C3) is the 13C-labeled Etravirine (HY-90005). Etravirine (R165335; TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Glycidamide- 13C3 (Oxiranecarboxamide- 13C3) is the 13C-labeled Glycidamide (HY-119329). Glycidamide is the genotoxic metabolite of Acrylamide. Glycidamide can react with proteins, such as hemoglobin, or with DNA, and induces genotoxic effects .
Adenosine- 15N5 (Adenine riboside- 15N5; D-Adenosine- 15N5) is the 15N labled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
Zonisamide- 13C6 (AD 810- 13C6) is 13C labeled Zonisamide. Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy [4].
Saracatinib-d3 (AZD0530-d3) (ZG5129) is the deuterium-labeled analog of Saracatinib (HY-10234). Saracatinib-d3 is an inhibitor of the Src kinase, which can inhibit severe sepsis caused by bacterial or various microbial infections .
Perindopril-d5 (S-9490-d5) is deuterium labeled Perindopril. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension [4].
Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
Iodopropynyl butylcarbamate-d9 (IPBC-d9) is the deuterium labeled Iodopropynyl butylcarbamate (HY-W009335). Iodopropynyl butylcarbamate (IPBC) is a potent fungicide and preservative, which has been used in the paints, coatings, wood preservatives, personal care, and cosmetics industries .
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders .
Nabumetone-d3 is the deuterium labeled Nabumetone. Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the proagent of the active metabolite 6MNA.
Eletriptan-d3 is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively .
Vericiguat-d3 (BAY1021189-d3) hydrochloride is a deuterated Vericiguat with tracer functionality. Vericiguat is an orally available stimulator of guanylate cyclase .
Licofelone-d6 is the deuterium labeled Licofelone . Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins [4].
Cyprodinil-d5(CGA-219417-d5) is the deuterium labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
Phytosphingosine-d7(4-Hydroxysphinganine-d7) is deuterium labeled Phytosphingosine. Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes [4] .
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation .
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity .
Dienogest-d6 is deuterium labeled Dienogest (HY-B0084). Dienogest is an orally active progesterone receptor agonist that can be used in the study of endometriosis .
Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B .
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Upadacitinib-d5 is the deuterium labeled Upadacitinib. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Quinapril-d5 hydrochloride (CI-906-d5) is the deuterium labeled Quinapril hydrochloride. Quinapril hydrochloride (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications .
Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM .
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM) .
Ertugliflozin-d9 is deuterated labeled Ertugliflozin (HY-15461). Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2 . Has the potential for the treatment of type 2 diabetes mellitus .
Dinotefuran-d3 is the deuterium labeled Dinotefuran . Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors .
Penicillin G-d5 (potassium) is the deuterium labeled Penicillin G potassium. Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas .
Trifloxystrobin-d3 is the deuterium labeled Trifloxystrobin (HY-123230). Trifloxystrobin (CGA 279202) is a type of fungicide. Trifloxystrobin has toxicity, antiparasitic activity and induce apoptosis, oxidative stress and DNA damage. Trifloxystrobin can be used for the reaesrch of fungal diseases [4] .
Trandolapril-d5 is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF) .
Dansyl chloride-d6 is the deuterium labeled Dansyl chloride (HY-D0017). Dansyl chloride is a reagent that produces stable blue or blue-green fluorescent sulfonamide adducts in the reaction of aliphatic and aromatic amines with primary amino groups, and is widely used for modified amino acids, protein sequencing and amino acid analysis .
Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer [4].
Voxelotor-d6 (GBT 440-d6) is deuterium labeled Voxelotor. Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment .
Etrasimod-d9 (APD334-d9) is a deuterium labeled Etrasimod (HY-12789). Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells. .
Posaconazole-d5 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity .
Mexiletine-d3 (hydrochloride) is deuterium labeled Mexiletine (hydrochloride). Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1][2].
Atenolol-d6 ((RS)-Atenolol-d6) is deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris .
Ergothioneine-d9 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant .
Cuminaldehyde-d8 is deuterated labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Flunixin-d3 is the deuterium labeled Flunixin. Flunixin Meglumine is a potent inhibitor of COX used as analgesic agent with anti-inflammatory and antipyretic activity .
Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively .
Permethrin-d6 (NRDC-143-d6) is deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) [4] .
Amoxapine-d8 is the deuterium labeled Amoxapine. Amoxapine (CL-67772) is a norepinephrine reuptake blocker and a 5-HT2/5-HT3 antagonist. Amoxapine can be used for the research of depression. Amoxapine has antibacterial activity. Amoxapine can enhance the killing effect of macrophages on mycobacterium by inducing autophagy, while protecting the cells from death [4].
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
Diethyl cromoglycate-d5 (Diethylchromoglycate-d5) is the deuterium labeled Diethyl 5,5'-((2-hydroxypropane-1,3-diyl)bis(oxy))bis(4-oxo-4H-chromene-2-carboxylate) (HY-W099125).
Resorufin-d6 is the deuterium labeled Resorufin. Resorufin (NSC 12097) is a highly fluorescent pink dye for the detection of ROS/RNS and a second analyte .
Parbendazole-d3 is the deuterium labeled Parbendazole. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects .
Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels .
Ledipasvir-d16 (GS-5885-d16) is deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Blonanserin-d5 (AD-5423-d5) is a deuterium labeled Blonanserin (HY-13575). Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic .
Glycolithocholic acid-d5 (Lithocholylglycine-d5) is the deuterium labeled Glycolithocholic acid (HY-116374). Glycolithocholic acid (Lithocholylglycine), an endogenous metabolite, is a glycine-conjugated secondary bile acid. Glycolithocholic acid can be used to diagnose ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH) and primary sclerosing cholangitis (PSC) [4].
Treprostinil-d7 (UT-15-d7) is a deuterated version of Treprostinil (HY-100441). Treprostinil is a highly potent DP1 and EP2 agonist with EC50s of 0.6 nM and 6.2 nM, respectively [4] .
Anastrozole-d12 is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM .
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage .
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research [4].
Danicamtiv-d6 (MYK-491-d6) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
Lauryl benzalkonium-d7 (Dimethylaurylbenzylammonium-d7) chloride is the deuterium labeled Lauryl benzalkonium chloride. Lauryl benzalkonium chloride is a cationic surfactant .
Dolasetron-d5 is deuterated labeled Dolasetron (HY-B0750). Dolasetron (MDL-73147) is a 5-HT3 receptor antagonist with potential for treatment of chemotherapy-induced nausea and vomiting.
Crizotinib-d9 (PF-02341066-d9) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
Benzyl alcohol-d5 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives . Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ropinirole-d14 hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Canagliflozin-d6 is the deuterium labeled Canagliflozin . Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively .
Parecoxib-d5 (SC 69124-d5) is deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
Losartan-d2 is the deuterium labeled Losartan . Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Pemetrexed-d5 is the deuterium labeled Pemetrexed . Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
Methylprednisolone-d2 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels [4].
Ropinirole-d3 (SKF 101468-d3) is deuterium labeled Ropinirole. Ropinirole (SKF 101468) is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole has no affinity for the D1 receptors. Ropinirole has the potential for Parkinson's disease .
Tazarotene-d6 (AGN 190168-d6) is deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
Tigecycline-d9 is deuterium labeled Tigecycline. Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL . MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively .
Zafirlukast-d6 is deuterated labeled Zafirlukast (HY-17492). Zafirlukast (ICI 204219) is a potent orally active leukotriene D4(LTD4)receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Ritodrine-d3 (hydrochloride) is the deuterium labeled Ritodrine (hydrochloride). Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
Prochloraz-d7 (BTS 40542-d7) is the deuterium labeled Prochloraz (HY-B0845). Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM .
Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity .
Permethrin-d9 is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
Losartan-d9 is the deuterium labeled Losartan . Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Ozenoxacin-d3 is the deuterium-labeled Ozenoxacin (HY-14957). Ozenoxacin-d3 is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Alfuzosin-d7 is the deuterium labeled Alfuzosin . Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) .
Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
1-Octanol-d5 is deuterated labeled 1-Octanol (HY-W032013). 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Leniolisib-d5 is a deuterated labeled Leniolisib . Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
Treprostinil-d9 (UT-15-d9) is the deuterium-labeled Treprostinil (HY-100441) . Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
1-Octanol-d17 is the deuterium labeled 1-Octanol . 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Diphenyl Phosphate-d10 (DPhP-d10) is the deuterium labled Diphenyl Phosphate (HY-W008151). Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.
Cefiderocol-d6 (S-649266-d6) is a deuterated labeled Cefiderocol (HY-17628). Cefiderocol is a siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less .
Sulindac-d3 is deuterium labeled Sulindac. Sulindac (MK-231) is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.
Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
Iodobenzene-d2 is the deuterium labeled 1-Iodobenzene. Iodobenzene can undergo Ullmann coupling reaction on copper catalyst to generate biphenyl. Iodobenzene can undergo Suzuki reaction with phenylboronic acid to generate biphenyl .
Creatinine-d5 is the deuterium labeled Creatinine. Creatinine (NSC13123) is a break-down product of creatine phosphate in muscle, and is usually produced at a fairly constant rate by the body .
Tandospirone-d8 (SM-3997-d8) is deuterium labeled Tandospirone. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms [4].
Dimethylamine-d6 hydrochloride is a deuterium labeled Dimethylamine hydrochloride. Dimethylamine hydrochloride is the immediate precursor of dimethylnitrosamine, a known potent carcinogen in a wide variety of animal species .
Terbinafine-d3 (TDT 067-d3) is deuterium labeled Terbinafine. Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
Goserelin-d10 (ICI 118630-d10) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
Pazopanib-d3 (GW786034-d3) is deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Fluorofenidone-d3 (AKF-PD-d3) is deuterium labeled Fluorofenidone (AKF-PD) (HY-121246). Fluorofenidone is an orally active compound with anti-fibrotic, antioxidant, and anti-inflammatory pharmacological effects. Fluorofenidone downregulates the expression of ACSL4, upregulates GPX4 expression and inhibits the NF-κB signaling pathway to alleviate inflammation and fibrosis. Fluorofenidone ameliorates cholestasis and fibrosis by inhibiting hepatic Erk/-Egr-1 signaling and Tgfβ1/Smad pathway in mice. Fluorofenidone demonstrates protective effects against chronic lung injury in mice. Fluorofenidone can be used for the study of chronic obstructive pulmonary disease (COPD), pulmonary interstitial fibrosis (PIF) and non-small cell lung cancer (NSCLC) .
Penicillin V-d5 (potassium) is the deuterium labeled Penicillin V Potassium . Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis [4] .
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Methoxyamine-d3 (O-Methylhydroxylamine-d3) hydrochloride is the deuterium labeled Methoxyamine hydrochloride. Methoxyamine hydrochloride is an orally active and potent base excision repair (BER) inhibitor .
Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Albendazole-d3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a agent indicated for the treatment of a variety of worm infestations .
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
Nirmatrelvir-d6 (PF-07321332-d6) is deuterium labeled Nirmatrelvir. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker . Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure . Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome .
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
Capsaicin-d3 is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects[1][2].
Povorcitinib-d6 (INCB54707-d6) is the deuterium labeled Povorcitinib (HY-145588). Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) .
Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
Benzyl alcohol-d7 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Ambroxol-d5 (hydrochloride) is the deuterium labeled Ambroxol hydrochloride. Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research .
Ethopabate-d5 (Ethyl pabate-d5) is the deuterium labeled Ethopabate (HY-B2138). Ethopabate (Ethyl pabate) is an orally active antiparasitic agent. Ethopabate is often used in combination with Amprolium hydrochloride (HY-B0937A) and others to prevent and treat poultry coccidiosis, leucosis, and other diseases .
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist .
Selinexor-d5 (KPT-330-d5) isthe deuterium labeled Selinexor (HY-17536). Selinexor (KPT-330), an analog of KPT-185, is an orally active and selective CRM1 inhibitor .
Bifenox-d3 is the deuterium labeled Bifenox. Bifenox (MC-4379) is a nitrophenyl ether herbicide. Bifenox disrupts cellular membrane, inhibits photosynthesis and inhibits the protoporphyrinogen oxidase. Bifenox increases the ROS production in the microalgae Chlamydomonas reinhardtii .
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Apalutamide-d3 is the deuterium labeled Apalutamide . Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM .
Trifloxystrobin-d6 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h .
Tadalafil-d3 is the deuterium labeled Nortadalafil. Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea .
Celecoxib-d7 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM .
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator [4].
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
Abemaciclib-d8 is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
Ditiocarb-d10 (Diethyldithiocarbamic acid-d10) is the deuterium labeled Ditiocarb (HY-126363) . Ditiocarb (Diethyldithiocarbamic acid) is an accelerator of the rate of copper cementation. Ditiocarb (Diethyldithiocarbamic acid) reduces the incidence of HIV infection, and also enhances adjuvant immunoresearch of high risk breast cancer [4].
Emtricitabine-d2 (BW1592-d2) is deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Dimethyl phthalate-d6 is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins .
Remdesivir-d5 (GS-5734-d5) is a deuterium labeled Remdesivir (HY-104077). Remdesivir (GS-5734) is a nucleoside analogue with effective antiviral activity. Remdesivir can inhibit the synthesis of viral DNA or RNA. Remdesivir can be used for the research of infection, such as SARS-CoV and MHV infection .
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Capsaicin-d7 is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects .
Omeprazole-d6 (H 16868-d6) is deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Parecoxib-d3 is the deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor . N-ethylmaleimide specific inhibits phosphate transport in mitochondria . N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor .
Eprinomectin-d3 (MK-397-d3) is the deuterium-labeled Eprinomectin (HY-12643). Eprinomectin is a type of avermectin. Eprinomectin，as a broad-spectrum fungicide，has insecticidal，insecticidal and acaricidal activities. Eprinomectin induces apoptosis and autophagy in prostate cancer cells and has antitumor activity .
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM .
Flurbiprofen-d3 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
Glyceryl monostearate-d5 (GMS-d5) is deuterium labeled Glyceryl monostearate. Glyceryl monostearate (GMS) is a single-tailed lipidic monoglyceride that can be used to synthesize nanoliposomes for drug delivery .
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al) .
Puromycin-d3 (dihydrochloride) is the deuterium labeled Puromycin dihydrochloride. Puromycin dihydrochloride (CL13900 dihydrochloride), an aminonucleoside antibiotic, inhibits protein synthesis .
Enalapril-d3 (MK-421-d3) is deuterium labeled Enalapril. Enalapril (MK-421) is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research .
Olmesartan-d6 (RNH-6270-d6) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure .
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .
Vapendavir-d5 is the deuterium labeled Vapendavir. Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
Flurbiprofen-d5 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
Aspartame-d3 is the deuterium labeled Aspartame. Aspartame (SC-18862) is a methyl ester of a dipeptide. Aspartame can be used as a synthetic nonnutritive sweetener. Aspartame is composed of phenylalanine (50%), aspartic acid (40%) and methanol (10%) .
Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium labeled Oxybenzone (HY-A0067). Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells .
Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity .
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Rupintrivir-d7 is a deuterated labeled Rupintrivir . Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect .
Goserelin-d7 (ICI 118630-d7) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Simvastatin-d6 (MK 733-d6) is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
Ertugliflozin-d5 is the deuterium labeled Ertugliflozin . Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2 . Has the potential for the treatment of type 2 diabetes mellitus .
Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Riociguat-d3 (BAY 632521-d3) is deuterium labeled Riociguat. Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
Methoprene-d7 is the deuterium labeled Methoprene . Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist .
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Chenodeoxycholic acid-d2 (CDCA-d2) is deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Teneligliptin-d5 (MP-513-d5) is deuterium labeled Teneligliptin. Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4(DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus [4] .
Spisulosine-d3 (ES-285-d3) is deuterium labeled Spisulosine (HY-13626). Spisulosine is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation. Spisulosine induces apoptosis in PC-3 and LNCaP cells .
Terbuthylazine-desethyl-d9 is the deuterium labeled Terbuthylazine-desethyl . Terbuthylazine-desethyl (Desethylterbuthylazine) is a chloro dealkylated metabolite of Terbuthylazine (a triazine herbicide) .
Probucol-d6 is deuterium labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
Deupirfenidone-d3 is the deuterium labeled Pirfenidone (HY-B0673). Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Brinzolamide-d5 (hydrochloride) is the deuterium labeled Brinzolamide hydrochloride . Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research .
Luliconazole-d3 (NND 502-d3) is deuterium labeled Luliconazole. Luliconazole (NND 502)?is a topical antifungal imidazole antibiotic with broad-spectrum and potent antifungal activity. Luliconazole can be used for the research of skin infection, including?dermatophytosis, tinea corporis, tinea pedis?et al .
Ethylenediaminetetraacetic acid-d16 is the deuterium labeled Ethylenediaminetetraacetic acid . Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds [4].
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
Cefditoren-d3 (sodium) (ME 1206-d3) is deuterium labeled Cefditoren (sodium). Cefditoren sodium (ME 1206) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren sodium has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren sodium can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections .
Quabodepistat-d7 (OPC-167832-d7) is deuterium labeled Quabodepistat. Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with?an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis?caused by?Mycobacterium tuberculosis .
Azimilide-d8 (NE-10064-d8) dihydrochloride is the deuterium labeled Azimilide dihydrochloride (HY-18600A). Azimilide dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation [4].
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
Lauryl benzalkonium-d5 chloride (Dimethylbenzyllaurylammonium-d5 chloride) is the deuterium labeled Lauryl benzalkonium chloride (HY-B1549). Lauryl benzalkonium (Dimethylbenzyllaurylammonium) chloride is a cationic surfactant that may produce some irritant contact dermatitis (ICD) to the skin .
Mexiletine-d3 (KOE-1173-d3) is deuterium labeled Mexiletine. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research [4] .
Tonabersat-d6 (SB-220453-d6) is deuterium labeled Tonabersat. Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system .
Losartan-d6 hydrochloride is deuterated labeled Losartan potassium (HY-17512A). Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis [4] .
Valsartan-d3 is the deuterium labeled Valsartan . Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
Solabegron-d8 (GW 427353-d8) is deuterium labeled Solabegron. Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM . Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome .
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity .
Varespladib-d7 (LY315920-d7) is a deuterated labeled Varespladib (HY-13402). Varespladib is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM .
Oseltamivir-d3 (phosphate)eis the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Mycophenolic acid-d3 (Mycophenolate-d3) is deuterium labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
Amitraz-d6 (BTS-27419-d6) is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
DL-dithiothreitol-d10 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. When DL-dithiothreitol is oxidized, it forms a stable six-membered ring with an internal disulfide bond .
Crizotinib-d8 (PF-02341066-d8) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514) . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
Fostemsavir-d8 (BMS-663068-d8) is deuterium labeled Fostemsavir. Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.
Nemonoxacin-d3 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
1-Octanol-d2 is the deuterium labeled 1-Octanol . 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Enasidenib-d6 (AG-221-d6) is the deuterium labeled Enasidenib (HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
Ribociclib-d6 (LEE011-d6) is a deuterium labeled Ribociclib (HY-15777). Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Hydroxymetronidazole-d2 is the deuterium labeled Hydroxymetronidazole(HY-136440).Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle .
Imeglimin-d3 (EMD 387008-d3) is deuterium labeled Imeglimin. Imeglimin (EMD 387008) is an oral glucose-lowering agent. Imeglimin improves insulin sensitivity. Imeglimin also reduces reactive oxygen species (ROS) production, increases mitochondrial DNA and improves mitochondrial function .
Omeprazole-d3 (H 16868-d3) is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
Ambroxol-d5 (NA-872-d5) is deuterium labeled Ambroxol. Ambroxol (NA-872), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research .
Ampyrone-d3 is the deuterium labeled Ampyrone (HY-B1398). Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy .
Piroxicam-d3 (CP-16171-d3) is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively .
Debutyldronedarone-d7 is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans.Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent .
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205) .
Eltrombopag-d3 (SB-497115-d3) is deuterium labeled Eltrombopag. Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well [4] .
Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
Prasugrel-d3 is the deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Glycoursodeoxycholic acid-d5 (Ursodeoxycholylglycine-d5) is the deuterium labeled Glycoursodeoxycholic acid (HY-N1424). Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid.
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
Ivacaftor-d18 is the deuterium labeled Ivacaftor . Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively .
Alfuzosin-d6 (SL 77499-d6) is deuterium labeled Alfuzosin. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) .
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
Ivosidenib-d5 (AG-120-d5) is deuterium labeled Ivosidenib. Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
Naproxen-d3 is the deuterium labeled Naproxen. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ethaboxam-d5 (Intego solo-d5) is the deuterium labeled Ethaboxam (HY-107492). Ethaboxam is a β-tubulin inhibitor that can be used as anti-oomycete fungicide .
Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Ergothioneine-d3 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant .
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) [4] .
Pirfenidone-d5 (AMR69-d5) is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
Sotalol-d6 is the deuterium labeled Sotalol. Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent [4].
Diflunisal-d3 is the deuterium labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
Methylprednisolone-d3 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels .
Famciclovir-d6 (BRL 42810-d6) is deuterium labeled Famciclovir. Famciclovir (BRL 42810) is an orally active nucleoside analogue. Famciclovir is an antiviral agent with potent activities against HBV, HSV and VZV. Famciclovir can be used for the research of herpesvirus infection .
2-Acetamidophenol-d3 (Orthocetamol-d3) is the deuterium labeled 2-Acetamidophenol (HY-W015600). 2-Acetamidophenol (Orthocetamol) is a regulator that targets ferroptosis and glutathione metabolic pathways, is the ortho-regioisomer of Paracetamol (HY-66005). 2-Acetamidophenol has anti-atherosclerotic activity, and inhibiting total cholesterol (TC) and triglyceride (TG) in a zebrafish hyperlipidemia model with IC50s for 30 μM and 40 μM, respectively. 2-Acetamidophenol upregulates the expression of glutathione synthesis-related genes (such as GCLC, GCLM, GSS) and iron ion transport genes (such as FPN1, FTH), reduces the accumulation of intracellular reactive oxygen species (ROS) and ferrous ions (Fe2+), and enhances the activity of glutathione peroxidase GPX4, thereby inhibiting macrophage phagocytosis of oxidized low-density lipoprotein (ox-LDL) and foam cell formation .
Afloqualone-d7 (HQ-495-d7) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome .
Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9) is the deuterium labeled Tylvalosin (HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
Ciprofloxacin-d8 (hydrochloride) is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Ropinirole-d7 hydrochloride is the deuterium labeled Ropinirole hydrochloride . Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Linezolid-d3 (PNU-100766-d3) is a deuterium labeled Linezolid (PNU-100766). Linezolid is a synthetic antibiotic that acts by inhibiting the initiation of bacterial protein synthesis .
Anisylacetone-d5 (p-Methoxybenzylacetone-d5) is deuterium labeled Anisylacetone. Anisylacetone (p-Methoxybenzylacetone) is a male fruit fly attractant .
Niclosamide-d3 (BAY2353-d3) is deuterium labeled Niclosamide. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells [4]. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction [4].
Dapoxetine-d7 (hydrochloride) is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI) .
Lusutrombopag-d13 is deuterium labeled Lusutrombopag. Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
Valdecoxib-d3 is the deuterium labeled Valdecoxib. Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain .
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Chenodeoxycholic Acid-d7 (CDCA-d7) is the deuterium labeled Chenodeoxycholic Acid (HY-76847). Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor .
Relebactam-d9 (MK-7655-d9) is deuterium labeled Relebactam. Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases and KPC) and class C (AmpC) enzymes. Relebactam shows antibacterial activity .
(±)-Duloxetine-d3 (hydrochloride) is deuterium labeled (±)-Duloxetine (hydrochloride). (±)-Duloxetine ((Rac)-Duloxetine) hydrochloride is the racemate of Duloxetine hydrochloride. Duloxetine hydrochloride, a serotonin-norepinephrine reuptake inhibitor, can be used for diabetic neuropathic pain and fibromyalgia as well as major depressive disorder research .
Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Niraparib-d5 (MK-4827-d5) is the deuterium labeled Niraparib (HY-10619). Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
Telcagepant-d8 (MK-0974-d8) is deuterium labeled Telcagepant. Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
Pazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Vericiguat-d6 (BAY1021189-d6) is deuterium labeled Vericiguat. Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase stimulator.
Ozenoxacin-d3 (hydrochloride) is the deuterium labeled Ozenoxacin hydrochloride. Ozenoxacin hydrochloride is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections .
Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
Penicillamine-d3 is the deuterium labeled Penicillamine. Penicillamine (D-(-)-Penicillamine) is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.
Triclabendazole-d3 is the deuterium labeled Triclabendazole (HY-B0621). Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors .
Pimozide-d5 (R6238-d5) is the deuterium labeled Pimozide (HY-12987). Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
Isoeugenol-d3 is deuterated labeled Isoeugenol (HY-N1952). Isoeugenol is an essential oil constituent of nutmeg, clove, and cinnamon. Isoeugenol inhibits growth of Escherichia coli and Listeria innocua with MICs of 0.6 mg/mL and 1 mg/mL, respectively .
Glycocyamine-d2 is the deuterium labeled Glycocyamine. Glycocyamine (Guanidinoacetic acid), a precursor of creatine, is a replacement of dietary arginine and could support overall energy homeostasis of the bird.
Brigatinib-d11 (AP-26113-d11) is deuterium labeled Brigatinib. Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC .
Ziprasidone-d88 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Albendazole-d7 is the deuterium labeled Albendazole. Albendazole is a broad-spectrum parasiticide with high effectiveness and low host toxicity. Albendazole is used for the research gastrointestinal parasites in humans and animals .
Eugenol acetate-d3 is the deuterated labeled Eugenol acetate (HY-W014612). Eugenol acetate (Eugenyl acetate) is an antibacterial, anticancer, anti-inflammatory and antioxidant. Eugenol acetate inhibits NF-κB and enhances the expression of p53 and p21 (WAF1). Eugenol acetate can prevent chemically induced skin cancer, inhibit cancer cell proliferation and induce apoptosis [4].
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Dexpanthenol-d6 is deuterium labeled D-Panthenol. D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .
Equilin-d2 (7-Dehydroestrone-d2) is deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism .
Ropinirole-d3 hydrochloride is the deuterium labeled Ropinirole hydrochloride . Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
DL-Arginine-d7 hydrochloride is deuterium labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Valsartan-d9 is deuterium labeled valsartan. Valsartan is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Biperiden-d5 (hydrochloride) is the deuterium labeled Biperiden hydrochloride. Biperiden (KL 373) hydrochloride is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
Nadifloxacin-d5 (OPC7251-d5) is deuterium labeled Nadifloxacin (HY-B0506). Nadifloxacin (OPC7251) is a broad-spectrum quinolone antibiotic. Nadifloxacin inhibits bacterial DNA gyrase and topoisomerase IV, interfering with DNA replication. It also suppresses the production of proinflammatory cytokines (such as IL-1α, IL-6, and IL-8). Nadifloxacin exhibits antibacterial activity against various pathogens, including Propionibacterium acnes and Staphylococcus aureus. Nadifloxacin also exhibits anti-inflammatory activity. Nadifloxacin can be used in the research of skin infections such as acne vulgaris, folliculitis, and impetigo [4] .
Tulobuterol-d9 (hydrochloride) is the deuterium labeled Tulobuterol. Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength .
Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4(M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
Tezacaftor-d6 (VX-661-d6) is deuterium labeled Tezacaftor. Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation [4].
Norfloxacin-d8 is the deuterium labeled Norfloxacin. Norfloxacin (MK-0366) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
Omeprazole sulfide-d3 is the deuterium labeled Omeprazole sulfide. Omeprazole metabolite Omeprazole sulfide (Ufiprazole) is a metabolite of Omeprazole, which is a proton pump inhibitor.
Tiludronate-d5 (sodium)mis the deuterium labeled Tiludronate disodium. Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties [4].
Ceftazidime-d5 is the deuterium labeled Ceftazidime. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
Methotrexate metabolite-d3 is the deuterium labeled Methotrexate metabolite. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent .
Ramelteon-d3 (TAK-375-d3) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.
Eliglustat-d15 (Genz 99067-d15) is deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM .
DL-dithiothreitol-d6 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
Olodaterol-d3 hydrochloride (BI1744-d3 hydrochloride) is the deuterium labeled Olodaterol hydrochloride (HY-14301A). Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis .
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
Diltiazem-d6 (hydrochloride) (CRD-401-d6 (hydrochloride)) is deuterium labeled Diltiazem (hydrochloride). Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
Sucrose-d14 is the deuterium labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preferen
Chlortetracycline-d6 (hydrochloride) is the deuterium labeled Chlortetracycline hydrochloride. Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
Empagliflozin-d6 (BI 10773-d6) is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2 .
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes .
Ribociclib-d6 (LEE011-d6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Vilanterol-d12 (GW642444-d12) is deuterium labeled Vilanterol. Vilanterol (GW642444) is a long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM .
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor [4] .
DL-Phenylephrine-d3 hydrochloride ((±)-Phenylephrine-d3 hydrochloride) is the deuterium labeled DL-Phenylephrine hydrochloride (HY-W014726). DL-Phenylephrine ((±)-Phenylephrine) hydrochloride is a selective agonist of the alpha1-adrenergic receptor, exhibiting potent vasoconstrictive activity.
Dronedarone-d6 (SR 33589-d6) is deuterium labeled Dronedarone. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4 .
Tenidap-d3 is the deuterium labeled Tenidap. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties . Tenidap is also a specific SLC26A3 inhibitor .
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker .
Etiracetam-d3 is the deuterium labeled Etiracetam. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .
Pemigatinib-d6 (INCB054828-d6) is deuterium labeled Pemigatinib. Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma .
Tetramethylthiuram Monosulfide-d12 (TMTM-d12) is the deuterium labeled Tetramethylthiuram monosulfide (HY-W020246). Tetramethylthiuram monosulfide (TMTM) is an active compound. Tetramethylthiuram monosulfide (TMTM) can be used for the research of rubber and various biochemical studies .
Medetomidine-d3 (hydrochloride) is the deuterium labeled Medetomidine hydrochloride. Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor .
Nicardipine-d3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure .
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Radotinib-d6 is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases .
Moxonidine-d3 (BDF5895-d3) is deuterium labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis [4] .
Dimesna-d8 (BNP-7787-d8) is the deuterium labeled Dimesna (HY-B1022). Dimesna combined with anticancer chemotherapeutic agents to reduce nephrotoxicity.
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Aripiprazole-d8 (OPC-14597-d8) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.
Ribociclib-d8 is the deuterium labeled Ribociclib . Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex .
Itraconazole-d9 is the deuterium labeled Itraconazole . Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor [4] .
Cilnidipine-d7 is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel [4]. Antihypertensive effects .
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
Ciprofloxacin-d8 (hydrochloride monohydrate) is the deuterium labeled Ciprofloxacin (hydrochloride monohydrate). Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Raltegravir-d3 (potassium) is the deuterium labeled Raltegravir potassium. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection .
Sodium 2-oxopropanoate-d3 is the deuterium labeled Sodium 2-oxopropanoate . Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS .
Terbinafine-d3 hydrochloride is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM . Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria .
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Isoxepac-d6 (HP 549-d6) is the deuterium labeled Isoxepac (HY-W050088). Isoxepac (HP 549) is an orally active non-steroidal anti-inflammatory agent. Isoxepac can inhibit Carrageenan (HY-125474) paw oedema, adjuvant-induced polyarthritis, and prostaglandin synthesis. Isoxepac (200 mg) has an analgesic effect after meniscectomy with a low incidence of side effects. Isoxepac can be used in the research of inflammatory (rheumatoid arthritis) and pain-related diseases .
Ciprofloxacin-d8 is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Acetohydrazide-d3 (Ethanehydrazonic acid-d3) is deuterium labeled Acetohydrazide. Acethydrazide is an organic building that undergo catalytic hydrogenation to produce N′-methyl acethydrazide (MAH) .
Imiquimod-d7 (R 837-d7) is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Acetylpyrazine-d3 is deuterated labeled Acetylpyrazine (HY-W007692). Acetylpyrazine (2-Acetylpyrazine) is used to form many polycyclic compounds, as useful structures in pharmaceuticals and perfumes. Acetylpyrazine is a component of the folates (vitamin B compounds) .
HMMNI-d3 (Hydroxy Dimetridazole-d3) is deuterium labeled HMMNI (HY-W008216). HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazol (HY-B1244). Dimetridazole is a nitroimidazole class agent that combats protozoan infections .
Sildenafil-d5 (UK-92480-d5) is deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) [4] .
Debutyldronedarone-d6 (hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent .
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [4].
Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth .
Venlafaxine-d9 (Wy 45030-d9) is a deuterium labeled Venlafaxine (HY-B0196). Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
Valsartan-d8 is the deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Posaconazole-d7 (SCH 56592-d7) is deuterium labeled Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Danicamtiv-d3 (MYK-491-d3) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
Mexiletine-d6 (KOE-1173-d6) is deuterium labeled Mexiletine. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research [4] .
Methylprednisolone-d7 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels .
Elesclomol-d2 (STA-4783-d2) is a deuterium labeled Elesclomol (HY-12040). Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research [4].
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
Ensifentrine-d6 (RPL-554-d6) is deuterium labeled Ensifentrine. Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
Selpercatinib-d3 (LOXO-292-d3) is deuterium labeled Selpercatinib. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity .
Sarafloxacin-d8 (A-56620-d8) hydrochloride is the deuterium labeled Sarafloxacin hydrochloride. Sarafloxacin hydrochloride (A-56620 hydrochloride) is a quinolone antibiotic drug.
Cilostazol-d2 (OPC 13013-d2) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM . Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria .
Cilostazol-d6 (OPC 13013-d6) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors [4].
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Posaconazole-d3 (SCH 56592-d3) is deuterium labeled Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
Ketoprofen-d3 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively .
Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .
Carteolol-d9 (hydrochloride) is the deuterium labeled Carteolol hydrochloride. Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma .
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
Lisinopril-d5 is the deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation [4] .
Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Atenolol-d7 is the deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris .
Tazarotene-d8 is the deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris .
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis .
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment .
Donepezil-d7 (hydrochloride) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .
Bendamustine-d7 hydrochloride (SDX-105-d7) is the deuterium labeled Bendamustine hydrochloride (HY-B0077). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties .
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule?depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of?bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity .
Adinazolam-d5 (U 41123-d5) is a deuterium labeled Adinazolam (HY-A0198). Adinazolam is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities .
Puromycin-d3 is the deuterium labeled Puromycin. Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
Betaxolol-d7 (hydrochloride) is the deuterium labeled Betaxolol hydrochloride. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
Ethylenediaminetetraacetic acid-d12 is the deuterium labeled Ethylenediaminetetraacetic acid . Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds [4].
Evogliptin-d9 (DA-1229-d9) is deuterium labeled Evogliptin. Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation [4].
Elagolix-d6 (sodium) (NBI-56418-d6 (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. [4] .
Hyodeoxycholic acid-d5 is the deuterium labeled Hyodeoxycholic acid. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
Doxazosin-d8 is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors .
Sunitinib-d10 (SU 11248-d10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules .
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively) .
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor .
Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Ponatinib-d8 (AP24534-d8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Rabeprazole-d3 sodium the deuterium labeled Rabeprazole sodium (HY-B0656A). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an b>IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
Cinacalcet-d3 (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death [4] .
Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19 .
1-PalMitoyl-2-arachidoyllecithin-d9-1 (1-Palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine-d9-1) is deuterium labeled 1-PalMitoyl-2-arachidoyllecithin. 1-Palmitoyl-2-arachidonoyl-sn-glycero-3-PC (PAPC) is a phospholipid containing palmitic acid (16:0) and arachidonic acid (20:4) at the sn-1 and sn-2 positions, respectively, that is found in biological membranes. PAPC is oxidized in vivo, and its oxidation products are involved in chronic inflammation and vascular disease. PAPC has been used to study signaling of oxidized phospholipids. Levels of PAPC are decreased in isolated human multiple myeloma cells .
Sanguinarine chloride- 13C,d3 (Sanguinarin chloride- 13C,d3) is the deuterium labeled Sanguinarine chloride (HY-N0052A). Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
Bosutinib- 13C,d3 (SKI-606- 13C,d3) is 13C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively .
Iloperidone- 13C,d3 (HP 873- 13C,d3) is 13C labeled Iloperidone. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms .
dGTP- 15N5 (2'-Deoxyguanosine-5'-triphosphate- 15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Ethyl linoleate- 13C18 is the 13C labeled Ethyl linoleate. Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Adenosine 5'-diphosphate- 13C5 (Adenosine diphosphate- 13C5) is the 13C-labeled Adenosine 5'-diphosphate (HY-W010918). Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
Ethynyl Estradiol- 13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Miconazole-d5 (nitrate) (2,4-Dichlorobenzyloxy-d5) is the deuterium labeled Miconazole nitrate. Miconazole nitrate (R18134 nitrate) is an imidazole antifungal agent. Miconazole nitrate also has antibacterial effects .
(Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
Adenine- 15N5 (6-Aminopurine- 15N5; Vitamin B4- 15N5) is 15N labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Levoglucosan-d7 is the deuterium labeled Levoglucosan. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature .
Thiamine- 13C3 (hydrochloride) is the 13C-labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Nε,Nε,Nε-Trimethyllysine-d9 (chloride) is the deuterium labeled Nε,Nε,Nε-Trimethyllysine (chloride) . Nε,Nε,Nε-Trimethyllysine chloride serves as a precursor for gut flora-dependent formation of N,N,N-trimethyl-5-aminovaleric acid (TMAVA) .
Butylparaben- 13C6 is the 13C labeled Butylparaben . Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
Adenosine monophosphate- 13C10, 15N5 (AMP- 13C10, 15N5) is the 13C- and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
2'-Deoxyadenosine-5'-triphosphate- 15N5,d14 (dATP- 15N5,d14) dilithium is deuterium and 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Adenine-15N5 hydrochloride hydrate (6-Aminopurine-15N5 hydrochloride hydrate) is the deuterium labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis .
Adenine- 13C5 (6-Aminopurine- 13C5; Vitamin B4- 13C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
AalphaC- 15N3 (2-Amino-α-carboline- 15N3) is 15N labeled AalphaC. AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
L-DOPA- 13C6 is the 13C-labled L-DOPA . L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease [4].
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al [4] .
Cobimetinib- 13C6 (GDC-0973- 13C6; XL518- 13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078) . Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor .
1-Stearoyl-sn-glycero-3-phosphocholine-d35 is deuterium labeled 1-Stearoyl-sn-glycero-3-phosphocholine (HY-125771). 1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylate is the deuterium labeled Rasagiline (mesylate) (HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
N,N-dimethyl-N′-p-tolylsulfamide-d7(4-Dimethylaminosulfotoluidide-d7; N,N-Dimethyl-N-Tolylsulfonyldiamide-d7) is the deuterium labeled N,N-dimethyl-N′-p-tolylsulfamide (HY-W286414).
Dapsone- 15N2 (4,4′-Diaminodiphenyl sulfone- 15N2) is 15N labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
Dabigatran- 13C6 is the 13C labeled Dabigatran . Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
Riboflavin- 13C5 is the 13C-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Neopterin- 13C5 (D-(+)-Neopterin- 13C5; D-erythro-Neopterin- 13C5) is the deuterium labeled Neopterin (HY-W040055) . Neopterin (D-(+)-Neopterin), a catabolic product of guanosine triphosphate (GTM), serves as a marker of cellular immune system activation .
dGTP- 15N5,d14 (2'-Deoxyguanosine-5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
(±)-1,2-Propanediol- 13C3 is 13C labeled (±)-1,2-Propanediol (HY-Y0921). (±)-1, 2-propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol that is often used as an excipient in many active molecular preparations to increase the solubility and stability of the active molecule. (±)-1, 2-propanediol can affect the neurobehavior of zebrafish .
C18 Dihydroceramide-d3-1 (N-octadecaoyl-D-eytho-Dihydosphigosie-d3) is deuterium labeled C18 Dihydroceramide. C18 Dihydroceramide is an ester product .
Oseltamivir acid-13C,d3 (GS 4071-13C,d3; Ro 64-0802-13C,d3) is a 13C- and deuterium-labeled Oseltamivir acid (HY-13318). Oseltamivir acid is the active metabolite of Oseltamivir phosphate and inhibits influenza virus neuraminidase (IC50=2 nM). Oseltamivir acid is orally active and can be used to study influenza A/B infections [4] .
Artemether- 13C,d3 (Dihydroqinghaosu methyl ether- 13C,d3) is the deuterium and 13C-labeled Artemether (HY-N0402). Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria .
Menaquinone-7- 13C6 is the 13C-labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors . Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins . Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS) .
2'-Deoxycytidine-5'-monophosphoric acid- 15N3 is the 15N labeled 2'-Deoxycytidine-5'-monophosphoric acid . 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite.
Cefotiam- 13C, 15N2 (SCE-963- 13C, 15N2) is the 13C- and 15N-labeled Cefotiam (HY-B0734). Cefotiam (SCE-963) is a parenteral cephalosporin antibiotic. Cefotiam has broad-spectrum activity against Gram-positive and Gram-negative bacteria .
N6-Methyladenosine- 13C3 (6-Methyladenosine- 13C3) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities .
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels [4].
N-Acetyl mesalazine-d3-1 (N-Acetyl-5-aminosalicylic acid-d3-1) is deuterium labeled N-Acetyl mesalazine (HY-66008). N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the primary intestinal metabolite of 5-Aminosalicylic Acid (HY-15027) and serves as a biomarker for evaluating the efficacy of 5-Aminosalicylic Acid (HY-15027). N-Acetyl mesalazine can scavenge free radicals, reduce DNA base hydroxylation, and ameliorate mucosal inflammation. N-Acetyl mesalazine can be used in the study of diseases such as colitis and colon cancer .
Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death .
L-Glutathione reduced-d5 (GSH-d5) ammonium is the deuterium labeled L-Glutathione reduced (HY-D0187). L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
Exemestane- 13C,d2 is 13C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
Tofacitinib- 13C,d3 (Tasocitinib- 13C,d3) is 13C labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
ATP- 13C10, 15N5 is the 13C and 15N labeled ATP . ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation .
Mitotane- 13C6 is the 13C labeled Mitotane . Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [4] .
Uridine-13C9,15N2 (β-Uridine-13C9,15N2) is 13C and 15N labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Zearalenone- 13C7 (Mycotoxin F2- 13C7) is 13C labeled Zearalenone. Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts .
Cytidine-d2-1 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catech
Ethyl Paraben- 13C6 (Ethyl parahydroxybenzoate- 13C6) is 13C labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Betaine- 13C3 (Trimethylglycine- 13C3) is the 13C labeled isotope of Betaine (HY-B0710). Betaine (Trimethylglycine) is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns [1,2]. Betaine is found ubiquitously in plants, animals, microorganisms, and rich dietary sources including seafood, spinach, and wheat bran. Betaine also acts as an osmolyte, to maintain the avian’s cellular water and ion balance to improve the avian’s capacity against heat stress via preventing dehydration and osmotic inactivation. It helps in maintaining the protective osmolytic activity, especially in heat-stressed birds. Betaine may promote various intestinal microbes against osmotic variations and thus improve microbial fermentation activity .
Ritonavir- 13C,d3 is the 13C- and deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Folic acid-13C6 is a deuterated labeled Folic acid . Folic acid (Vitamin B9) is a orally active essential nutrient from the B complex group of vitamins. Folic acid shows antidepressant-like effect. Folic acid sodium reduces the risk of neonatal neural tube defects. Folic acid can be used to the research of megaloblastic and macrocytic anemias due to folic deficiency [4] .
L-Ascorbic acid- 13C6 is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor . L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells [4].
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor . Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
17α-Hydroxyprogesterone- 13C3 is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
rU Phosphoramidite- 13C2,d1 (DMT-2'O-TBDMS-rU phosphoramidite- 13C2,d1) is deuterium and 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Folic acid- 13C5 is the 13C-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
D-Mannitol- 13C,d2 is the deuterium and 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells [4] . D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed .
Ornidazole- 13C2, 15N2 is the 13C, 15N labeled Ornidazole. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease .
N-Acetylneuraminic Acid- 13C,d3 (N-Acetyl-β-D-neuraminic acid- 13C,d3) is the deuterium labeled and 13C-labeled N-Acetyl-β-D-neuraminic acid (HY-75278).
Levulinic acid- 13C3 (4-Oxovaleric acid- 13C) is the 13C-labeled Levulinic acid (HY-Y0839). Levulinic acid is a precursor for the synthesis of biofuels, such as ethyl levulinate. Levulinic acid is also a 5-keto-pentanoic acid. Levulinic acid can be utilized by the cells as a cosubstrate for biopolymer synthesis. Levulinic acid can be used in antibacterial research .
Zearalenone- 13C18 (Mycotoxin F2- 13C18; Toxin F2- 13C18) is the 13C labeled Zearalenone (HY-103447) . Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts .
Mandelic Acid- 13C8 ((±)-Mandelic acid- 13C8) is the 13C-labeled Mandelic acid (HY-W015591). Mandelic acid ((±)-Mandelic acid), an alpha-hydroxycarboxylic acid, has been widely used as an intermediate of pharmaceutical and fine chemicals. Mandelic acid shows antimicrobial activity and has been used for the research of urinary tract infections and vaginal trichomoniasis. Mandelic acid exhibits high sperm-immobilizing activity and low vaginal irritation .
Doxorubicinone- 13C,d3 (Adriamycin aglycone- 13C,d3) is 13C labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects .
Uridine 5'-monophosphate- 15N2,d11 (5'- Uridylic acid- 15N2,d11) dilithium is deuterium and 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa [4] .
Mitotane- 13C12 (2,4′-DDD- 13C12) is 13C labeled Mitotane. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [4][4] .
Propyl paraben- 13C6 (Propyl parahydroxybenzoate- 13C6) is 13C labeled Propylparaben. Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods. Propylparaben disrupts follicular growth and steroidogenic function by altering cell cycle, apoptosis and steroidogenic pathways. Propylparaben also reduced sperm count and motility in rats [4] .
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
Trans-Anethole-d3 is deuterated labeled Trans-Anethole (HY-N0367). Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor [4] .
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
Tricaine-d5 methanesulfonate is the deuterium labeled Tricaine methanesulfonate (HY-W011777). Tricaine methanesulfonate (MS-222) is a commonly used agent that can suppress or relieve pain. agent for immobilization of aquatic species. Tricaine methanesulfonate, the most widely used agent that can suppress or relieve pain. in fish, has been shown to induce embryotoxic effects in zebrafish .
Phenylglyoxylic acid-d5 (Benzoylformic acid-d5) is a deuterium labeled Phenylglyoxylic acid (HY-W010255). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human. Phenylglyoxylic acid can be used as drug intermediate for synthesis of antineoplastic compounds .
2,6-Dimethoxyphenol-d6 (Syringol-d6) is deuterated labeled 2,6-Dimethoxyphenol (HY-W003972). 2,6-Dimethoxyphenol is a phenolic compound that scavenges free radicals and exhibits antioxidant activity. 2,6-Dimethoxyphenol is the substrate for determining laccase activity .
Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Hydroxy Itraconazole-d6 (R-63373-d6) is deuterium labeled Hydroxy Itraconazole. Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
Pentyl 4-hydroxybenzoate-d11 (Amylparaben-d11) is the deuterium labeled Pentyl 4-hydroxybenzoate (HY-W267444). Pentyl 4-hydroxybenzoate (Amylparaben) is a type of paraben compound commonly used as a preservative, it has antibacterial properties and is related to the inhibition of induced oxygen consumption .
(Rac)-Levomepromazine-d3 (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors .
Ornidazole-d5 is deuterium labeled Ornidazole. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease .
Octanoic acid-d15 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Lignoceric acid-d3 is the deuterium labeled Lignoceric acid . Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research .
Piperonyl butoxide-d9 is the deuterium labeled Piperonyl butoxide.Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice [4].
Amifampridine-d3(3,4-Diaminopyridine-d3) is deuterium labeled Amifampridine. Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research .
Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8 .
Nanofin-d2 (2,6-Lupetidine-d2) is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
CX516-d10 is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) .
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Metazachlor-d6 (BAS 479H-d6) is a deuterium labeled Metazachlor (HY-136373). Metazachlor (BAS 479H) is a herbicide belonging to the chloroacetamides class. Metazachlor can inhibit the synthesis of very long chain fatty acids during the germination and emergence of weed seeds, thereby interfering with cell division and tissue differentiation, and thus hindering the normal growth and development of weeds .
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Farnesyl pyrophosphate-d3 (Farnesyl diphosphate-d3) is a deuterium labeled Farnesyl pyrophosphate (HY-113037B). Farnesyl pyrophosphate is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
Aripiprazole (1,1,2,2,3,3,4,4-d8) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM .
Deruxtecan-d5 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
DPPC-d66 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Alfuzosin-d7 (hydrochloride) is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Scopolamine-d3 hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc [4] .
Djalonensone-d3 is a deuterium labeled Djalonensone (HY-W013863). Djalonensone, isolated from the roots of Anthocleista djalonensis (Loganiaceae), is an important taxonomic marker of the plant species .
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Cariprazine-d8-1 (RGH-188-d8-1) is the deuterium labeled Cariprazine (HY-14763). Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma .
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
Stigmasterol-d5-1 is deuterium labeled Stigmasterol. Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases .
Ketotifen-d3 (HC 20-511-d3) is deuterium labeled Ketotifen. Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention [4].
DPPC-d75 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Nonanoic acid-d3 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Cyfluthrin-d6 (β-Cyfluthi-d6) is deuterium labeled Cyfluthrin. Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product .
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
trans-Stilbene-d10 ((E)-Stilbene-d10) is the deuterium labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
D-Leucine-d10 is the deuterium labeled D-Leucine. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro .
Arachidic acid-d2 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Parecoxib-d5 sodium is the deuterium labeled Parecoxib sodium. Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo .
Levocarnitine propionate-d9 hydrochloride (L-Propionylcarnitine-d9 chloride) is deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride is used to study diseases such as renal function deterioration, congestive heart failure, and intermittent claudication .
Homovanillic acid-d5 (Vanilacetic acid-d5) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage .
N-Arachidonylglycine-d8 is a deuterated labeled N-Arachidonylglycine . N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration .
Banoxantrone-d12 is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Vortioxetine-d3 (Lu AA 21004-d3) is a deuterium labeled Vortioxetine (HY-15414). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
Tenofovir alafenamide-d6 (GS-7340-d6) is deuterium labeled Tenofovir alafenamide. Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor .
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
Dabigatran etexilate-d11 (BIBR 1048-d11) is the deuterium labeled Dabigatran etexilate (HY-10274). Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation .
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
Apixaban-d3 (BMS-562247-01-d3) is the deuterium labeled Apixaban (HY-50667) . Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590), is the first deuterium approved worldwide for the research of Huntington's disease, or other hyperkinetic movement disorders .
Nimodipine-d7 is the deuterium labeled Nimodipine. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders .
Fosetyl-aluminum-d15 (Fosetyl-Al-d15) is the deuterium labeled Fosetyl-aluminum. Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops .
Prednisolone acetate-d8 is the deuterium labeled Prednisolone acetate. Prednisolone acetate (Prednisolone 21-acetate) is an adrenal cortico hormones, with anti-inflammatory, anti-allergic and immune suppressive effects.
Docosanoic acid-d2 (Behenic acid-d2) is deuterium labeled Docosanoic acid (HY-W013049).
Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Lignoceric acid-d47 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research .
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
N-Desbutyl bupivacaine-d6 (Desbutylbupivacaine-d6) is the deuterium labeled N-Desbutyl Bupivacaine (HY-W045132). N-Desbutyl Bupivacaine (compound 100) is a metabolite of Bupivacaine (HY-B0405), an NMDA receptor inhibitor and SCN5A antagonist .
(S)-(+)-Ibuprofen-d3 is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects .
Taurocholic acid-d5 (Taurocholic Acid-d5) is deuterium labeled Taurocholic acid. Taurocholic acid (N-Choloyltaurine) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid has immunoregulation effect .
Farnesyl pyrophosphate-d6 (Farnesyl diphosphate-d6) is a deuterium labeled Farnesyl pyrophosphate (HY-113037B). Farnesyl pyrophosphate is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Decanoyl-L-carnitine-d3 ((-)-Decanoylcarnitine-d3) is deuterium labeled Decanoyl-L-carnitine. Decanoyl-L-carnitine has stimulatory effect on the formation of desaturated fatty acid metabolites from both [1- 14C]-22:4 (n-6) and [1- 14C]-22:5 (n-3) .
Granisetron-d6 (BRL 43694-d6) is deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
2,6-Dimethoxyphenol-d3 (Syringol-d3) is the deuterium labeled 2,6-Dimethoxyphenol (HY-W003972) . 2,6-Dimethoxyphenol is a phenolic compound that scavenges free radicals and exhibits antioxidant activity. 2,6-Dimethoxyphenol is the substrate for determining laccase activity .
Azelaic acid-d14 is the deuterium labeled Azelaic acid . Azelaic acid is an organic compound produced by the ozonolysis of oleic acid;component of a number of hair and skin conditioners .
L-Valine-d1 ((S)-Valine-d1) is the deuterium labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
(S)-Lisinopril-d5 (sodium) (MK-521-d5 (sodium)) is deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
1-Phenylpyrrole-d9 (N-Phenylpyrrole-d9) is the deuterium labeled 1-Phenylpyrrole (HY-124891). 1-Phenylpyrrole (N-Phenylpyrrole) has dual fluorescent properties. 1-Phenylpyrrole displays a single band in nonpolar solvents and a second red-shifted fluorescent band in polar solvents .
Homovanillic acid-d3 (Vanilacetic acid-d3) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
N-(2,6-Dimethylphenyl)-2-(piperazin-1-yl)acetamide-d6 (N-[(2-chlorophenyl)carbamoyl]phenylalanine-d6) is deuterium-labeled CVT-2738 (HY-W009512). CVT-2738 is an orally active metabolite of Ranolazine (HY-B0280). CVT-2738 has a protective effect against isoprenaline (HY-108353)-induced myocardial ischemia in mice. CVT-2738 can be used in myocardial ischemia research .
Octanoic acid-d3 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .
1-Eicosanol-d41 (Arachidyl alcohol-d41) is the deuterium labeled 1-Eicosanol (HY-W004263) . 1-Eicosanol is a natural compound with antioxidant activity found in Justicia insularis leaves. 1-Eicosanol can be used as an antioxidant .
Mometasone furoate-d3 is a deuterium labeled Mometasone furoate. Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity .
Veratrole-d6 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Cyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
Prednisone acetate-d3 is the deuterium labeled Prednisone acetate. Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties .
Octanoic acid-d2 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Propofol-d14 (2,6-Diisopropylphenol-d14) is the deuterium labeled Propofol (HY-B0649). Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
Oxcarbazepine-d8-1 is a deuterium of Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Oxcarbazepine-d8-1 has anti-cancer and anticonvulsant effects .
Cilazapril-d5 (Ro 31-2848-d5) trifluoroacetate is the deuterium labeled Cilazapril (HY-A0043). Cilazapril is an angiotensin-converting enzyme (ACE) inhibitor used for the study of hypertension and congestive heart failure.
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
Ethyl acetoacetate-d5 is the deuterium labeled Ethyl acetoacetate . Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds [4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm .
L-Arginine-d7 (hydrochloride) is the deuterium labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Octanoic acid-d5 is the deuterium labeled Octanoic acid . Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Eslicarbazepine-d3 (BIA 2-194-d3) is the deuterium labeled Eslicarbazepine (HY-114703). Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
Uridine-d12 (β-Uridine-d12) is the deuterium labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Docosanoic acid-d43 (Behenic acid-d43) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
Taurochenodeoxycholic acid-d5 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
Deruxtecan-d2 is the deuterium labeled Deruxtecan (HY-13631E) . Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
eCF506-d5 (NXP900-d5) is deuterated labeled eCF506 (HY-112096). eCF506 is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer .
Ulipristal acetate-d3 (CDB-2914-d3) is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma .
Pyridoxal Phosphate-d3 is the deuterium labeled Pyridoxal 5'-phosphate. Pyridoxal 5'-phosphate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′-phosphate (PMP) .
Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). Carbidopa, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
Nanofin-d5 (2,6-Lupetidine-d5) is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
Calcium phosphorylcholine-d9 (chloride) is the deuterium labeled Calcium phosphorylcholine chloride. Calcium phosphorylcholine chloride is the main phospholipid component in eukaryotic biofilms. Calcium phosphorylcholine chloride exists in commensal or pathogenic bacteria associated with eukaryotes in prokaryotes. Calcium phosphorylcholine chloride exhibits a surprising range of immunomodulatory properties .
Isradipine-d6 is the deuterium labeled Isradipine . Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease [4].
Homovanillic acid-d2 (Vanilacetic acid-d2) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
Ethyl palmitate-d31 is the deuterium labeled Ethyl palmitate. Ethyl palmitate, a fatty acid ethyl ester (FAEE), shows a marked preference for the synthesis of ethyl palmitate and ethyl oleate over other FAEEs in human subjects after ethanol consumption. Ethyl palmitate is used as a hair- and skin-conditioning agent .
N,N-Dimethylacetamide-d3 is the deuterium labeled N,N-Dimethylacetamide . N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent .
Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells .
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
N,N-Dimethylacetamide-d6 is the deuterium labeled N,N-Dimethylacetamide . N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent .
trans-Stilbene-d12 ((E)-Stilbene-d12) is the deuterium labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
Moroxydine hydrochloride-d8 (ABOB hydrochloride-d8) is the deuterium labeled Moroxydine (ABOB) hydrochloride (HY-B0420A). Moroxydine hydrochloride is a broad-spectrum agent with multi-antiviral activities against DNA and RNA viruses, including influenza virus, herpes simplex, varicella zoster, measles, mumps disease, hepatitis C virus, etc. Moroxydine hydrochloride exhibits excellent antiviral activity and shows low cytotoxicity to cells infected by dsRNA viruses (grass carp reovirus, GCRV) and large DNA viruses (giant salamander iridovirus, GSIV). Moroxydine hydrochloride blocks the GCRV-induced cytopathic effects and eliminates nucleocapsids in ctenopharyngodon idella kidney (CIK) cells to keep the normal morphological structure. Moroxydine hydrochloride significantly inhibits the apoptosis, the caspase 3 activity, Bax expression and down-regulates Bcl-2 levels [1][2][3].
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .
ar-Turmerone-d3 is the deuterium labeled ar-Turmerone. ar-Turmerone ((+)-ar-Turmerone) is an orally active and major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities. ar-Turmerone induces apoptosis in U937 cells. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation in vitro and in vivo, and can be used for various neurologic disorders study [4] .
Arachidic acid-d3 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
D-Serine-d3 ((R)-Serine-d3) is a deuterium labeled D-Serine (HY-100808). D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration .
Velpatasvir-d3 (GS-5816-d3) is deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases [4].
Alfuzosin-d3 hydrochloride is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Daurisoline-d5 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Candesartan Cilexetil-d11 (TCV-116-d11) is deuterium labeled Candesartan Cilexetil. Candesartan Cilexetil (TCV-116) is an angiotensin II receptor inhibitor. Candesartan Cilexetil ameliorates the pulmonary fibrosis and has antiviral and skin wound healing effect. Candesartan Cilexetil can be used for the research of high blood pressure [4] .
Octreotide-d8 (SMS 201-995-d8) is deuterium labeled Octreotide. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
Abiraterone acetate-d3 (CB7630-d3) is deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598) .
Granisetron-d6 (Hydrochloride) (BRL 43694A-d6) is deuterium labeled Granisetron (Hydrochloride). Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
Tetraethylammonium bromide-d20 (TEA bromide-d20) is the deuterium labeled Tetraethylammonium bromide (HY-W014408). Tetraethylammonium bromide is a quaternary ammonium salt consisting of a positively charged tetraethylammonium cation and a negatively charged bromide anion. This compound is commonly used as a phase transfer catalyst in organic chemical reactions, facilitating the transfer of reactants between immiscible phases. It can also be used as a reagent for the synthesis of various organic compounds, an electrolyte in electrochemical experiments, and a source of tetraethylammonium ions in biochemical and pharmacological research.
Phenytoin-d5 (5,5-Diphenylhydantoin-d5) is deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
Taurochenodeoxycholic acid-d9 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties .
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively [4].
Prosulfocarb-d7 (S-Benzyl dipropylthiocarbamate-d7) is deuterium labeled Prosulfocarb. Prosulfocarb is a herbicide with a rapidly growing use trend. Prosulfocarb is used in winter cereals to help address the problem of increasing biotic resistance of weeds to certain pesticides. Environmental and food effects of prosulfocarb have been observed, and its transfer pattern from target crops to non-target areas has been studied. The volatility effect of prosulfocarb is an important factor explaining the inefficiency of isolated area contamination and marginal protection against residue spread .
Adipic acid-d10 (Hexanedioic acid-d10) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Veratrole-d2 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Cyclohexanecarboxylic acid-d11 is the deuterium labeled Cyclohexanecarboxylic acid . Cyclohexanecarboxylic acid is a Valproate structural analogue with anticonvulsant action .
Fosinopril-d5 (SQ28555-d5 (free acid)) is deuterium labeled Fosinopril. Fosinopril (SQ28555 free acid) is the ester proagent of angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an Ki value of 1.675 μM .
Tolcapone-d7 (Ro 40-7592-d7) is the deuterium labeled Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4].
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
Octreotide-d8 (acetate) (SMS 201-995-d8 (acetate)) is deuterium labeled Octreotide. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
DPPC-d71 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Butamben-d9 is the deuterium labeled Butamben. Butamben (Butyl 4-aminobenzoate) results in long-lasting relief from pain, without impairing motor function or other sensory functions .
9-Fluorenol-d9 (9-Hydroxyfluorene-d9) is the deuterium labeled 9-Fluorenol (HY-W016388). 9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 μM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo .
Trihydroxycholestanoic acid-d5 (Coprocholic acid-d5) is deuterium labeled Trihydroxycholestanoic acid. Trihydroxycholestanoic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Refsum Disease, D Bifunctional Protein Deficiency and Infantile Refsum Disease [4][4] .
Tazarotenic acid-d6 is deuterium labeled Tazarotenic acid. Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma .
Cyproheptadine hydrochloride-d3 (Cyproheptadine HCl-d3) is the deuterium labeled Cyproheptadine hydrochloride (HY-B0366A). Cyproheptadine hydrochloride is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders .
Suberic acid-d12 is the deuterium labeled Suberic acid . Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency .
Tropicamide-d3 is the deuterium labeled Tropicamide . Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops .
Myrcene-d6 is the deuterium labeled Myrcene. Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity [4] .
(S)-Lisofylline-d5 ((S)-Lisophylline-d5) is the deuterium labeled (S)-Lisofylline (HY-109854). (S)-Lisofylline is a kind of Lisofline enantiomer with optical activity. (S)-Lisofylline can interconversion with pentoxifylline .
Tenofovir alafenamide-d5 fumarate (GS-7340-d5 fumarate) is the deuterium labeled Tenofovir alafenamide fumarate (HY-15232A). Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Nanofin-d2 (2,6-Lupetidine-d2) hydrochloride is the deuterium labeled Nanofin (HY-B1191). Nanofin (2,6-Lupetidine) is a neuro-blocking agent with antihypertensive effects, which can be used for the study of mild to moderate hypertension.
1-Undecanol-d23 (Undecyl alcohol-d23) is the deuterium labeled 1-Undecanol (HY-W004292). 1-Undecanol (Undecyl alcohol) is the main product generated from the degradation of 2-tridecanone by Pseudomonas bacteria isolated from the soil. 1-Undecanol can enhance the attraction of Grapholita molesta to sex pheromone traps .
Banoxantrone-d12 (dihydrochloride) is the deuterium labeled Banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Finerenone-d5 (BAY 94-8862-d5) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
Benserazide-d3 (hydrochloride) is the deuterium labeled Benserazide hydrochloride (HY-B0404A). Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma .
TRIA-662-d3 is the deuterium labeled TRIA-662 . TRIA-662 (1-Methylnicotinamide chloride) is an endogenous metabolite. TRIA-662 shows antithrombotic and anti-inflammatory activities .
Veratrole-d10 is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
Gliquidone-d6 is deuterium labeled Gliquidone. Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Benazepril-d5 hydrochloride is deuterium labeled Benazepril hydrochloride. Benazepril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy .
Nisoldipine-d3 is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.
Tempol-d17 is the deuterium labeled Tempol . Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS) .
Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4 .
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
(±)-Carnitine-d9 (chloride) is the deuterium labeled (±)-Carnitine chloride. (±)-Carnitine chloride exists in two isomers, known as D and L. L-carnitine plays an essential role in the β-oxidation of fatty acids and also shows antioxidant, and anti-inflammatory activities.
D-Valine-d8 is the deuterium labeled D-Valine. D-Valine is the enantiomer of L-Valine (HY-N0717). L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid.
Arachidic acid-d39 is the deuterium labeled Arachidic acid (HY-W004260). Arachidic acid (Eicosanoic acid) is a long-chain saturated fatty acid. Arachidic acid can be found in the human organism from the plasma phospholipid, fish, cannabis and other plant oils. Arachidic acid conjugated with Chitosan oligosaccharide (HY-112108) can be used for anti-cancer drug delivery research .
Nitrendipine-d5 is the deuterium labeled Nitrendipine (HY-B0424). Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma [4] .
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
trans-Stilbene-d2 ((E)-Stilbene-d2) is the deuterium labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
Hydroxy Itraconazole-d8 is the deuterium labeled Hydroxy Itraconazole (HY-12772). Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
Salmeterol-d5 is a deuterated labeled Salmeterol . Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata .
SAR405838-d10 (MI-77301-d10) is the deuterium labeled SAR405838 (HY-18986). SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity .
Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties .
Muscarine-d9 (iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist .
Silybin B-d3 (Silibinin B-d3) is a deuterated Silybin B (HY-N7046). Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity [4].
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
Tazarotenic acid-d8 (AGN 190299-d8) is the deuterium labeled Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene (HY-15388) .
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms [4] .
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
DPPC-d13 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Mianserin-d3 (hydrochloride) is the deuterium labeled Mianserin hydrochloride. Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
N,N-Dimethylacetamide-d9 is the deuterium labeled N,N-Dimethylacetamide . N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent .
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma [4] .
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
Ospemifene-d5 (FC-1271a-d5) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
Adipic acid-d8 (Hexanedioic acid-d8) is the deuterium labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
Methyl methanesulfonate-d3 is the deuterium labeled Methyl methanesulfonate (HY-W004702). Methyl methanesulfonate is an alkylating agent which transfers methyl groups, and induces DNA damage. Methyl methanesulfonate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Theobromine-d3 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Nonanoic acid-d17 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers . DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice .
Rimsulfuron-d6 is deuterium labeled Rimsulfuron. Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide for postemergence use in maize to control grasses and some broadleaf weeds .
Metformin-d6 (1,1-Dimethylbiguanide-d6) is a deuterated labeled Metformin (HY-B0627). Metformin inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [4] .
Moxifloxacin-d3 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin hydrochloride is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
DL-Dipalmitoylphosphatidylcholine-d62 is deuterium labeled DL-Dipalmitoylphosphatidylcholine. DL-Dipalmitoylphosphatidylcholine (DL-DPPC) is a biochemical reagent .
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents .
Ciclopirox-d11 is the deuterium labeled Ciclopirox. Ciclopirox (HOE296b) is a synthetic antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic .
25-Hydroxycholesterol-d6 (25-OHC-d6) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells .
Docosanoic acid-d3 (Behenic acid-d3) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans .
5-Fluorouracil-d is the deuterium labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer . 5-Fluorouracil also inhibits HIV .
DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers . DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice .
Rufinamide- 15N,d2-1 (CGP 33101- 15N,d2-1) is 15N- and deuterium-labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome [4].
2-Deoxy-D-glucose- 13C6 (2-DG- 13C6) is 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
Vanillin- 13C,d3 is the 13C and deuterium labeled Vanillin . Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine .
PSI-6206- 13C,d3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
13,14-Dihydro-15-keto prostaglandin D2-d9 (DK-PGD2-d9) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay . Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses .
DSPC-d9 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d9) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
L-Cysteine- 13C3, 15N,d3 is the deuterium, 13C-, and 15-labeled L-Isoleucine (HY-Y0337). L-isoleucine is a nonpolar hydrophobic amino acid . L-Isoleucine is an essential amino acid.
L-Serine- 15N,d3 is the deuterium and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
D-(+)-Trehalose-13C12 is a 13C isotope labeled version of D-(+)-Trehalose (HY-N1132). D-(+)-Trehalose,which is widespread, can be used as a food ingredient and pharmaceutical excipient .
DSPC-d74 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d74) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
Guanosine triphosphate- 13C10, 15N5 (tetraammonium) is the 13C and 15N labeled Guanosine triphosphate tetraammonium . Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19 .
DSPC-d70 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d70) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
DL-Alanine- 13C2, 15N (DL-2-Aminopropionic acid- 13C2, 15N) is 13C and 15N labeled DL-Alanine. DL-alanine, an orally active amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver [4] .
3-Indoleacetic acid-2,2-d2 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Adenosine monophosphate- 13C10, 15N5 (AMP- 13C10, 15N5) disodium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
L-Histidine- 13C6, 15N3 hydrochloride hydrate is the 13C- and 15N-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
DSPC-d13 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d13) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
DSPC-d79 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d79) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
L-Thyroxine- 13C6-1 (Levothyroxine- 13C6-1; T4- 13C6-1) is a 13C labeled L-Thyroxine (HY-18341). L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4) .
p-Anisic acid- 13C6 is the 13C-labeled p-Anisic acid. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties .
Ondansetron- 13C,d3 is the 13C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy [4] .
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [4].
DSPC-d83 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83) is the deuterium labeled DSPC (HY-W040193). DSPC is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system .
LysoPC(14:0/0:0)-d7 (14:0 Lyso PC-d7) is deuterium labeled LysoPC(14:0/0:0). LysoPC(14:0/0:0) is a lysophospholipid (LyP). It is a monoglycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. LysoPC(14:0/0:0) has potent antispasmodic effect .
Lamivudine-13C,15N2,d2 (BCH-189-13C,15N2,d2) is a 13C, 15N, and deuterium labeled Lamivudine (HY-B0250). Lamivudine is an orally active and blood-brain barrier permeable nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine inhibits HIV reverse transcriptase 1 and 2 and hepatitis B virus (HBV) reverse transcriptase [4].
5-Methyltetrahydrofolic acid- 13C6 (5-Methyl THF- 13C6) is 13C labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases .
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .
Adenosine monophosphate- 13C10, 15N5(AMP- 13C10, 15N5) is the 13C-labeled and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Thymidine-5'-monophosphate- 13C10, 15N2 (disodium) is the 13C and 15N labeled Thymidine-5'-monophosphate disodium salt . Thymidine-5'-monophosphate disodium salt is an endogenous metabolite.
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
(±)11(12)-EET-d11 methyl ester (11,12-EET methyl ester-d11) is the deuterium labeled (±)11(12)-EET methyl ester (HY-139938). (±)11(12)-EET methyl ester is a type of epoxyeicosatrienoic acid (EET). EETs are endogenous lipid signaling molecules with cardioprotective and vasodilatory actions. (±)11(12)-EET methyl ester binds to and activates GPR132. (±)11(12)-EET methyl ester enhances hematopoietic induction and engraftment in mice and zebrafish .
Mirogabalin- 13C2,d1 (Mixture of Diastereomers) is a 13C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
Intermediate of tranexamic Acid- 13C2, 15N (Aminomethylbenzoic acid- 13C2, 15N) is 13C and 15N labeled 4-(Aminomethyl)benzoic acid. 4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis . 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis .
Cytidine-5'-triphosphate- 13C5 (Cytidine triphosphate- 13C5) is the 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii .
2'-Deoxycytidine-5'-monophosphoric acid- 13C9 dilithium is the 13C-labeled 2'-Deoxycytidine-5'-monophosphoric acid (HY-W009216). 2'-Deoxycytidine-5'-monophosphoric acid is an endogenous metabolite .
Valdecoxib- 13C2, 15N (SC 65872- 13C2, 15N) is the 13C- and 15N-labeled Valdecoxib (HY-15762). Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
(+/-)-Catechin Gallate- 13C3 is the 13C-labeled (-)-Catechin gallate. (-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract .
Uridine triphosphate- 15N2 (UTP- 15N2 dilithium; Uridine 5'-triphosphate- 15N2) dilithium is 15N labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
5-Methyltetrahydrofolic acid- 13C5 is the 13C-labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid .
L-Valine- 13C5, 15N,d8 ((S)-Valine- 13C5, 15N,d8) is the deuterium, 13C-, and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Acid Orange 7- 13C6 (Orange II- 13C6) is the 13C-labeled Acid orange 7 (HY-N1442). Acid Orange 7 (Orange II; D&C Orange NO. 4) is an azo dye widely used in the textile, food and cosmetic industries. Acid Orange 7 is mainly used as a colorant by combining with fibers and other substances through azo bonds. Acid Orange 7 has a maximum absorption wavelength at 484-485 nm, and the concentration is measured using a UV-visible spectrophotometer. Acid Orange 7 is difficult to degrade and has a certain degree of toxicity. It is often used to study various sewage treatment technologies and photocatalytic degradation reactions, and to evaluate the removal effects of different treatment methods on organic pollutants .
O-Phospho-L-serine- 13C3 (L-Serine O-phosphate- 13C3) is the 13C-labeled O-Phospho-L-serine (HY-15129). O-Phospho-L-serine is the immediate precursor to L-cystein in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2 .
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
L-Glutamine- 13C5, 15N2 is the 13C- and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
O-Desmethyl midostaurin- 13C6 (CGP62221- 13C6; O-Desmethyl PKC412- 13C6) is the 13C-labeled O-Desmethyl Midostaurin (HY-129491). O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo . Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM.
p,p'-DDE- 13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Imatinib- 13C,d3 (STI571- 13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively [4]. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
Deoxythymidine-5'-triphosphate- 13C10, 15N2 (dTTP- 13C10, 15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Cinnamic acid- 13C3 (3-Phenylacrylic acid- 13C3) is the 13C labeled Cinnamic acid (HY-N0610A). Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells .
3-Indoleacetic acid- 13C6 is the 13C labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
DL-Lysine- 13C6, 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6, 15N2 hydrochloride) is 13C and 15N-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
L-Valine- 13C5, 15N,d2 ((S)-Valine- 13C5, 15N,d2) is the deuterium, 13C-, and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Uridine triphosphate- 13C9 (UTP- 13C9 dilithium; Uridine 5'-triphosphate- 13C9) dilithium is 13C-labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Guanosine 5'-diphosphate- 13C10, 15N5 (GDP- 13C10, 15N5) dilithium is 13C and 15N-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
Sofosbuvir- 13C,d3 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Adenosine 5'-diphosphate- 15N5 (Adenosine diphosphate- 15N5 dilithium) dilithium is 15N labeled Adenosine 5'-diphosphate (HY-W010918). Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant .
Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms [4] .
2-Methylcitric acid-d3 is the deuterium labeled 2-Methylcitric acid. 2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate .
PIPES-d18 is the deuterium labeled PIPES . PIPES (1,4-Piperazinediethanesulfonic acid) is an important component of PIPES buffer agent used in biochemistry .
1-Methylguanosine-d3 (N1-Methylguanosine-d3) is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker .
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol . Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin .
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12.?Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .
Idasanutlin-d3-1 (RG7388-d3-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of MDM2/p53. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .
Methyl cinnamate-d7 is deuterated labeled Methyl cinnamate (HY-W017212). Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway .
Cholestenone-d7 is deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop
Oxaceprol-d3 (N-Acetyl-L-hydroxyproline-d3) is deuterium labeled Oxaceprol. Oxaceprol (N-Acetyl-L-hydroxyproline), an orally active derivative of L-proline, possesses distinct anti-inflammatory activity. Oxaceprol is usually used for the research of osteoarthritis and rheumatoid arthritis .
Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate . Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
Resolvin D3-d5 is the deuterium labeled Resolvin D3. Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation .
Rosuvastatin-d3 (ZD 4522-d3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals .
Dimethyl adipate-d8 (Hexanedioic acid dimethyl ester-d8) is the deuterium labeled Dimethyl adipate (HY-W015301). Dimethyl adipate is an aliphatic dicarboxylate compound. Dimethyl adipate is mainly used as a plasticizer and an intermediate in organic synthesis.
Azilsartan mepixetil-d5 (QR-01019-d5) is deuterium labeled Azilsartan mepixetil. Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A) .
Tridecanoic acid-d25 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation .
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation .
Melatonin-d7 is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation [4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
(Rac)-Valsartan-d9 is deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research .
Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator .
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Ribavirin- 13C2 (Ribasphere- 13C2) is the 13C-labeled Ribavirin (HY-B0434). Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.
Hippuric acid-d2 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
1-Methylinosine-d3 is the deuterium labeled 1-Methylinosine. 1-Methylinosine is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA .
Danicamtiv-d3-1 (MYK-491-d3-1) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .
Tridecanoic acid-d2 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation .
Brexpiprazole S-oxide-d8 (DM-3411 D8) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
N-Desmethyl Selegiline-dd5 hydrochloride is the deuterium labeled N-Desmethyl Selegiline hydrochloride . N-Desmethyl Selegiline-d5 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Degarelix-d7 (FE 200486-d7 free base) is deuterium labeled Degarelix. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
1-Aminopropan-2-ol-d6 (Monoisopropanolamine-d6) is the deuterium labeled 1-Aminopropan-2-ol (HY-W015969). 1-Aminopropan-2-ol is a microbial metabolism of amino alcohol metabolism via propionaldehyde and acetaldehyde in a species of Pseudomonas .
2-Phenylglycine-d5 is the deuterium labeled 2-Phenylglycine. 2-Phenylglycine (DL-α-Phenylglycine) is a metabolite in breast milk during the W2 to W4 lactation period .
Isovanillin-d3 is the deuterium labeled Isovanillin . Isovanillin is an aldehyde oxidase inhibitor . Antispasmodic activities . Antidiarrheal activities [4].
Leukotriene B4-d5(LTB4-d5) is deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs [4].
(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
Methyl tetradecanoate-d27 is the deuterium labeled Methyl myristate. Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma .
Docosahexaenoic acid ethyl ester-d5 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects .
Bifenox-d3-1 (Modown-d3; MC-4379-d3) is the deuterium labeled Bifenox (HY-136513). Bifenox (Modown; MC-4379) is a potent herbicide. Bifenox increases the ROS production. Bifenox causes cellular membrane disruption, inhibition of photosynthesis .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Levomefolic acid-d3 (L-5-MTHF-d3) is deuterium labeled Levomefolic acid. Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .
(Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist .
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties . Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways . Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM .
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes .
Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively .
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Resolvin D1-d5 is the deuterium labeled Resolvin D1. Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α-mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages .
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid Budesonide (HY-13580). 16α-Hydroxyprednisolone formation is catalyzed by isoenzymes within the cytochrome P450 3A (CYP3A) subfamily. 16α-Hydroxyprednisolone formation can be inhibited by antibodies targeting the CYP3A subfamily .
4-Hydroxypropranolol-d7 (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties .
Leukotriene E4-d5 is the deuterium labeled Leukotriene E4. Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
(R)-Pioglitazone-d1 ((R)-U 72107-d1) is a stabilized and deuterated R-enantiomer of pioglitazone, exhibiting pharmacological properties that are beneficial for NASH treatment, including modulation of mitochondrial function, non-steroidal anti-inflammatory effects, and glucose-lowering capabilities.
L-Histidine-d5 hydrochloride hydrate is the deuterium labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 .
Fluoxetine-d6 (LY-110140 (free base)-d6) is deuterium labeled Fluoxetine. Fluoxetine (LY-110140 free base) is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively .
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
L-Histidine-d3 hydrochloride hydrate is the deuterium labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons .
Asymmetric dimethylarginine-d7 (hydrochloride hydrate) is the deuterium labeled Asymmetric dimethylarginine. Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a num
Albendazole-d3-1 (SKF-62979-d3-1) is the deuterium labeled Albendazole (HY-B0223). Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells [4] .
L-(+)-Ampicillin-d5 (L-(+)-α-Aminobenzylpenicillin-d5) is the deuterium labeled L-(+)-Ampicillin (HY-B0522C). L-(+)-Ampicillin (L-(2S) ampicillin) is the L-isomer of Ampicillin (HY-B0522). Ampicillin is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria .
11-Oxo etiocholanolone-d5 (11-Ketoetiocholanolone-d5) is the deuterium labeled 11-Oxo etiocholanolone (HY-113457). 11-Oxo etiocholanolone (11-Ketoetiocholanolone) is a steroid. 11-Oxo etiocholanolone is a key indicator for detecting cortisol metabolites in feces and urine. 11-Oxo etiocholanolone has the potential to be a pheromone .
Guanosine triphosphate-d14 (GTP-d14) dilithium is a deuterium labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19 .
Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM [4].
DL-dithiothreitol-d10-1 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases [4]
o-Phenanthroline-d8 is the deuterium labeled o-Phenanthroline. o-Phenanthroline (1,10-Phenanthroline), a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells. o-Phenanthroline (1,10-Phenanthroline) forms a red chelate with Fe2+ that absorbs maximally at 510 nm. o-Phenanthroline (1,10-Phenanthroline) is also a MMP inhibitor .
2-Hydroxymethyl olanzapine-d3 (LY-290411-d3) is a deuterium labeled 2-Hydroxymethyl olanzapine. 2-Hydroxymethyl olanzapine is a metabolite of Olanzapine. .
Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
3-Hydroxy Midostaurin-d5 is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively .
Acetyl coenzyme A-d3 (Acetyl-CoA-d3) is the deuterium labeled Acetyl coenzyme A (HY-114293). Acetyl-coenzyme A (Acetyl-CoA) is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A is also a key precursor of lipid synthesis [4].
Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
Alfuzosin (hydrochloride)-d6 (SL 77499-10-d6) is deuterium labeled Alfuzosin (hydrochloride). Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH) .
Sudan I-d5 is a the deuterated Sudan I. Sudan I is a diazo-conjugate red dye and can be used as an additive to products such as oils, solvents or polishes. Sudan I inhibits growth of bacterial strains Clostridium perfringens and L. rhamnosus .
1-Octanol-d2-1 is deuterated labeled 1-Octanol (HY-W032013). 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents . 1-Octanol is a highly attractive biofuel with diesel-like properties .
Sarafloxacin-d8 (hydrochloride trihydrate) is the deuterium labeled Sarafloxacin hydrochloride trihydrate. Sarafloxacin hydrochloride trihydrate is a quinolone antibiotic compound .
Nemonoxacin-d3-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
Hippuric acid-d5 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
Adenosine monophosphate-d12 (AMP-d12) dilithium is deuterium labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Eliglustat-d15 (tartrate) is the deuterium labeled Eliglustat. Eliglustat tartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Ethyl butyrylacetate-d5 (Ethyl 3-oxohexanoate-d5) is the deuterium labeled Ethyl butyrylacetate (HY-W015487). Ethyl butyrylacetate is an organic compound belonging to the class of esters. Synthesized by the reaction of ethyl acetate, butyric acid and acetic anhydride. Ethyl butyrylacetate has a fruity aroma and is commonly used as a flavoring agent in various food and beverages such as candies, ice cream and soft drinks. It is also used as a fragrance ingredient in perfumes and personal care products. In addition to its use in the food and fragrance industries, Ethyl butyrylacetate is also used in industrial settings, such as in the production of solvents.
Vitamin D4-d5 is the deuterium labeled Vitamin D4. Vitamin D4 (22-Dihydroergocalciferol) is a Vitamin D derived from fungi. The precursor of Vitamin D4 is 22,23-dihydroergosterol .
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
Itopride-d6 (HSR803-d6 (free base)) is deuterium labeled Itopride. Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD) .
Perindoprilat-d3 disodium is deuterated labeled Perindoprilat (HY-B1433). Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research .
Bendamustine-d8 is the deuterium labeled Bendamustine . Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties .
rac-Trandolapril-d5 (rac-RU44570-d5) is deuterium labeled Trandolapril. Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
Cholestenone-d5 is the deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells .
Voriconazole N-oxide-d3 (Voriconazole oxynitride-d3) is deuterium labeled Voriconazole N-oxide. Voriconazole N-oxide (Voriconazole oxynitride) is a potent antifungal agent. Voriconazole N-oxide has phototoxicity and photocarcinogenicity. Voriconazole N-oxide does not sensitize keratinocytes to ultraviolet B (UVB) .
2,3-Oxidosqualene-d6 (Squalene oxide-d6) is a deuterium labeled 2,3-Oxidosqualene (HY-114296). 2,3-Oxidosqualene (Squalene oxide) is an intermediate in the biological synthesis of sterols from squalene .
Prostaglandin D2-d9 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals . Prostaglandin D2 is one of the most potent endogenous sleep promoting substances . PGD2 plays a protective role by suppressing inflammation .
Bimatoprost-d5 is a deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog and is a topical hypotensive agent frequently used for treating ocular hypertension and glaucoma. Bimatoprost also has an antiadipogenic effect .
Methyl paraben-d3 (Methyl 4-hydroxybenzoate-d3) is the deuterium labeled Methyl paraben (HY-N0349). Methyl Paraben is a standardized methyl paraben allergen isolated from Yunnan hemlock (Tsuga dumosa). Methyl Paraben is commonly used as a stable, non-volatile preservative. Methyl Paraben increases histamine release and cellular regulation of immunity, blocks sodium channels, and prevents ischemia-reperfusion injury [4].
Tridecanoic acid-d9 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation .
Linagliptin-d3-1 (BI 1356-d3-1) is the deuterium labeled Linagliptin (HY-10284). Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM .
Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research .
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule?depolymerization with an IC50 value of 0.2 μM . Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of?bcl-2?and?bcl-xL?gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis .
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively .
Lurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM .
rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142) . Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively .
22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone (HY-131543). 22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcoholic metabolite with antiprogestational and antiglucocorticoidal activities, which contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. The relative binding affinity of 22-Hydroxy Mifepristone to the human glucocorticoid receptor is 48% .
Kinetin riboside-d5 (N6-Furfuryladenosine-d5) is the deuterium labeled Kinetin riboside (HY-101055). Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM .
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
Norethindrone acetate-d8 is the deuterium labeled Norethindrone acetate. Norethindrone acetate is a female hormone used for the research of endometriosis . Norethindrone acetate-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Alogliptin-d3 is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes .
Miconazole-d5 (nitrate) is the deuterium labeled Miconazole. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects .
Ethyl 3-oxopentanoate-d3 (Ethyl Propionylacetate-d3) is the deuterium labeled Ethyl 3-oxopentanoate (HY-78211). Ethyl 3-oxopentanoate is an organic ester compound commonly used as a reactant or solvent in organic synthesis. It can be used as an important raw material for the preparation of pharmaceuticals, food flavors, spices and other products. In addition, because of its stability and reactivity in certain chemical reactions, it is also widely used in some industrial productions. Although Ethyl 3-oxopentanoate has no direct application in the medical field, it still plays an important role in chemical research and industry.
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
Paroxetine-d6-1 is a deuterated labeled Paroxetine . Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs .
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation [4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
Ipidacrine-d9 (NIK-247-d9 (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases [4] .
Benzyl benzoate-d12 is the deuterium labeled Benzyl benzoate . Benzyl benzoate (Benzoic acid benzyl ester) is a fragrance ingredient in cosmetic products. Benzyl benzoate can be used for the research of Scabies and Demodex-associated inflammatory skin conditions [4].
Donepezil-d7 (E2020-d7 (free base)) is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
2-Acetylthiazole- 13C2 is 13C labeled 2-Acetylthiazole (HY-Y0045). 2-Acetylthiazole (1-(1,3-Thiazol-2-yl)ethanone; 1-(Thiazol-2-yl)ethanone; Methyl 2-thiazolyl ketone) is a flavor compound. 2-Acetylthiazole is a kind of biological materials or organic compounds that are widely used in life science research .
Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine . Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity .
Deoxycytidine triphosphate- 13C9 (dCTP- 13C9 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9) dilithium is 13C-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
DMT-dA(bz) Phosphoramidite- 13C10, 15N5 is the 13C and 15N labeled DMT-dA(bz) Phosphoramidite . DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA .
Cytidine-5'-triphosphate- 13C9 (Cytidine triphosphate- 13C9 dilithium; 5'-CTP- 13C9) dilithium is 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
2'-Deoxyadenosine-5'-triphosphate- 13C10, 15N5 tetraammonia is the 13C10 and 15N5 labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase .
Menaquinone-4- 13C6 is the 13C-labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
Cytidine-5'-triphosphate- 15N3 (Cytidine triphosphate- 15N3 dilithium; 5'-CTP- 15N3) dilithium is 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii.
Estrone 3-methyl ether- 13C6 is a 13C-labeled Estrone 3-methyl ether (HY-79576). Estrone 3-methyl ether (Oestrone methyl ether; 3-O-Methylestrone) is a synthetic intermediate useful for synthesis of estrogen receptor modulator .
Hexadecane-1,2- 13C2 (n-Hexadecane-1,2- 13C2) is the 13C labeled Hexadecane (HY-W099580). Hexadecane (n-Hexadecane) is a saturated hydrocarbon of alkanes or paraffins and can be used as an organic solvent. Hexadecane is a component of petroleum, belongs to hydrophobic substrates, and is a model substance for studying bacterial degradation of hydrophobic compounds .
Thymine- 13C5, 15N2 (5-Methyluacil- 13C5, 15N2) is 13C and 15N labeled Thymine. Thymine is one of the four nucleobases in the nucleic acid of DNA and can be a target for actions of 5-fluorouracil (5-FU) in cancer treatment, with a Km of 2.3 μM .
dGTP- 13C10, 15N5 (2'-Deoxyguanosine-5'-triphosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Deoxycytidine triphosphate- 15N3 (dCTP- 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3) dilithium is 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
2'-Deoxyadenosine-5'-triphosphate- 13C10, 15N5 (dATP- 13C10, 15N5) dilithium is 13C and 15N-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
5-Hydroxymethylfurfural- 13C6 (2-Hydroxymethyl-5-furfural- 13C6; 2-Formyl-5-hydroxymethylfuran- 13C6) is a 13C labeled 5-Hydroxymethylfurfural (HY-Y0051). 5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from Cornus officinalis, inhibits yeast growth and fermentation as stressors.
p,p'-DDD- 13C12 is 13C labeled p,p'-DDD. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT .
Oleic acid- 13C18 is the 13C labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
Rapamycin- 13C,d3-1 (Sirolimus- 13C,d3-1) is the deuterium labeled and 13C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
2'-Deoxycytidine- 13C, 15N3 (Deoxycytidine- 13C, 15N3) is 13C and 15N labeled 2'-Deoxycytidine. 2'-Deoxycytidine, a deoxyribonucleoside, can inhibit biological effects of Bromodeoxyuridine (Brdu). 2'-Deoxycytidine is essential for the synthesis of nucleic acids, that can be used for the research of cancer .
Droxidopa- 13C2, 15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood-brain barrier .
Acetaminophen- 13C2, 15N is the 13C and 15N labeled Acetaminophen . Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent [4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor .
Hydrocinnamic acid-2,3- 13C2 is the 13C-labeled Hydrocinnamic acid. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities.
Cytidine 5′-monophosphate- 13C9 (5'-Cytidylic acid- 13C9 dilithium; 5'-CMP- 13C9) dilithium is 13C-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid- 13C10 (5'-GMP- 13C10 dilithium; 5'-guanosine monophosphate- 13C10) dilithium is 13C-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
N-Acetyl mesalazine- 13C6 (N-Acetyl-5-aminosalicylic acid- 13C6) is a deuterated labeled N-Acetyl mesalazine (HY-66008). N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the primary intestinal metabolite of 5-Aminosalicylic Acid (HY-15027) and serves as a biomarker for evaluating the efficacy of 5-Aminosalicylic Acid (HY-15027). N-Acetyl mesalazine can scavenge free radicals, reduce DNA base hydroxylation, and ameliorate mucosal inflammation. N-Acetyl mesalazine can be used in the study of diseases such as colitis and colon cancer .
(E,E)-Farnesol- 13C3 (trans,trans-Farnesol- 13C3) is the 13C-labeled (E,?E)?-?Farnesol (HY-Y0248). (E, E)-Farnesol (trans,trans-Farnesol;(2E,6E)-Farnesol) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Uridine 5'-monophosphate- 13C9, 15N2 disodium is the 13C and 15N labeled Uridine 5'-monophosphate disodium salt (HY-W013175). Uridine 5'-monophosphate (5'-Uridylic acid) disodium salt is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate disodium salt can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Cytidine- 13C9 (Cytosine β-D-riboside- 13C9) is 13C labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function .
Fmoc-Asp(OtBu)-OH-d3 (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate-d3) is deuterium labeled Fmoc-Asp(OtBu)-OH. Fmoc-Asp(OtBu)-OH (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate) is a aspartate derivative containing amine protecting group Fmoc. Fmoc-Asp(OtBu)-OH can be used for peptide synthesis .
rU Phosphoramidite- 13C9, 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9, 15N2) is 13C and 15N-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Cytidine- 15N3 is the 15N labeled Cytidine . Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [4].
2'-Deoxyguanosine 5'-monophosphate- 13C10, 15N5 (dGMP- 13C10, 15N5) disodium is the 13C and 15N labeled 2'-Deoxyguanosine 5'-monophosphate disodium (HY-W013159). 2'-Deoxyguanosine 5'-monophosphate (5′-dGMP) disodium is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a reactant involved in analysis of self-assembling in solution and nucleation/growth of G-qudruplexes, nucleophilic trapping and reductive alkylation. 2'-Deoxyguanosine 5'-monophosphate disodium can be used as an oxidizable target. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative and is a nucleotide precursor used in DNA synthesis .
Cytidine 5′-monophosphate- 15N3 (5'-Cytidylic acid- 15N3 dilithium; 5'-CMP- 15N3) dilithium is 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Acetyl-L-carnitine hydrochloride- 13C3 (O-Acetyl-L-carnitine hydrochloride- 13C3) is the 13C-labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression .
Uridine 5'-monophosphate- 13C9, 15N2 (5'- Uridylic acid- 13C9, 15N2) dilithium is 13C and 15N-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
Sulfadimethoxine- 13C6 is the 13C-labeled Sulfadimethoxine. Sulfadimethoxine (Sulphadimethoxine) is a sulfonamide antibiotic used to treat many infections .
Mebeverine acid-d5 (Mebeverine metabolite Mebeverine acid-d5) is the deuterium labeled Mebeverine Acid (HY-12769). Mebeverine acid is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine.
1,3,5-Trimethoxybenzene-d3 (Trimethyl phloroglucinol-d3) is the deuterium labeled 1,3,5-Trimethoxybenzene (HY-Y0678). 1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor .
Sulfachloropyridazine- 13C6 is the 13C6 labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
N-Acetyl-L-methionine-d3 is the deuterium labeled N-Acetyl-L-methionine. N-Acetyl-L-methionine, a human metabolite, is nutritionally and metabolically equivalent to L-methionine. L-methionine is an indispensable amino acid required for normal growth and development .
6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
Zeranol-d5-1 (α-Zearalanol-d5-1) is the deuterium labeled Zeranol (HY-N6709). Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity .
D-Glutamic acid-d5 is the deuterium labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods .
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Borocaptate- 10B12 (BSH- 10B12) sodium is a boron-10 labeled Borocaptate (HY-142041). Borocaptate sodium is a boron-containing compound that can be used as a therapeutic agent in boron neutron capture therapy (BNCT), exhibiting anticancer activity .
3-Methoxytyramine-d3 hydrochloride (3-O-methyl Dopamine-d3 hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride (HY-103638). 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1).
5,6-Dihydro-5-methyluracil-d6 is the deuterium labeled 5,6-Dihydro-5-methyluracil. 5,6-Dihydro-5-methyluracil (Dihydrothymine), an intermediate breakdown product of thymine, comes from animal or plants. 5,6-Dihydro-5-methyluracil (Dihydrothymine) can be toxic when present at abnormally high levels .
3-O-Methyltolcapone-d7 (Ro 40-7591 d7) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma [4] .
Valerylcarnitine-d9 (C5:0 L-carnitine-d9) is the deuterium labeled Valerylcarnitine (HY-113266). Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines .
L-Alanine-d7 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Betamethasone dipropionate-d10 is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
Benzisothiazolinone-13C5 (1,2-Benzothiazol-3-one-13C5) is a 13C-labeled Benzisothiazolinone. Benzisothiazolinone is widely used as an antiseptic and antibacterial agent .
ATP-d14 (Adenosine 5'-triphosphate-d14) dilithium is deuterium labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Mebeverine acid-d3 (Mebeverine metabolite Mebeverine acid-d3) is the deuterium labeled Mebeverine Acid (HY-12769). Mebeverine acid is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine.
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model [4].
Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
Glibenclamide- 13C6 (Glyburide- 13C6) is 13C labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability [4]. Glibenclamide can induce autophagy .
L-Glutamine-d5 is the deuterium labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Epiallopregnanolone-d5 (5α,3β-THDOC-d5) is deuterium labeled Epiallopregnanolone. Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer .
2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity .
(2R)-Isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate-d5 is the deuterium labeled (2R)-isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate [
(S)-Verapamil-d6 ((S)-(-)-Verapamil-d6) hydrochloride is the deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
PAC-1-d8 (Procaspase activating compound 1-d8) is the deuterium labeled PAC-1 (HY-13523). PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC50 of 2.08 μM.
Ceftriaxone-d3 (disodium) is the deuterium labeled Ceftriaxone. Ceftriaxone is a third-generation cephalosporin antibiotic with excellent activity against many gram-negative, and reasonable activity against most gram-positive microorganisms. Anti-inflammatory and antioxidant characteristics .
Indolelactic acid-d5 is the deuterium labeled Indolelactic acid. Indolelactic acid is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures.
Adenosine-d is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
O-Toluic acid-d7 is the deuterium labeled o-Toluic acid . o-Toluic acid (2-Methylbenzoic acid) is a benzoic acid substituted by a methyl group at position 2. O-Toluic acid plays a role as a xenobiotic metabolite.
Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects [4] .
Diethyl phosphate-d10-1 is the deuterium labeled Diethyl phosphate. Diethylphosphate (Diethyl phosphoric acid) is an orally active organophosphorus pesticides metabolite. Diethylphosphate can interfere with thyroid hormone-related mechanisms and affect intestinal microbes in rats .
(±)11(12)-EET-d11 is the deuterium labeled (±)11(12)-EET. (±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective [4] .
Ribavirin- 13C5 is the 13C-labeled Ribavirin. Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV.
Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader .
Homovanillic acid-d3-1 (Vanilacetic acid-d3-1) is deuterated labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
L-Alanine-d3 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
MCA-d3 (7-Methoxycoumarin-4-acetic acid3) is the deuterium labeled MCA (HY-W027544) . MCA is a Coumarin (HY-N0709) derivative. MCA quantitates platelet-activating factor (PAF) by high-performance liquid chromatography with fluorescent detection. MCA can modify FRET peptide substrates for analyzing protease activities .
2-Hydroxy Ibuprofen-d6 is the deuterium labeled 2-Hydroxy Ibuprofen. 2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively .
Norethindrone- 13C2 (Norethisterone- 13C2) is the 13C labeled Norethindrone (HY-B0554) . Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea [4] .
TCEP-d12 (hydrochloride) (Tris(2-?carboxyethyl)?phosphine hydrochloride-d12) is deuterium labeled TCEP (hydrochloride). TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry [4] .
Calcifediol-d3 is a deuterium labeled Calcifediol. Calcifediol, is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels .
Veratrole-d2-1 is the deuterium labeled Veratrole (HY-B1812). Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii .
d-KLA Peptide-d30 (D-(KLAKLAK)2-d30) is the deuterium labeled d-KLA Peptide (HY-P10285). d-KLA Peptide is a synthetic pro-apoptotic peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrial membrane. d-KLA Peptide activates biochemical pathways associated with apoptosis, including the activation of caspase family proteins and PARP (poly ADP ribose polymerase). d-KLA Peptide can be used to carry and deliver genes or small molecules to enhance anti-tumor effects .
Migalastat-d5 (GR181413A-d5 (free base)) is deuterium labeled Migalastat. Migalastat (GR181413A free base) is an orally active α-galactosidase A molecular chaperone, with an IC50 value of 0.04 μM for human α-Gal A. Migalastat binds to the active site of certain unstable mutant forms of α-galactosidase A, facilitating their transport to the lysosome. After dissociation in the acidic environment, Migalastat enables the mutant α-galactosidase A to exhibit biological activity .
Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
D-Threonine-d2 (H-D-Thr-OH-d2) is the deuterium labeled D-Threonine (HY-W012874). D-Threonine is one of the important unnatural amino acids used as chiral building blocks in pharmaceutical drugs. D-Threonine is a metabolite of Saccharomyces cerevisiae. D-Threonine is cleaved into glycine and acetaldehyde by the catalytic action of D-threonine aldolase.
Mebeverine acid-d5 (Mebeverine metabolite Mebeverine acid-d5) hydrochloride is deuterium labeled Mebeverine acid hydrochloride. Mebeverine acid hydrochloride is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid hydrochloride is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid hydrochloride is an important marker for oral Mebeverine.
Ercalcidiol-d3 is the deuterium labeled Ercalcidiol. Ercalcidiol is a metabolite of Vitamins D2. Ercalcidiol can be used as an indicator of vitamins D status .
14(S)-HDHA-d5 (14(S)-HDoHE-d5) is deuterium labeled 14(S)-HDHA. 14(S)-HDHA (14(S)-HDoHE) is an oxygenation product of Docosahexaenoic acid (DHA). 14(S)-HDHA is a marker reflecting activation of a Docosahexaenoic acid carbon 14-lipoxygenation pathway .
1-Decanol-d2-2 is deuterated labeled 1-Decanol (HY-Y1004). 1-Decanol is used in the production of lubricants, surfactants, plasticizers and solvents. It has also been used to study the thermal properties of polymeric monolithic stationary phases and to enhance homopolyglycine acceptor function. Used in cosmetics, daily flavors, and food flavors.
1-Butynylbenzene-d5 is the deuterium labeled 1-Butynylbenzene . 1-Butynylbenzene-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ibufenac- 13C6 (Dytransin- 13C6) is the 13C-labeled Ibufenac (HY-W040672). Ibufenac (Dytransin) is an orally active nonsteroidal anti-inflammatory agent. Ibufenac exerts anti-inflammatory, analgesic and antipyretic effects. Ibufenac is being studied for the treatment of rheumatic diseases such as rheumatoid arthritis .
Moxifloxacin-d5 (BAY 12-8039-d5 (free base)) is deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Estriol- 13C3 is the 13C-labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Dimetridazole-d3 (1,2-Dimethyl-5-nitroimidazole-d3) is a deuterium labeled Dimetridazole (HY-B1244). Dimetridazole is a nitroimidazole antibiotic. Dimetridazole inhibits protein synthesis in cultures of Campylobacter jejuni. Dimetridazole is genotoxic. Dimetridazole can be used in the research of protozoal and bacterial infections [4].
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide . Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect [4].
Doxercalciferol-d6 (1.alpha.-Hydroxyvitamin D2-d6) is deuterium labeled Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
Ciraparantag-d8 (PER977-d8) tetrahydrochloride diacetate is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban [4].
DL-Alanine-d3 is the deuterium labeled DL-Alanine. DL-alanine, an amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine, and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver [4] .
(E)-β-Farnesene-d6 is deuterated labeled (E)-β-Farnesene (HY-N7364). (E)-β-Farnesene (trans-β-Farnesene) is an aphid alarm pheromone, which can be found in Phlomis aurea Decne essential oil. (E)-β-Farnesene shows good binding score with a value of -30.64 kcal/mol to the CDK2 receptor. (E)-β-Farnesene also exhibits good affinity to odorant-binding protein 3 (OBP3). (E)-β-Farnesene can be used as a feeding stimulant for the sand fly Lutzomyia longipalpis [4].
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .
DL-Alanine-d7 (DL-2-Aminopropionic acid-d7) is deuterium labeled DL-Alanine. DL-alanine, an orally active amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver [4] .
2-Sec-butyl-3-methoxypyrazine-d3 is deuterated labeled cis-?Jasmone (HY-N7058). Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies .
p-Toluic acid-d3 is the deuterium labeled p-Toluic acid . p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
3-Methoxybenzeneboronic acid-d3 is the deuterium labeled 3-Methoxybenzeneboronic acid (HY-W000854). 3-Methoxybenzeneboronic acid (3-Methoxyphenylboronic acid) is a boronic acid derivative. 3-Methoxybenzeneboronic acid shows best suitable binding pattern at the active site by interacting non-covalently with amino acid residues of proteins. 3-Methoxybenzeneboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities . Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling . Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation .
Abemaciclib metabolite M20-d8 is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor .
Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
3,4-Dehydro Cilostazol-d11 is deuterated labeled 3,4-Dehydro Cilostazol (HY-135910). 3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study .
Patulin- 13C7 (Terinin- 13C7) is the 13C labeled Patulin (HY-N6779) . Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage [4] .
Calcifediol-d6 monohydrate is the deuterium labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels .
2-Hydroxypalmitic acid-d30 (2-Hydroxyhexadecanoic acid-d30) is deuterium labeled 2-Hydroxypalmitic acid. 2-Hydroxypalmitic acid is an intermediate in phytosphingosine metabolism .
Deoxythymidine-5'-triphosphate-d15 (dTTP-d15) dilithium is the deuterium labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA .
Calcitriol-d3 is the deuterium labeled Calcitriol . Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist [4] .
1,3-Dimethoxybenzene-d3 (Resorcinol dimethyl ether-d3) is the deuterium labeled 1,3-Dimethoxybenzene (HY-34487). 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds .
Histamine- 15N3 is the 15N3-labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
H-D-Trp-OH-d5 (D-Tryptophan-d5) is the deuterium labeled H-D-Trp-OH. H-D-Trp-OH is a D-stereoisomer of tryptophan and occasionally found in naturally produced peptides such as the marine venom peptide.
Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
Perospirone-d8 (SM-9018-d8 (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
NAPQI-d3 (N-Acetyl-4-benzoquinone Imine-d3) is the deuterium labeled NAPQI (HY-W017464). NAPQI is the toxic metabolite of Acetaminophen (HY-66005). NAPQI is also an inhibitor of enzymes in the vitamin K cycle. NAPQI is rapidly detoxified by glutathione (GSH), but in situations of GSH deficiency, excess NAPQI reacts with cysteine residues in proteins, causing cell death and toxicity in the liver .
DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers . DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice .
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299 .
Ibuprofen- 13C6 ((±)-Ibuprofen- 13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [4] .
Moxifloxacin-d3-1 hydrochloride (BAY 12-8039-d3-1) is a deuterium labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
Histamine- 13C5 is the 13C labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma [4] .
(Rac)-DPPC-d6 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [4] .
Gimeracil- 13C3 (Gimestat- 13C3) is the 13C-labeled Gimeracil (HY-17469). Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD) .
(±)14,15-DiHETrE-d11 ((±)14(15)-DiHET-d11) is the deuterium labeled (±)14,15-DiHETrE (HY-143664). (±)14,15-DiHETrE is an epoxide hydrolases enzymatically hydrated metabolite of (±)14(15)-EET .
2-(Benzhydrylsulfinyl)acetic acid-d10 (Modafinil acid-d10) is the deuterium labeled 2-(Benzhydrylsulfinyl)acetic acid (HY-W103882). 2-Benzhydrylsulfinylacetic acid (Modafinil acid) is the metabolite of modafinil .
p-Toluic acid-d7 is the deuterium labeled p-Toluic acid . p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Sulfacetamide- 13C6 (Sulphacetamide 13C6) is the 13C6 labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
2-Phenylethyl isothiocyanate-d5 isothiocyanate-d5 is the deuterium labeled 2-Phenylethyl isothiocyanate[1]. 2-Phenylethyl isothiocyanate is a potent antifungal agent. 2-Phenylethyl isothiocyanate significantly inhibited spore germination and mycelial growth of Alternaria alternata, with a MIC (minimum inhibitory concentration) of 1.22 mM. The antifungal effect of 2-Phenylethyl isothiocyanate against Alternaria alternata might be via reduction in toxin content and breakdown of cell membrane integrity[2][3].
Farnesyl pyrophosphate-d2 (Farnesyl diphosphate-d2) triammonium is a deuterium labeled Farnesyl pyrophosphate triammonium (HY-113037C). Farnesyl pyrophosphate ammonium is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate ammonium is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate ammonium is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Tetrahydrofolic acid- 13C6 (L-5,6,7,8-Tetrahydrofolic acid- 13C6) is 13C labeled Tetrahydrofolic acid. Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid .
Fmoc-Trp(Boc)-OH- 13C11, 15N2 (Fmoc-L-Trp(Boc)-OH- 13C11, 15N2) is the 13C-labeled and 15N-labeled Fmoc-Trp(Boc)-OH (HY-W008034). Fmoc-Trp(Boc)-OH (Fmoc-L-Trp(Boc)-OH) is an amino acid derivative with protective groups. Fmoc-Trp(Boc)-OH can self-assemble into stable and pH-responsive spherical nanoparticles, which can load and release bioactive molecules, with good biocompatibility and high cell uptake rate. Fmoc-Trp(Boc)-OH can be used in research on drug delivery .
3-Chloropropane-1,2-diol dipalmitate- 13C3 is 13C labeled 3-Chloropropane-1,2-diol dipalmitate. 3-Chloropropane-1,2-diol dipalmitate is a free fatty acid consisting mainly of diesters .
(R)-3-Hydroxybutanoic acid- 13C2 sodium is the 13C labeled (R)-3-Hydroxybutanoic acid sodium (HY-W015851). (R)-3-Hydroxybutanoic acid sodium is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones .
Tetrahydrofolic acid- 13C5 (L-5,6,7,8-Tetrahydrofolic acid- 13C5) is 13C labeled Tetrahydrofolic acid. Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid .
Guanidine- 13C, 15N3 (hydrochloride)is the 13C-labeled and 15N-labeled Guanidine hydrochloride. Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins .
L-Phenylalanine- 13C9, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Levoglucosan- 13C6 is the 13C labeled Levoglucosan . Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature .
Brivudine- 13C, 15N2 (Bromovinyldeoxyuridine- 13C, 15N2) is 13C and 15N labeled Brivudine. Brivudine is a thymidine analogue with antiviral activity, indicated for the early treatment of acute herpes zoster.
Avanafil- 13C5 (TA1790- 13C5) is 13C labeled Avanafil. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
5-Methyl-1H-benzotriazole-d6 (5-Methylbenzotriazole-d6) is the deuterium labeled 5-Methyl-1H-benzotriazole (HY-W086988). 5-Methyl-1H-benzotriazole is a biological material or organic compound that can be used in life science research .
3-Hydroxybutyric acid-d2 (sodium) is the deuterium labeled 3-Hydroxybutyric acid sodium . 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids .
3-Epiglycyrrhetinic acid-d2 (3α-Glycyrrhetic acid-d2) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
Riluzole- 13C6 (PK 26124- 13C6) is 13C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
N-Nitrosodibutylamine-d18 is the deuterium labeled N-Nitrosodibutylamine . N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water .
Progesterone-d9 is the deuterium labeled Progesterone. Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.
Acemetacin- 13C6 (TVX 1322- 13C6) is 13C labeled Acemetacin. Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
trans-Cinnamic acid-d7 is the deuterium labeled trans-Cinnamic acid . trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1 .
Dapagliflozin- 13C6 (BMS-512148- 13C6) is 13C labeled Dapagliflozin. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Ketorolac- 13C6 (RS37619- 13C6) is 13C labeled Ketorolac. Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorolac tromethamine is also a DDX3 inhibitor that can be used for cancer research [4].
Tranexamic acid- 13C6 (Cyclocapron- 13C6) is 13C labeled Tranexamic acid. Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis [4] .
Cyprodinil- 13C6 (CGA-219417- 13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens .
Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate . Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research . Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells [4] .
Sulfamerazine- 13C6 (RP2632- 13C6) is 13C labeled Sulfamerazine (HY-B0512). Sulfamerazine (RP-2632) is a sulfonamide antibacterial. Sulfamerazine, the monomethyl derivative of sulfadiazine, is 2-sulfanilamido-4-methylpyrimidine. Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthesizes.
p-Cresol sulfate-d7 (potassium) is the deuterium labeled p-Cresyl sulfate potassium. p-Methylphenyl potassium sulfate is a prototype protein-bound uremic toxin[1][2].
Sucrose- 13C6 is the 13C labeled Sucrose . Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preference, and diabetes, et al .
Dimethyl Phthalate- 13C2 (DMP- 13C2) is the 13C-labeled Dimethyl phthalate (HY-N7106). Dimethyl phthalate (DMP) can be used as a plasticizer to impart flexibility to rigid polyvinyl chloride (PVC) resin. Additionally, Dimethyl phthalate is an oral active endocrine disruptor that can cause ovarian dysfunction in mice. Dimethyl phthalate can also induce oxidative stress and apoptosis in cells, thereby affecting blood and red blood cell function in rats .
N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide .
Adenosine monophosphate- 13C5 (AMP- 13C5) is 13C labeled Adenosine monophosphate. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Bis(1-chloro-2-propyl) phosphate-d12 is deuterium labeled Bis(1-chloro-2-propyl) phosphate. Bis(1-chloro-2-propyl) phosphate (BCIPP) is a metabolite of organophosphate flame retardants (OPFR) that may alter energy metabolism by influencing the levels of steroid hormones, such as cortisol and cortisone. Bis(1-chloro-2-propyl) phosphate holds potential for research on metabolism-related diseases caused by environmental exposure .
Amiloride- 15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride . Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC ) and urokinase-type plasminogen activator receptor (uTPA ). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2 [4]) channel.
Bexarotene- 13C6 (LGD1069- 13C6) is 13C labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
N-Dodecyl-β-D-maltoside-d25 (Lauryl Maltoside-d25) is deuterium labeled N-Dodecyl-β-D-maltoside (HY-128974). N-Dodecyl-β-D-maltoside is a non-ionic detergent. N-Dodecyl-β-D-maltoside has strong adsorption on alumina, titanium dioxide and hematite. N-Dodecyl-β-D-maltoside can promote the reactivation of various proteins. N-Dodecyl-β-D-maltoside can effectively stabilize photoactive reaction center complexes (RCs) and inhibit the degradation of Rhodopseudomonas spheroides R-26 reaction center in solution. N-Dodecyl-β-D-maltoside can be used for purification and stabilization of RNA polymerase and for detection of protein-lipid interactions [4].
Ivosidenib- 13C5 (AG-120- 13C5) is 13C labeled Ivosidenib. Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
N-Nitrosodibutylamine-d9 is the deuterium labeled N-Nitrosodibutylamine . N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water .
3-Epiglycyrrhetinic acid-d3 (3α-Glycyrrhetic acid-d3) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Sodium 2-oxopropanoate- 13C3 is the 13C-labeled Sodium 2-oxopropanoate. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS .
Florfenicol- 13C6 (SCH-25298- 13C6) is 13C labeled Florfenicol. Florfenicol ((-)-Florfenicol) is an orally active broad-spectrum antibacterial antibiotic with anti-inflammatory, pro apoptotic, and immunomodulatory functions .
Prasugrel-13C6 is a deuterated labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Ketoprofen- 13C6 (RP-19583- 13C6) is 13C labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity .
1-Bromo-3-methoxybenzene-d3 is the deuterium labeled 1-Bromo-3-methoxybenzene. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
trans-Cinnamic acid-d5 is the deuterium labeled trans-Cinnamic acid . trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1 .
Famotidine- 13C3 (MK-208- 13C3) is the 13C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
N-Palmitoyl-D-sphingomyelin-d9 (Sphingomyelin 16:0-d9) is deuterium labeled N-Palmitoyl-D-sphingomyelin. N-Palmitoyl-D-sphingomyelin (Sphingomyelin 16:0) (Compound SM-03) can be used for the synthesis of lipid nanoparticles .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
Ethyl 11(E)-octadecenoate-d5 (Vaccenic acid ethyl ester-d5) is the deuterium labeled Ethyl 11(E)-octadecenoate (HY-166122). Ethyl 11(E)-octadecenoate is an ester product.
Diclofenac- 13C6 (Sodium) is the 13C6 labeled Diclofenac (Sodium). Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
Penicillin V- 13C6 (potassium) is the 13C6 labeled Penicillin V (potassium). Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis.
Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .
Docosahexaenoic acid ethyl ester-d5-1 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects .
Methyl(E)-cinnamate-d7 is the deuterium labeled Methyl (E)-cinnamate . Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry .
dGTP-d14 (2'-Deoxyguanosine-5'-triphosphate-d14) dilithium is deuterium labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Vandetanib- 13C6 is a 13C labeled Vandetanib (HY-10260) . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
Paroxetine-d2 (CTP 347) is a deuterium labeled Paroxetine (HY-122272). Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches [4].
Ivacaftor- 13C6 (VX-770- 13C6) is 13C labeled Ivacaftor. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities .
Anthracene-9-carboxylic acid-d9 is the deuterium labeled Anthracene-9-carboxylic acid . Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells .
Pomalidomide- 13C5 (CC-4047- 13C5) is 13C labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
2-Oxopropanoate- 13C2 (sodium) is the 13C labeled Sodium 2-oxopropanoate . Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS .
Mead acid-d6 is the deuterium labeled Mead acid. Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency .
Acetyl-L-carnitine-d3 (O-Acetyl-L-carnitine-d3) hydrochloride is the deuterium labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression [4].
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation [4] .
Fenoprofen- 13C6 (LILLY-53858- 13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .
Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Gallic acid-d2 is the deuterium labeled Gallic acid . Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2) . Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities .
Pragliflozin- 13C6 (ASP1941- 13C6) is 13C labeled Ipragliflozin. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent .
Luliconazole- 13C7 (NND 502- 13C7) is 13C labeled Luliconazole. Luliconazole (NND 502)?is a topical antifungal imidazole antibiotic with broad-spectrum and potent antifungal activity. Luliconazole can be used for the research of skin infection, including?dermatophytosis, tinea corporis, tinea pedis?et al .
Mono(5-carboxy-2-ethylpentyl) phthalate-d9 (MECPP-d9) is the deuterium labeled Mono(5-carboxy-2-ethylpentyl) phthalate (HY-133675). Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking .
Sulcatone-d5 (6-Methyl-5-hepten-2-one-d5) is the deuterium labeled Sulcatone (HY-W010435). Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis [4].
DMT-dA(bz) Phosphoramidite-d9 (DA-CE phosphoramidite-d9) is deuterium labeled DMT-dA(bz) Phosphoramidite (HY-W013059). DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA.
3,3-Dimethylbutyric acid-d9 (tert-Butylacetic acid-d9) is a deuterated derivative of 3,3-Dimethylbutyric acid, which is a short-chain branched carboxylic acid and can be used in organic synthesis .
Favipiravir- 13C3 is the 13C labeled isotope of Favipiravir- 13C3(HY-14768 ).Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
Empagliflozin- 13C6 (BI 10773- 13C6) is 13C labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2 .
Saxagliptin- 13C2 (BMS-477118- 13C2) is 13C labeled Saxagliptin. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4(DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
DL-Arginine- 13C6 hydrochloride is 13C-labeled DL-Arginine hydrochloride (HY-W014375). DL-Arginine ((±)-Arginine) hydrochloride is the racemic compound of L-Arginine (HY-N0455) and D-Arginine (HY-W016781). Arginine is an essential amino acid that requires additional supplementation in traumatic or diseased conditions. Arginine is involved in T cell activation, proliferation, and differentiation, and affects the function of immune cells .
Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide .
Exatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research .
Bezafibrate- 13C6 (BM15075- 13C6) is 13C labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
D,L-Sulforaphane glutathione-d5 (DL-SFN-GSH-d5) is deuterium labeled DL-Sulforaphane glutathione. DL-Sulforaphane glutathione (DL-SFN-GSH) is a metabolite of Sulforaphane (HY-13755) in rat plasma .
Sumatriptan-d6 is the deuterium labeled Sumatriptan. Sumatriptan is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research .
(E)-10-Hydroxynortriptyline-d3 is a deuterium labeled (E)-10-Hydroxy Nortriptyline. (E)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression .
Fludioxonil- 13C3 (CGA-173506- 13C3) is 13C labeled Fludioxonil. Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells [4].
2-Hydroxyestrone- 13C6 is the 13C-labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic .
Sumatriptan-d5 is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [4].
Meclofenamic acid- 13C6 is the 13C6 labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker.
Methyl (E)-cinnamate-d5 is the deuterium labeled Methyl (E)-cinnamate . Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry .
Ezetimibe- 13C6 (SCH 58235- 13C6) is the 13C-labeled Ezetimibe (HY-17376). Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Amprenavir- 13C6 (VX-478- 13C6) is 13C labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.09 μM.
Loratadine- 13C6 (SCH 29851- 13C6) is 13C labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
1-Naphthoic acid-d7 (Naphthalene-1-carboxylic acid-d7) is the deuterium labeled 1-Naphthoic acid (HY-Y0236). Naphthalene-1-carboxylic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Urea- 15N2 is the 15N-labeled Urea. Urea is a powerful protein denaturant via both direct and indirect mechanisms . A potent emollient and keratolytic agent . Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function . Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Rimeporide- 15N3 (hydrochloride) (EMD-87580- 15N3 (hydrochloride)) is 15N labeled Rimeporide hydrochloride. Rimeporide hydrochloride (EMD-87580 hydrochloride) is a potent and selective inhibitor of the Na +/H + exchanger (NHE-1).
Nimesulide- 13C6 (R805- 13C6) is 13C labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
Betrixaban- 13C6 (PRT054021- 13C6) is 13C labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
Tazarotene- 13C6 (AGN 190168- 13C6) is 13C labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2-Ketoglutaric acid-d6 (Alpha-Ketoglutaric acid-d6) is the deuterium labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
Amiloride- 15N3 (MK-870- 15N3) is 15N labeled Amiloride. Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC ) and urokinase-type plasminogen activator receptor (uTPA ). Amiloride is a blocker of polycystin-2 (PC2; TRPP2 ) channel.
Deferasirox- 13C6 (ICL 670- 13C6) is 13C labeled Deferasirox. Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload .
Atenolol- 13C6 ((RS)-Atenolol- 13C6) is 13C labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris .
Hippuric acid- 13C6 (Benzoylglycine- 13C6) is 13C labeled Hippuric acid. Hippuric Acid is an orally active metabolite. Hippuric Acid can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Hippuric Acid decreases NRF2, MMP9 and leads to ROS accumulation. Hippuric Acid activates TGFβ/SMAD signaling. Hippuric Acid improves hyperuricemia and colitis. Hippuric Acid can also be used in cardiovascular disease research [4].
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Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation .
DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals [4].
Diflunisal- 13C6 (MK-647- 13C6) is 13C labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain , binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) .
Dimethyl phthalate- 13C6 (DMP- 13C6) is the 13C-labeled Dimethyl phthalate (HY-N7106). Dimethyl phthalate (DMP) can be used as a plasticizer to impart flexibility to rigid polyvinyl chloride (PVC) resin. Additionally, Dimethyl phthalate is an oral active endocrine disruptor that can cause ovarian dysfunction in mice. Dimethyl phthalate can also induce oxidative stress and apoptosis in cells, thereby affecting blood and red blood cell function in rats .
16-Ketoestradiol-d5 (16-keto-17β-Estradiol-d5) is the deuterium labeled 16-Ketoestradiol (HY-W587691). 6-Ketoestradiol is an active metabolite of the endogenous estrogen estrone .
Isosorbide dinitrate- 13C6 is the 13C labeled Isosorbide dinitrate . Isosorbide dinitrate (ISDN) is an NO donor that prevents LV remodeling and degradation of cardiac function following myocardial infarction (MI) .
trans-2-Decenal-d2 is deuterated labeled trans-2-Decenal (HY-W015551). trans-2-Decenal is an important raw material and intermediate used in organic synthesis, medicine, pesticides and dyes.
2-(Dodecyloxy)ethanol-d25 (Ethylene glycol monododecyl ether-d25) is the deuterium labeled 2-(Dodecyloxy)ethanol (HY-W250300). 2-(Dodecyloxy)ethanol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Angiotensin II human- 13C6, 15N TFA (Ang II- 13C6, 15N TFA) is 13C- and 15N-labeled Angiotensin II human (TFA) (HY-13948B). Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions .
Liothyronine- 13C9, 15N is the 13C and 15N labeled Liothyronine . Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively [4].
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N) is the 13C and 15N labeled AICAR (HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
Nicotinamide- 15N, 13C3 is the 13C-labeled and 15N-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Tofacitinib- 13C3, 15N (Tasocitinib- 13C3, 15N) is 13C and 15N labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
2-(1-Ethoxyethylidene)malononitrile- 13C2 (Propanedinitrile, 2-(1-ethoxyethylidene)- 13C2) is the 13C-labeled 2-(1-Ethoxyethylidene)malononitrile (HY-W008403).
Entecavir- 13C2, 15N (BMS200475- 13C2, 15N; SQ34676- 13C2, 15N) is a 13C- and 15N-labeled Entecavir (HY-13623). Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
Tegafur- 13C, 15N2 (FT 207- 13C, 15N2) is the 13C- and 15N-labeled Tegafur (HY-17400). Tegafur (FT 207; NSC 148958) is a chemotherapeutic 5-FU proagent used in the treatment of cancers; is a component of tegafur-uracil.
L-Serine- 13C3, 15N is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Mandelic acid-2,3,4,5,6-d5 is the deuterium labeled Mandelic acid. Mandelic acid ((±)-Mandelic acid), an alpha-hydroxycarboxylic acid, has been widely used as an intermediate of pharmaceutical and fine chemicals. Mandelic acid shows antimicrobial activity and has been used for the research of urinary tract infections and vaginal trichomoniasis. Mandelic acid exhibits high sperm-immobilizing activity and low vaginal irritation .
Serotonin- 13C2, 15N hydrochloride is the 13C- and 15N-labeled Serotonin hydrochloride (HY-B1473). Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Hypoxanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Didanosine- 13C2, 15N (2',3'-Dideoxyinosine- 13C2, 15N; ddI- 13C2, 15N) is the 13C- and 15N-labeled labeled Didanosine (HY-B0249). Didanosine (2',3'-Dideoxyinosine; ddI) is a a potent and orally active dideoxynucleoside analogue, and also is a potent nucleoside reverse transcriptase inhibitor. Didanosine shows antiretroviral activity for HIV .
Hypoxanthine- 13C2, 15N is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Cefdinir- 13C, 15N2 (FK-482- 13C, 15N2) is 13C and 15N labeled Cefdinir. Cefdinir (FK-482) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for infections caused by several Gram-negative and Gram-positive bacteria. Cefdinir can be used for the research of common bacterial infections of the ear, sinus, throat, and skin .
2'-Deoxyguanosine- 13C, 15N2 (Deoxyguanosine- 13C, 15N2; Guanine deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled 2'-Deoxyguanosine (HY-17563). 2’-Deoxyguanosine (Deoxyguanosine) is a purine nucleoside with a variety of biological activities. 2’-Deoxyguanosine can induce DNA division in mouse thymus cells. 2’-Deoxyguanosine is a potent cell division inhibitor in plant cells .
Zileuton- 13C2, 15N is 15N and 13C labeled Zileuton (HY-14164). Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
Lamotrigine- 13C7, 15N (LTG- 13C7, 15N) is 13C and 15N labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
6-Mercaptopurine- 13C2, 15N is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
1,2-Dioleoyl-sn-glycero-3-phosphocholine-d9 is deuterium labeled 1,2-Dioleoyl-sn-glycero-3-phosphocholine. 1,2-Dioleoyl-sn-glycero-3-phosphocholine (DOPC) is a phospholipid and is commonly used alone, or with other components, in the generation of micelle
Fenofibric acid- 13C8 (FNF acid- 13C8) is 13C labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine-d70 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine. 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE) is a phosphoethanolamine (PE) lipid that can be used in the synthesis
Uridine- 13C9 (β-Uridine- 13C9) is a 13C9-labeled form of Uridine (HY-B1449). Uridine (β-Uridine) is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Oxiran-2-ylmethyl hexadecanoate-d31 is deuterium labeled Glycidyl palmitate. Glycidyl Palmitate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
D-Ribofuranose- 13C5 (D-Ribose- 13C5) is the 13C-labeled D-Ribofuranose (HY-113375). D-Ribofuranose (D-Ribose) is an endogenous metabolite present in Cerebrospinal_Fluid that can be used for the research of Ribose 5 Phosphate Isomerase Deficiency and Medium Chain Acyl Co A Dehydrogenase Deficiency .
Taurine- 13C2 is the 13C-labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
trans-2-Hexenal-d2-1 is the deuterium labeled trans-2-Hexenal (HY-128429). trans-2-Hexenal ((E)-2-Hexenal) is a volatile compound widely present in fresh plants, vegetables, and fruits, with a unique leafy aroma. trans-2-Hexenal has antifungal activity and can also inhibit the germination of soybean seeds and the growth of seedlings. In addition, trans-2-Hexenal can be used to determine low-molecular-weight carbonyl compounds that are reactive with biological nucleophiles in biological samples .
Uridine 5'-monophosphate-d11 (5'- Uridylic acid-d11) dilithium is deuterium labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Lansoprazole sulfone- 13C6 (AG-1813- 13C6) is 13C labeled Lansoprazole sulfone. Lansoprazole sulfone (AG-1813) is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease .
L-Phenylalanine-d is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
L-Phenylalanine-d2 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Avibactam sodium salt- 13C5 (NXL-104- 13C5) is 13C labeled Avibactam (sodium). Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
DPPG-d62 (sodium) is deuterium labeled DPPG. DPPG sodium (1,2-Dipalmitoyl-sn-glycero-3-PG sodium) is a phospholipid containing the long-chain(16:0) palmitic acid inserted at the sn-1 and sn-2 positions. DPPG sodium is used in the generation of micelles, l
L-Valine- 13C5 ((S)-Valine- 13C5) is the 13C-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Ibuprofen- 13C,d3 is the 13C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively .
L-Arginine- 13C6 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Benzene-1,3,5-tricarboxylic acid-d3 is the deuterium labeled Benzene-1,3,5-tricarboxylic acid (HY-78985). Benzene-1,3,5-tricarboxylic acid (Trimesic acid) is a scaffold. Benzene-1,3,5-tricarboxylic acid enhances the binding ability of bicyclic peptides to proteins and improves the mechanical stability of hydrogels .
Phosphoenolpyruvic acid (potassium)- 13C2 is the 13C labeled Phosphoenolpyruvic acid potassium (HY-W008807) . Phosphoenolpyruvic acid (Phosphoenolpyruvate) potassium is a glycolysis metabolite with a high-energy phosphate group. Phosphoenolpyruvic acid potassium is involved in glycolysis and gluconeogenesis, and used as energy source to produce ATP, under the energy-limited conditions. Phosphoenolpyruvic acid potassium also exhibits cytoprotective and anti-oxidative properties .
L-Arginine- 15N2 (hydrochloride) is the 15N-labeled L-Arginine (hydrochloride). L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
L-Phenylalanine-d7 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Nifedipine-13C8 is a deuterated labeled Nifedipine . Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
Homovanillic Acid- 13C6 (Vanilacetic acid- 13C6) is the 13C-labeled Homovanillic acid (HY-N0384). Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
L-Phenylalanine-d8 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Indole-3-carboxaldehyde- 13C (3-Formylindole- 13C) is a 13C labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde (3-Formylindole), a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin .
Diethylene glycol-d8 (2,2'-Oxybis(ethan-1-ol)-d8) is the deuterium labeled Diethylene glycol (HY-B1952). Diethylene glycol has excellent solubility and reactivity in certain chemical reactions and can help accelerate the activation of certain reactants.
Myrcene- 13C3 is 13C labeled Myrcene (HY-N0803). Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity [4] .
Tolfenamic acid- 13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
Cefadroxil- 13C6 (BL-S 578- 13C6) is 13C labeled Cefadroxil (HY-B1190). Cefadroxil is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain [4] .
N-(Phenylacetyl-d5)glycine is the deuterium labeled Phenylacetylglycine. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion .
2,4-Di-tert-butylphenol-d19(2,4-DTBP-d19) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
Saquinavir- 13C6 (Ro 31-8959- 13C6) is 13C labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells .
DPPC-13C2 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [4] .
Adipic acid- 13C2 (Hexanedioic acid- 13C2) is 13C labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Vitamin B12- 13C7 is the 13C-labeled Vitamin B12. Vitamin B12 is a vitamin. Vitamin B12 plays a key role in the normal functioning of the brain and nervous system, and for the formation of blood .
N4-Acetylsulfamethoxazole- 13C6 (Acetylsulfamethoxazole- 13C6) is the 13C-labeled N4-Acetylsulfamethoxazole (HY-W013266). N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of?Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections .
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect .
Lactic acid- 13C2 (DL-Lactic acid- 13C2) sodium is the 13C-labeled Lactic acid sodium . Lactic acid (DL-Lactic acid) sodium is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium is an oncometabolite and has immune protective role of lactate in anti-tumor immunity . Lactic acid sodium also has antimicrobial activity, which can be used as a food preservative .
Phenylglyoxylic acid- 13C8 (Benzoylformic acid- 13C8) is the 13C-labeled Phenylglyoxylic acid (HY-W010255). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human. Phenylglyoxylic acid can be used as drug intermediate for synthesis of antineoplastic compounds .
N-Hexanoyl-L-Homoserine lactone-d3 (C6-HSL-d3) is deuterium labeled N-Hexanoyl-L-homoserine lactone. N-Hexanoyl-L-homoserine lactone is a short-chained N-acyl homoserine lactone (AHL). Diatoms are frequently found in association with Proteobacteria, many members of which employ cell-to-cell communication via AHLs in aquatic habitats .
Pyruvic acid- 13C2 (Acetylformic acid- 13C2) is the 13C-labeled Pyruvic acid (HY-Y0781). Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats.
Ercalcitriol-d3 is the deuterium labeled Ercalcitriol. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Glycolic acid- 13C2 is the 13C-labeled Glycolic acid (HY-W015967). Glycolic acid- 13C2 is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
Secalciferol-d6 is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification .
2,4-Di-tert-butylphenol-d21(2,4-DTBP-d21) is the deuterium labeled 2,4-Di-tert-butylphenol (HY-W014589). 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
Triacetonamine-d17 (2,2,6,6-Tetramethyl-4-piperidone-d17) is the deuterium labeled Triacetonamine. Triacetonamine has oral activity and can induce acute liver failure (ALF) in rats .
Diphenyl ether- 13C12 is 13C labeled Diphenyl ether. Oxydibenzene is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Moxonidine- 13C,d3 (BDF5895- 13C,d3) is the 13C-labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
Uridine- 13C5 (β-Uridine- 13C5) is a 13C labeled Uridine (HY-B1449). Uridine (β-Uridine) is a nucleoside compound consisting of uracil and a ribose ring, which are linked by a β-N1- glycosyl bond.
Fructose-alanine- 13C6 is 13C labeled Fructose-alanine. Fructose-alanine, an amadori compound, is an aroma precursor that formed in the initial phase of the Maillard reaction (MR). Fructose-alanine can be isolated from tobacco, miso and white wine. Fructose-alanine significantly induces oxidative browning and correlates with Maillard product (furfuryl alcohol) with a roasted and sweet aroma. Fructose-alanine can be used for food industry and tobacco processing research [4].
Adipic acid- 13C6 (Hexanedioic acid- 13C6) is the 13C labeled Adipic acid (HY-W017522). Adipic acid (Hexanedioic acid) is an orally active compound with anti-HSV-1 activity. Adipic acid has low toxicity and can be used as a food additive and a gelling agent. Adipic acid can also be used in the synthesis of lubricants, artificial resins, plastics, etc .
Octachlorodibenzo-p-dioxin- 13C12 is Octachlorodibenzo-p-dioxin- 13 C-labeled octachlorodibenzo-p-dioxin- 13C. Octachlorodibenzo-p-dioxin is a widespread environmental pollutant .
Metformin- 13C2 (1,1-Dimethylbiguanide- 13C2) hydrochloride is the 13C-labeled Metformin hydrochloride (HY-17471A). Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo [4] .
Pyruvic acid-13C is isotype-labeled compound of Pyruvic acid. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats .
5'-Deoxy-5-fluorocytidine-d3 is deuterated labeled 5'-Deoxy-5-fluorocytidine (HY-W009538). 5'-Deoxy-5-fluorocytidine (5-Fluoro-5'-deoxycytidine) is a cytidine analog and metabolite of Capecitabine (HY-B0016). 5'-Deoxy-5-fluorocytidine is converted from Capecitabine by carboxylesterase in the liver. 5'-Deoxy-5-fluorocytidine is deaminated by cytidine deaminase to generate 5'-deoxy-5-fluorouridine, which is finally converted into 5-fluorouracil (HY-90006) by thymidine phosphorylase in tumor tissues to exert anti-tumor effects. 5'-Deoxy-5-fluorocytidine is used in the researches for solid tumors such as colorectal cancer, non-small cell lung cancer and breast cancer [4].
trans-Stilbene- 13C2 ((E)-Stilbene- 13C2) is the 13C labeled trans-Stilbene (HY-128793) . trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens .
Eplerenone- 13C,d3 (Epoxymexrenone- 13C,d3) is 13C labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC50 value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV) .
Sulfamethoxazole- 13C6 (Ro 4-2130- 13C6) is a 13C labeled Sulfamethoxazole (HY-B0322). Sulfamethoxazole (Ro 4-2130) is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
N-Acetylglycine- 13C2, 15N (Aceturic acid- 13C2, 15N) is the 13C- and 15N-labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
Orotic acid- 13C, 15N2 (monohydrate) is the 13C and 15N labeled Orotic acid . Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats [4].
Salicylic acid- 13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity .
N-Lactoyl-Phenylalanine- 13C6 (Lac-Phe- 13C6) is 13C labeled N-Lactoyl-Phenylalanine. N-Lactoyl-Phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-Phenylalanine can reduce obesity and improve glucose tolerance .
Pemetrexed disodium- 13C5 (LY231514 disodium- 13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d62 (POPC-d64) is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for the preparation of liposomes and studying the properties of lipid bilayers .
3-Hydroxy Midostaurin- 13C6 (CGP52421- 13C6) is the 13C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
Zafirlukast- 13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
5,6-trans-Bimatoprost-d5 (5,6-trans-AGN 192024-d5) is the deuterium labeled 5,6-trans-Bimatoprost (HY-B0191A). 5,6-trans-Bimatoprost is the isomer of Bimatoprost (HY-B0191), and can be used as an experimental control. Bimatoprost is a prostaglandin analogue that can be used in studies of ocular hypertension and glaucoma and also has anti-fat formation effects.
Selpercatinib- 13C,d3 (LOXO-292- 13C,d3) is 13C labeled Selpercatinib. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity .
5-Methylcytidine 5′-triphosphate-d3 trisodium is the deuterium labeled 5-Methylcytidine 5’-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5′-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5′-triphosphate trisodium can apply in replacing unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Sucrose- 13C6-1 is 13C labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose?can be applied in some animal models, including metabolic disease, obesity,?diet on preference,?and diabetes, et al .
Adenosine-d-2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Chlortetracycline-13C,d3 hydrochloride (7-Chlorotetracycline-13C,d3 hydrochloride) is the 13C- and deuterium labeled Chlortetracycline hydrochloride (HY-B1327). Chlortetracycline hydrochloride is an orally active, selective antibiotic, that inhibits methanogenic bacteria through inhibition of bacterial protein synthesis. Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, that inhibits binding of aminoacyl-tRNA to ribosomes [4] .
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Axitinib- 13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50 values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .
17β-Estradiol sulfate-d3 sodium (17β-Estradiol 3-sulfate-d3 sodium) is the deuterium labeled 17β-Estradiol sulfate sodium (HY-141672). 17β-Estradiol sulfate sodium, also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid .
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride . Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Sulfasalazine-d3, 15N is 15N and deuterated labeled Sulfasalazine (HY-14655). Sulfasalazine (NSC 667219) is an anti-rheumatic agent for the research of rheumatoid arthritis and ulcerative colitis. Sulfasalazine can suppress NF-κB activity. Sulfasalazine is a type 1 ferroptosis inducer [4].
Emtricitabine- 15N,d2 is a 15N-labeled and deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [4] .
Succinic acid- 13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
Moxonidine- 13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis [4] .
Adenosine-d-1 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib . Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Guanosine triphosphate- 15N5 (GTP- 15N5) dilithium is 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Fmoc-Gly-OH- 13C2 (Fmoc-glycine- 13C2) is a 13C-labeled Fmoc-Gly-OH (HY-Y1250). Fmoc-Gly-OH (Fmoc glycine) is a Fmoc-protected glycine derivative, can be used for the synthesis of compounds .
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively .
Triclocarban- 13C6 is the 13C labeled isotope of Triclocarban (HY-B1805). Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes .
3-Phenoxybenzoic acid- 13C6 is the 13C6 labeled 3-Phenoxybenzoic acid. 3-Phenoxybenzoic acid is the metabolite of pyrethroid insecticides. 3-Phenoxybenzoic acid induces immunotoxicity and oxidative stress, and inhibits the phagocytic ability of macrophages .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d31 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
Linagliptin- 13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levomefolic acid- 13C5 is the 13C labeled Levomefolic acid . Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid (HY-B0172A). Isoallolithocholic acid is a T cell regulator and enhances regulatory T cells (Tregs) differentiation .
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base . Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ [4].
Saxagliptin-15N,d2 Hydrochloride (BMS-477118-15N,d2 Hydrochloride) is the 15N and deuterium labeled isotope of Saxagliptin (HY-10285). Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4(DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
Raltegravir- 13C,d3 potassium is 13C labeled Raltegravir potassium (HY-10353A). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
Pravastatin- 13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
L-Alanine-1,2- 13C2 (Alanine- 13C2) is 13C labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
2'-Deoxy-N-ethylguanosine-d6 (N2-Ethyl-2'-deoxyguanosine-d6) is the deuterium labeled 2-(Ethylamino)-9-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1H-purin-6(9H)-one (HY-W013267).
Guanosine triphosphate- 13C10 (GTP- 13C10) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
Cholestenone- 13C2 is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells .
D-α-Hydroxyglutaric acid-d5 disodium (Disodium (R)-2-hydroxyglutarate-d5) is the deuterium labeled D-α-Hydroxyglutaric acid disodium (HY-100542). D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling [4] .
rac-1-Linoleoyl-3-chloropropanediol-d5 is deuterium labeled 1-Linoleoyl-3-chloropropanediolte. 1-Linoleoyl-3-chloropropanediolte (3-Chloro-2-hydroxypropyl (9Z,12Z)-octadeca-9,12-dienoate) is an ester product .
Flurbiprofen- 13C,d3 is the 13C- and deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d82 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
MTSSL- 15N,d15-1 (Otmpmms- 15N,d15) is the deuterium and 15N-labeled MTSSL (HY-130509). MTSSL (Otmpmms) is highly reactive thiol-specific spin label, which is used to label protein thiol residues for protein structure and dynamics determination and protein-protein interaction studies .
Thiabendazole- 13C6 is the 13C6 labeled Thiabendazole. Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
2,2-Dibromomalonamide- 13C3 (Dibromo Malonamide- 13C3) is the 13C-labeled 2,2-Dibromomalonamide (HY-W324382). 2,2-Dibromomalonamide is a biochemical agent .
Fluvoxamine- 13C, d3 maleate is 13C and deuterated labeled Fluvoxamine maleate (HY-B0103A). Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
Butanedioic acid- 13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Velpatasvir- 13C,d3 (GS-5816- 13C,d3) is 13C and deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
Riociguat- 13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
Benzyl 4-hydroxybenzoate- 13C6 (Benzyl Paraben- 13C6) is the 13C-labeled Benzyl 4-hydroxybenzoate (HY-W013482). Benzyl 4-hydroxybenzoate is a prominent material. Benzyl 4-hydroxybenzoate can be used as an excipient, such as bacteriostatic agent, preservative. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Zafirlukast- 13C,d3 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Norflurazon- 13C,d3 (SAN 9789- 13C,d3) is the deuterium and 13C-labeled Norflurazon (HY-114849). Norflurazon (SAN 9789) is a bleaching herbicide. Norflurazon can block carotenoid biosynthesis by inhibiting phytoene desaturase activity .
Benoxaprofen- 13C,d3 (LRCL 3794- 13C,d3) is the deuterium and 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a potent and long-acting anti-inflammatory and antipyretic compound. Benoxaprofen is a relatively weak inhibitor of cyclooxygenase in in vitro systems, inhibits lipoxygenase in other systems, and inhibits monocyte migration in some animal models of inflammation .
Rabeprazole- 13C,d3 (sodium) (LY307640- 13C,d3 (sodium)) is 13C labeled Rabeprazole (sodium). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux .
L-Histidine- 15N3 hydrochloride hydrate is the 15N-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Acetyl-L-carnitine-d3-1 (O-Acetyl-L-carnitine-d3-1) hydrochloride is the deuterium labeled Acetyl-L-carnitine hydrochloride (HY-B0762). Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression .
5-Methylcytidine 5'-triphosphate-d8 trisodium is the deuterium-labeled form of 5-Methylcytidine 5'-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5'-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5'-triphosphate trisodium can be used to replace unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Asenapine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
Trelagliptin-13C,d3 is a deuterated labeled Trelagliptin . Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) .
Lamivudine- 15N,d2 is 15N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
Methyl arachidonate- 13C5 (Arachidonic acid methyl ester- 13C5) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
Acetophenone- 13C8 (1-Phenylethan-1-One- 13C8) is the 13C-labeled Acetophenone (HY-Y0989). Acetophenone (1-Phenylethan-1-One) is an organic compound with simple structure. Acetophenone can be bioreduced to phenylethanol (PEA) .
Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
4-Methyl-2-oxopentanoic acid-d7 (α-Ketoisocaproic acid-d7) sodium is the deuterium labeled 4-Methyl-2-oxopentanoic acid (HY-W012722).4-Methyl-2-oxopentanoic acid is a metabolite of L-leucine and is involved in energy metabolism. 4-Methyl-2-oxopentanoic acid increases endoplasmic reticulum stress, promotes lipid accumulation in preadipocytes and insulin resistance by impairing mTOR and autophagy signaling pathways .
Argininic acid- 13C6 (L-Argininic Acid- 13C6) is the 13C-labeled Argininic acid (HY-113079). Argininic acid is an α-amino acid that is used in the biosynthesis of proteins.
1-(4-Chlorophenyl)cyclobutanecarbonitrile-d6(1-(4-Chlorophenyl)-1-cyclobutanecarbonitrile-d6) is the deuterium labeled 1-(4-Chlorophenyl)cyclobutanecarbonitrile (HY-W010002).
2-Methyl-3-(trifluoromethyl)aniline-d3 (3-Trifluoromethyl-2-methylaniline-d3) is deuterium labeled 2-Methyl-3-(trifluoromethyl)aniline. 2-Methyl-3-(trifluoromethyl)aniline is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Butenafine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled. Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Triclocarban- 13C13 (3,4,4'-Trichlorocarbanilide- 13C13) is 13C labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes [4].
Adenosine monophosphate- 13C10 (AMP- 13C10) dilithium is 13C-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Asenapine- 13C,d3 Maleate is the deuterium labeled and 13C-Asenapine Maleate (HY-11100). Asenapine (Org 5222) Maleate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine Maleate can be used in the research of schizophrenia and bipolar disorder .
Sumatriptan-d6 (formate) (GR 43175 free base-d6 (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [4] .
L-Histidine- 13C6 (hydrochloride hydrate) is the 13C-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
Methyl Paraben- 13C6 (Methyl 4-hydroxybenzoate- 13C6) is a 13C labeled Methyl Paraben (HY-N0349) . Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity .
Rabeprazole-13C,d3 is a deuterated labeled Rabeprazole . Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux [4].
2,3-Diphosphoglyceric acid-d3 ammonium (2,3-DPG-d3 ammonium) is the deuterium labeled 2,3-Diphosphoglyceric acid (HY-113050). 2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2, 3-diphosphoglyceric acid has antiparasitic activity. 2,3-Diphosphoglyceric acid can be used in the study of Alzheimer's disease (AD) [4].
Ketoprofen- 13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively .
Carisbamate-d2,- 15N (RWJ-333369-d2,- 15N) is the deuterium labeled Carisbamate (HY-14948). Carisbamate (RWJ-333369) is an orally active neuromodulator. Carisbamate prevents the development and production of epilep-like discharges and has a neuroprotective effect after in vitro epilepticus-like injury. Carisbamate has good antiepileptic activity in genetic models of generalized and nonconvulsive epilepsy .
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Oseltamivir- 13C,d3 (phosphate) (GS 4104- 13C,d3 (phosphate)) is 13C labeled Oseltamivir (phosphate). Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Asenapine-d3, 13C (Org 5222-d3, 13C) is deuterium and 13C labeled Asenapine. Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder .
Fmoc-Gly-OH-2,2-d2 (Fmoc-glycine-2,2-d2) is the deuterium labeled Fmoc-Gly-OH (HY-Y1250). Fmoc-Gly-OH (Fmoc glycine) is a Fmoc-protected glycine derivative, can be used for the synthesis of compounds .
Lactic acid-d3 (DL-Lactic acid-d3) sodium (60% in water) is the deuterium labeled Lactic acid sodium (60% in water) (HY-B2227B) . Lactic acid (DL-Lactic acid) sodium (60% w/w in water) is a hydroxycarboxylic acid receptor 1 (HCAR1) activator and an epigenetic modulator inducing lysine residues lactylation. Lactic acid sodium (60% w/w in water) is a glycolysis end-product, bridging the gap between glycolysis and oxidative phosphorylation. Lactic acid sodium (60% w/w in water) is an oncometabolite and has immune protective role of lactate in anti-tumor immunity . Lactic acid sodium (60% w/w in water) also has antimicrobial activity, which can be used as a food preservative .
Tecarfarin- 13C,d3 (ATI-5923- 13C,d3) is 13C labeled Tecarfarin. Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X . Tecarfarin has the antithrombotic activity .
Hypoxanthine- 13C2, 15N-1 is a 15N-labeled and 13C-labled Hypoxanthine (HY-N0091). Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
β-Alanine- 13C3, 15N is the 13C- and 15N-labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
(1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide-d4 is deuterated labeled (1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide.
2′,2′-Difluorodeoxyuridine- 13C, 15N2 (dFdU- 13C, 15N2) is a 13C- and 15N-labeled compound. 2’,2’-Difluorodeoxyuridine (dFdU) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells [4].
O-Phospho-L-serine- 13C3, 15N is the 13C- and 15N-labeled O-Phospho-L-serine. O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2 .
L-Valine- 15N,d8 ((S)-Valine- 15N,d8) is the deuterium and 15N labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
(2R)-Octyl-α-hydroxyglutarate-d17 ((2R)-Octyl-2-HG-d17) is deuterium labeled (2R)-Octyl-α-hydroxyglutarate (HY-103641). (2R)-Octyl-α-hydroxyglutarate is a modified form of S-isomer 2-Hydroxyglutarate .
1-Palmitoyl-sn-glycero-3-phosphocholine-d31 (16:0 Lyso PC-d31) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Indole-3-carboxaldehyde- 13C8 (3-Formylindole- 13C8) is the 13C-labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde, a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin. Indole-3-carboxaldehyde also enhances the epithelial barrier and anti-inflammatory activity in the intestinal tract .
L-Glutamine- 13C5 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Apixaban- 13C,d3 (BMS-562247-01- 13C,d3) is a deuterium and 13C labeled Apixaban (HY-50667). Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively .
ATP- 13C2 (Adenosine 5'-triphosphate- 13C2) dilithium is 13C-labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
(Z)-Aconitic acid- 13C6 is the 13C-labeled (Z)-Aconitic acid (HY-W016814). (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is the cis-isomer of Aconitic acid. (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is an intermediate in the tricarboxylic acid cycle produced by the dehydration of citric acid.
Calcifediol- 13C5 monohydrate is the 13C-labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels .
Deoxythymidine-5'-triphosphate- 15N2 (dTTP- 15N2) dilithium is 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin . Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
ATP- 13C10 (Adenosine 5'-triphosphate- 13C10) dilithium is 13C-labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Glycidyl palmitate- 13C16 (Oxiran-2-ylmethyl palmitate- 13C16) is the 13C-labeled Glycidyl palmitate (HY-W127578). Glycidyl Palmitate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
L-Alanine- 13C3 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
MCPA- 13C8 is the 13C-labeled MCPA (HY-B0859). MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds [4] .
1-Palmitoyl-sn-glycero-3-phosphocholine-d9 (16:0 Lyso PC-d9) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Flavin adenine dinucleotide- 13C5 (FAD- 13C5) ammonium is 13C labeled Flavin adenine dinucleotide (HY-B1654). Flavin adenine dinucleotide (FAD) is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.
2,3’-Anhydrothymidine-d3 (2’-Deoxy-3’,2-anhydro-5-methyluridine-d3) is the deuterium labeled 2,3’-Anhydrothymidine (HY-154340). 2,3’-Anhydrothymidine; 2’-Deoxy-3’,2-anhydro-5-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
1-Palmitoyl-sn-glycero-3-phosphocholine-d49 (16:0 Lyso PC-d49) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Guanosine 5'-diphosphate- 13C10 (GDP- 13C10) dilithium is 13C-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
1-Acetyl-4-(4-hydroxyphenyl)piperazine-d8 (Tetraethoxy C methyl propane-d8) is the deuterium labeled 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone (HY-W014037).
DL-Lysine- 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 15N2 hydrochloride) is 15N labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
2-(3,4-Dimethoxyphenyl)-3-methylbutanenitrile-d7 (alpha-Isopropyl homoveratronitrile-d7) is the deuterium labeled 2-(3,4-Dimethoxyphenyl)-3-methylbutanenitrile (HY-W101691).
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
Uridine 5'-monophosphate- 15N2 (5'-Uridylic acid- 15N2) is the 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
Caffeic acid- 13C3 is an 13C labeled caffeic acid. Caffeic acid is a phytonutrient belonging to the flavonoids. Caffeic acid and its derivatives, are potential antimicrobial agents, chronic infection induced by microbes such as bacteria, fungi, and viruses .
L-Alanine- 13C2 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
2-Methyl-2-[(trimethylsilyl)oxy]propanenitrile-d6 (2-methyl-2-trimethylsilyloxypropanenitrile-d6) is the deuterium labeled 2-Methyl-2-[(trimethylsilyl)oxy]propanenitrile (HY-W176004).
AChE-IN-23-d10 (4-Amino-Alpha-diethyl amino-o-cresol-d10 (dihydrochloride)) is the deuterium labeled AChE-IN-23 (HY-W077226). AChE-IN-23 (compound 3h) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 48.3 μM .
Homovanillic acid- 13C,d3 (Vanilacetic acid- 13C,d3) is 13C and deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
Guanosine 5'-diphosphate- 15N5 (GDP- 15N5) dilithium is 15N labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI) .
5-Hydroxymethylcytosine- 13C,d2 is the 13C and deuterium labeled 5-Hydroxymethylcytosine (HY-W018324). 5-Hydroxymethylcytosine (5hmC) is an oxidized forms of 5-methylcytosine (5mC) in mammalian DNA. 5-Hydroxymethylcytosine is produced from 5mC in an enzymatic pathway involving three 5mC oxidases, Ten-eleven translocation (TET)1, TET2, and TET3. The conversion of 5mC into 5hmC can be the first step in a pathway leading towards DNA demethylation. 5-Hydroxymethylcytosine is associated with gene transcription and frequently used as a mark to investigate dynamic DNA methylation conversion during mammalian development. 5-Hydroxymethylcytosine can be used for the study of non-small cell lung cancer (NSCLC), neurodegenerative diseases (Alzheimer’s, Parkinson’s) and hematological malignancies (acute myeloid leukemia, myelodysplastic syndromes) [4].
DL-Lysine- 13C6 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6 hydrochloride) is 13C-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
L-Glutamine- 15N2 is the 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
N,N-Di-(beta-carboethoxyethyl)methylamine-d8 (Di-Beta-carbethoxyethyl-methylamine-d8) is the deuterium labeled N,N-Di-(beta-carboethoxyethyl)methylamine (HY-76097).
Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
ATP- 15N5 (Adenosine 5'-triphosphate- 15N5) dilithium is 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Moxifloxacin- 13C,d3 hydrochloride (BAY 12-8039- 13C,d3) is 13C and deuterated labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
Tempol-d17, 15N is the deuterium labeled Tempol . Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS) .
D-Glutamic acid- 13C5 ((R)-Glutamic acid- 13C5) is 13C labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
Deoxythymidine-5'-triphosphate- 13C10 (dTTP- 13C10) dilithium is 13C-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
(Rac)-Folic acid- 13C5, 15N is the 13C-labeled and 15N-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
L-Glutathione reduced- 13C2, 15N is the 13C- and 15N-labeled L-Glutathione reduced. L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
dGTP- 13C10 (2'-Deoxyguanosine-5'-triphosphate- 13C10) dilithium is 13C-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
D-(+)-Glucono-1,5-lactone- 13C6 (Gluconic acid lactone- 13C6) is the 13C-labeled D-(+)-Glucono-1,5-lactone (HY-I0301). D-(+)-Glucono-1,5-lactone is a polyhydroxy (PHA) that is capable of metal chelating, moisturizing and antioxidant activity.
L-Gulono-1,4-lactone- 13C6 (L-Gulonolactone- 13C6) is the 13C-labeled L-Gulono-1,4-lactone (HY-W016628). L-Gulono-1,4-lactone is a substrate of L-gulono-1,4-lactone oxidoreductase, which catalyzes the last step of the biosynthesis of L-ascorbic (Vatamin) C. In other words, L-Gulono-1,4-lactone is a direct precursor of vitamin C in animals, in plants and in some protists.
2-Naphthoic acid- 13C6 (Naphthalene-2-carboxylic acid- 13C6) is the 13C-labeled 2-Naphthoic acid (HY-W007437). 2-Naphthoic acid is an organic compound commonly used as a raw material for dyes and the production of other chemicals. It can form dyes with other organic substances and is widely used in textile, printing and manufacturing fields. In addition, the compound is also used as a photosensitive material and a lubricant.
3-?Bromo-?L-?tyrosine- 13C6 (3-Bromo-Tyr- 13C6) is a 13C-labeled 3-?Bromo-?L-?tyrosine (HY-W018386). 3- Bromo- L- tyrosine (3-Bromo-Tyr) is a tyrosine derivative .
11-Beta-hydroxyandrostenedione-d7 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor
Lamotrigine- 13C (LTG- 13C) is 13C labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
4-Octyl itaconate- 13C5-1 is 13C-labeled 4-Octyl itaconate (HY-112675). Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
N4-Acetylsulfamethazine- 13C6 (Sulfamethazine-n4-acetyl- 13C6) is the 13C-labeled N4-Acetylsulfamethazine (HY-W290839). N4-Acetylsulfamethazine is a metabolite of Sulfamethazine (HY-B0035). Sulfamethazine is one of the most frequently used sulfonamides in the poultry farming industry .
2'-Deoxyadenosine-5'-triphosphate- 13C10 (dATP- 13C10) dilithium is 13C-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
DMT-dA(bz) Phosphoramidite- 15N5 is the 15N labeled DMT-dA(bz) Phosphoramidite . DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA .
Lysophosphatidylcholine 18:2-d9 is deuterium labeled Lysophosphatidylcholine 18:2. Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary
Topiramate- 13C (McN 4853- 13C) is 13C labeled Topiramate. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
Dehydro Nifedipine-13C,d3 is a deuterated labeled Dehydro Nifedipine . Dehydro nifedipine (BAY-b 4759) is a metabolite of Nifedipine (HY-B0284). Nifedipine (BAY-a-1040) is a potent calcium channel blocker and an agent of choice for cardiac insufficiencies .
(Rac)-Nebivolol-d2, 15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
Ethyl 3,4-Dihydroxybenzoate- 13C3 (Protocatechuic acid ethyl ester- 13C3) is the 13C-labeled Ethyl 3,4-dihydroxybenzoate (HY-W016409). Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema [4].
5-(Hydroxymethyl)-1-phenylpyridin-2(1H)-one-d5 (Pirfenidone Impurity 6-d5) is the deuterium labeled 5-(Hydroxymethyl)-1-phenylpyridin-2(1H)-one (HY-W349458).
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase .
PhIP-d3(2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine-d3) is the deuterium labeled PhIP (HY-118716). PhIP (2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine) is the most abundant of generation of heterocyclic amines (HCA), resulted in the cooking of meat . DNA damaging and mutagenic activities. PhIP also has oestrogenic activity that could contribute to its tissue specific carcinogenicity .
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
9(S)-HODE- 13C18 ((+)-α-Dimophecolic acid- 13C18) is 13C labeled 9S-HODE. 9S-HODE (Alpha-dimorphecolic acid) is an octadecadienoic acid and the main active derivative of linoleic acid, which can reduce the viability of HL-60 cells and induce apoptosis. 9S-HODE is rich in lipid peroxidation (LPO) products and is almost an ideal marker for LPO .
3-Hydroxybutyric acid- 13C2 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids .
2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development .
Oleoyl coenzyme A- 13C18 (lithium) is the 13C labeled Oleoyl Coenzyme A lithium . Oleoyl coenzyme A (Oleoyl-CoA) is a thioester of oleic acid and coenzyme A. Oleoyl coenzyme A has a role as an Escherichia coli metabolite and a mouse metabolite .
Acetyl coenzyme A- 13C2 lithium is the 13C-labeled Acetyl coenzyme A (HY-114293). Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ethyl maltol-d5 is the deuterium labeled Ethyl maltol. Ethyl maltol (2-Ethyl-3-hydroxy-4H-pyran-4-one) is an orally active and important food additive and flavor enhancer. Ethyl maltol is less toxic to rats and dogs. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells .
Levomefolic acid- 13C,d3 is the deuterium labeled Levomefolic acid (HY-14781) . Levomefolic acid (5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .
3,5,6-Trichloro-2-pyridinol- 13C3 (TCPy- 13C3) is the 13C-labeled 3,5,6-Trichloro-2-pyridinol (HY-W018171). 3,5,6-Trichloro-2-pyridinol (TCPy) is the main degradation product of the herbicide Triclopyr and the insecticides Chlorpyrifos and Chlorpyrifos-methyl .
2-Ketoglutaric acid- 13C2 (Alpha-Ketoglutaric acid- 13C2) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
Varenicline- 13C 15N (CP 526555- 13C 15N) is 13C and 15N labeled Varenicline. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation [4] .
(1S,2R)-Tranylcypromine-d5 (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride . Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression [4].
2'-Deoxyadenosine-5'-triphosphate- 15N5 (dATP- 15N5) dilithium is 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Dibenzo[a,c]anthracene- 13C6 (2,3-Benzotriphenylene- 13C6) is 13C labeled Benzo[f]tetraphene. Benzo[f]tetraphene (Dibenz[a,c]anthracene) is a polycyclic aromatic hydrocarbon with significant antitumor activity. Benzo[f]tetraphene is used as a luminescent probe in cell biology research and can effectively detect reactive oxygen species in biological systems. Benzo[f]tetraphene can also be used as a potential photosensitizer and shows good application prospects in photodynamic inhibition.
(S)-Velpatasvir- 13C,d3 ((S)-GS-5816- 13C,d3) is 13C labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM .
Prostaglandin E2-1-glyceryl ester-d5 (PGE2-1-glyceyl ester-d5) is deuterium labeled Prostaglandin E2-1-glyceryl ester. Prostaglandin E2-1-glyceryl ester, a Prostaglandin Glycerol Ester, is an endocannabinoid ligand for the CB1 receptor. Prostaglandin E2-1-glyceryl ester induces rapid, transient elevation of intracellular free Ca 2+ .
2-Ketoglutaric acid- 13C5 (Alpha-Ketoglutaric acid- 13C5) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
1,2-Dioctanoyl-3-chloropropanediol-d5 is deuterium labeled 1,2-Dioctanoyl-3-chloropropanediol. 1,2-Dioctanoyl-3-chloropropanediol (3-Chloropropane-1,2-diyl dioctanoate) is an ester product .
L-2-Hydroxyglutaric acid-d5 disodium ((2S)-2-Hydroxyglutaric acid-d5 disodium) is the deuterium labeled L-2-Hydroxyglutaric acid disodium (HY-W015114). L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation . L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively .
VD3-d6 (Vitamin D3-26,26,26,27,27,27-d6) is deuterated VD3. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action [4].
2-Amino-6-hydroxypyrimidin-4(1H)-one- 13C2 (2-Amino-6-hydroxy-1H-pyrimidin-4-one- 13C2) is the 13C-labeled 2-Amino-6-hydroxypyrimidin-4(1H)-one (HY-Y0559).
1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE-d11 (15(S)-HETE-SAPE-d11) is deuterium labeled 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE. 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 (HY-N6687) by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE (SAPE) by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes .
1-beta-D-Arabinofuranosyluracil- 13C, 15N2 (1-b-D-Arabinofuranosyluracil- 13C, 15N2; Uracil 1-β-D-arabinofuranoside- 13C, 15N2) is the 13C- and 15N-labeled labeled 1-beta-D-Arabinofuranosyluracil (HY-N6652). 1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties . 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells .
2-Chloro-5-methylpyrimidin-4-amine- 15N2, 13C (4-Amino-2-chloro-5-methylpyrimidine- 15N2, 13C) is the 13C- and 15N-labeled 2-Chloro-5-methylpyrimidin-4-amine (HY-W002966).
L-Arginine-1,2- 13C2 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
L-Valine-d8 is a deuterated form of L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Cefazolin- 13C2, 15N (Cephazolin- 13C2, 15N) is 13C and 15N labeled Cefazolin. Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
Gimeracil- 13C3, 15N (Gimestat- 13C3, 15N) is 13C and 15N labeled Gimeracil. Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD) .
L-Lactic acid-2- 13C1 is the 13C-labeled L-Lactic acid (HY-Y0479). L-Lactic acid is a buildiing block which can be used as a precursor for the production of the bioplastic polymer poly-lactic acid .
Emtricitabine- 13C, 15N2 (BW1592- 13C, 15N2) is a 13C- and 15N-labeled Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Uridine 5'-monophosphate- 15N2 (5'- Uridylic acid- 15N2) dilithium is 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
rU Phosphoramidite- 13C9 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9) is 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
1-Palmitoyl-sn-glycero-3-phosphocholine-d9-1 (16:0 Lyso PC-d9-1) is deuterium labeled 1-Palmitoyl-sn-glycero-3-phosphocholine (HY-125783). 1-Palmitoyl-sn-glycero-3-phosphocholine (16:0 Lyso PC) is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis [4].
Phenyl-boronic acid-d5 (Boronic acid,B-(phenyl-2,3,4,5,6)-d5) is the deuterium labeled Phenylboronic acid (HY-W001090). Phenylboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Nitrofurazone- 13C, 15N2 (Nitrofural- 13C, 15N2) is the 13C and 15N labled Nitrofurazone (HY-B0226) . Nitrofurazone is a potential antibiotic that can be used topically to treat wounds, burns, ulcers and skin infections to combat various microorganisms and to prepare surfactants . Nitrofurazone may affect the ecosystem function in Marine environment and affect the functional processes of epiphytic fauna .
[1,1'-Biphenyl]-3-amine-13C6 hydrochloride (Biphenyl-3-amine-13C6 hydrochloride) is the 13C labeled isotope of [1,1'-Biphenyl]-3-amine hydrochloride (HY-W106014) .
N-Acetyl-D-glucosamine-d3 (N-Acetyl-2-amino-2-deoxy-D-glucose-d3) is deuterium labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose), the D isomer of N-acetylglucosamine, is an orally active monosaccharide derivative of glucose with anti-tumor and anti-inflammation properties. N-Acetyl-D-Glucosamine is also a bacterial metabolite, which is found in Escherichia coli. N-Acetyl-D-Glucosamine can induce yeast-mycelial conversion in Candida albicans. N-Acetyl-D-Glucosamine also enhances healing of cartilaginous injuries in rabbits .
Uridine 5′-diphosphoglucose- 13C6 (UDP-D-Glucose- 13C6) disodium is the 13C labeled Uridine 5′-diphosphoglucose disodium (HY-N7032) . Uridine 5’-diphosphoglucose (UDP-glucose) disodium, secreted by cardiomyocytes during ischemia and reperfu, is a potent agonist of the proinflammatory P2Y14 receptor. It acts an important role in the regulation of inflammation and neutrophil polarization in neutrophils. Uridine 5’-diphosphoglucose disodium is also the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine 5’-diphosphoglucose disodium is promising for research in counteracting myocardial infarction/reperfusion (MIR)-induced inflammation in the heart tissue [4] .
L-Alanine- 13C,d is the 13C- and deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N,N'-Dimethyl-3,3'-dithiodipropionamide-d6 (Propanamide, 3,3'-dithiobis[n-methyl-d6) is the deuterium labeled N,N'-Dimethyl-3,3'-Dithiodipropionamide (HY-W045680).
2,6-Dichlorodiphenylamine- 13C6 (2,6-Dichloro-N-phenylaniline- 13C6) is the 13C-labeled 2,6-Dichlorodiphenylamine (HY-W012126). 2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a?COX?inhibitor, with?IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
2-Amino-2-deoxyglucose hydrochloride- 13C6 (D-Glucosamine Hydrochloride- 13C6) is the 13C-labeled 2-Amino-2-deoxyglucose hydrochloride (HY-N9459). 2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc .
Mannosan,95%- 13C6 (1,6-Anhydro-β-D-mannopyranose- 13C6) is the 13C-labeled Mannosan,95% (HY-124095). Mannosan,95% (1,6-Anhydro-β-D-mannopyranose,95%) is a class of biochemical reagents used in glycobiology research. Glycobiology studies the structure, synthesis, biology, and evolution of sugars. It involves carbohydrate chemistry, enzymology of glycan formation and degradation, protein-glycan recognition, and the role of glycans in biological systems. This field is closely related to basic research, biomedicine, and biotechnology .
5'-Deoxy-5-fluorocytidine-13C5 is the 13C labeled isotope of 5'-Deoxy-5-fluorocytidine (HY-W009538). 5'-Deoxy-5-fluorocytidine (5-Fluoro-5'-deoxycytidine) is a cytidine analog and metabolite of Capecitabine (HY-B0016). 5'-Deoxy-5-fluorocytidine is converted from Capecitabine by carboxylesterase in the liver. 5'-Deoxy-5-fluorocytidine is deaminated by cytidine deaminase to generate 5'-deoxy-5-fluorouridine, which is finally converted into 5-fluorouracil (HY-90006) by thymidine phosphorylase in tumor tissues to exert anti-tumor effects. 5'-Deoxy-5-fluorocytidine is used in the researches for solid tumors such as colorectal cancer, non-small cell lung cancer and breast cancer [4].
1,5-Anhydrosorbitol- 13C6 (1,5-Anhydro-D-glucitol- 13C6) is the 13C-labeled 1,5-Anhydrosorbitol (HY-113075). 1,5-Anhydrosorbitol is a short-term marker for glycemic control.
L-Phenylalanine- 13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
L-Phenylalanine- 13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
(3S,5R)-Fluvastatin-d6 (sodium)?is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
rU Phosphoramidite- 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 15N2) is 15N labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
trans-2,cis-6-Nonadienal- 13C2 is 13C labeled trans-2,cis-6-Nonadienal (HY-W127515). Trans-2, cis-6-NonadienalIt is an organic compound belonging to aldehydes. It has a strong, pungent smell and is commonly found in a variety of foods, including fruits and vegetables. Trans-2, cis-6-NonadienalIt has a variety of applications in the flavor and fragrance industry, especially as a fragrance agent in products such as perfume, cologne and air fresheners. In addition, it can also be used as an intermediate in the synthesis of various chemicals and drugs.
Uridine 5'-monophosphate- 13C9 (5'- Uridylic acid- 13C9) dilithium is 13C-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea .
(E)-3-Methyl-2-hexenoic acid-d5 ((2E)-3-Methyl-2-hexenoic acid-d5) is a deuterium labeled (E)-3-Methyl-2-hexenoic acid. (E)-3-Methyl-2-hexenoic acid is an axillary odor-related compound .
2-Thiouracil- 13C, 15N2 is the 13C, 15N labeled 2-Thiouracil. 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
(E)-3,4-Dimethoxycinnamic acid- 13C3 ((E)-O-Methylferulic acid- 13C3) is the 13C-labeled (E)-3,4-Dimethoxycinnamic acid (HY-N1778A). (E)-3,4-Dimethoxycinnamic acid is the less active isomer of 3,4-Dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway . Anti-apoptotic effects .
DL-Phenylmercapturic Acid- 13C6 (N-Acetyl-S-phenyl-L-cysteine- 13C6) is the 13C-labeled DL-Phenylmercapturic Acid (HY-W141770). DL-Phenylmercapturic Acid is a cysteine derivative .
Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Ethyl linoleate-d5 (Linoleic Acid ethyl ester-d5) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators . .
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole . Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC- 13C16 (POPC- 13C16) is 13C labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for the preparation of liposomes and studying the properties of lipid bilayers .
Urea- 13C, 15N2 is the 13C and 15N labeled Urea . Urea is a powerful protein denaturant via both direct and indirect mechanisms . A potent emollient and keratolytic agent . Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function . Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Fluconazole-13C2,15N (UK-49858-13C2,15N) is the 13C and 15N labeled isotope of Fluconazole (HY-B0101). Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL .
1,2-Dilauroyl-3-chloropropanediol-d5 (1,1′-[1-(Chloromethyl)-1,2-ethanediyl] didodecanoate-d5) is the deuterium labeled 1,2-Dilauroyl-3-chloropropanediol (HY-W587507). 1,2-Dilauroyl-3-chloropropanediol (1,1′-[1-(Chloromethyl)-1,2-ethanediyl] didodecanoate) is an ester product.
3,3'-Diiodo-L-thyronine- 13C6 is the 13C labeled 3,3'-Diiodo-L-thyronine . 3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity .
Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled Gemcitabine hydrochloride . Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis .
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway .
Zidovudine O-β-D-glucuronide-d3 (sodium) (3'-Azido-3'-deoxythymidine β-D-glucuronide-d3 (sodium)) is a deuterium labeled Zidovudine O-β-D-glucuronide (sodium) (HY-137522). Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection .
L-Lactic acid- 13C3 ((S)-2-hydroxypropanoic- 13C3) sodium (20% in water) is the 13C labeled L-Lactic acid. L-Lactic acid- 13C3 sodium (20% in water) can be used for lactate metabolism research .
Captopril- 13C5, 15N (SQ 14225- 13C5, 15N) is 13C and 15N labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM .
1-(4,4-Dimethylthiochroman-6-yl)ethanone-d8(6-Acetyl-4,4-dimethylthio-chroman-d8) is the deuterium labeled 1-(4,4-Dimethylthiochroman-6-yl)ethanone (HY-I0187).
Laninamivir- 13C, 15N2 (R 125489- 13C, 15N2) is 13C and 15N labeled Laninamivir. Laninamivir (R 125489) is a potent influenza neuraminidase (NA) inhibitor with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively .
1-Oleoyl-2-linoleoyl-rac-glycerol-d5 (DG(18:1/0:0/18:2)-d5) is the deuterium labeled 1-Oleoyl-2-linoleoyl-rac-glycerol (HY-W777107). 1-Oleoyl-2-linoleoyl-rac-glycerol (DG(18:1/0:0/18:2)) is a diacylglycerol, which is composed of a linoleic acid and an oleic acid. 1-Oleoyl-2-linoleoyl-rac-glycerol can be found in dry-cured ham, and acts as the food additive .
Lisinopril- 13C5, 15N (MK-521- 13C5, 15N) is 13C and 15N labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
Pomalidomide- 15N, 13C5 is 15N and 13C labeled Pomalidomide (HY-10984). Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Lamivudine- 13C, 15N3 (BCH-189- 13C, 15N3) is 13C and 15N labeled Lamivudine. Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
((2R,3S,4R,5R)-5-(4-Amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate- 13C9, 15N3 (sodium) is the 13C and 15N labeled Sodium ((2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate .
PSI-6206-d1, 13C, 15N2 is 15N and 13C labeled PSI-6206 (HY-15236). PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Nonanoic acid-d2 is the deuterium labeled Nonanoic acid . Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2 .
L-Glutamine-1,2- 13C2 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
(9S,13R)-12-OPDA-d5 ((9S,13R)-12-OPDA-d5) is an isotopic label of (9S,13R)-12-oxyphytodienoic acid. (9S,13R)-12-Oxophytodienoic acid is an isomer of 12-oxoPDA (HY-118828). (9S,13R)-12-Oxo phytodienoic Acid is a lipoxygenase metabolite in green plant leaves .
1-(4-Chlorophenyl)-2-methylpropan-2-ol-d6(1-(4-Chlorophenyl)-2-methyl-2-propanol-d6) is the deuterium labeled 1-(4-Chlorophenyl)-2-methylpropan-2-ol (HY-W101971).
L-Ascorbic acid- 13C6-1 (L-Ascorbate-1; Vitamin C- 13C6-1) is a 13C labeled L-Ascorbic acid (HY-B0166) . L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor [4]. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells .
Zidovudine Glucuronide- 13C6 (3'-Azido-3'-deoxythymidine β-D-glucuronide- 13C6) is 13C labeled Zidovudine O-β-D-glucuronide. Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection .
LacCer (d18:1/16:0)-d3 (C16 Lactosylceramide (d18:1/16:0)-d3) is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
5-Fluorouracil- 13C, 15N2 is the 13C and 15N labeled 5-Fluorouracil . 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer . 5-Fluorouracil also inhibits HIV [4].
2-Amino-2-deoxyglucose hydrochloride- 13C2 (D-Glucosamine Hydrochloride-1,2- 13C2) is the 13C-labeled 2-Amino-2-deoxyglucose hydrochloride (HY-N9459). 2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc .
N-Phthaloylglycine- 13C2, 15N (Phthaloyl glycine- 13C2, 15N) is the 13C- and 15N-labeled N-Phthaloylglycine (HY-W014665). N-Phthaloylglycine (Phthaloyl glycine) is an FX-type hapten that attaches to free amine groups of proteins .
1-(Adamantan-1-yl)ethan-1-one-d3 (N-Benzyl-3-carboethoxy-4-piperidone hydrochloride-d3) is the deuterium labeled 1-(Adamantan-1-yl)ethan-1-one (HY-W067624).
Diacetone-β-D-fructose-d12(2,3:4,5-Di-O-isopropylidene-β-D-fructopyranose-d12) is the deuterium labeled Diacetone-β-D-fructose (HY-W011792). Diacetone-β-D-fructose is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
Homovanillic acid- 13C6, 18O (Vanilacetic acid- 13C6, 18O) is the 13C- and 18O-labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency .
L-Valine- 13C5, 15N ((S)-Valine- 13C5, 15) is the 13C- and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
(S)-2-Hydroxy-3-phenylpropanoic acid- 13C9 (L-(-)-3-Phenyllactic Acid- 13C9) is the 13C-labeled (S)-2-Hydroxy-3-phenylpropanoic acid (HY-30220). (S)-2-Hydroxy-3-phenylpropanoic acid is the L-configuration of 2-Hydroxy-3-phenylpropanoic acid, and its level is closely related to some diseases, such as phenylketonuria .
Octreotide- 13C9, 15N (SMS 201-995- 13C9, 15N) is 13C and 15N labeled Octreotide. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
Taurine- 13C2, 15N is the 13C- and 15N- labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes .
Dihydrouracil- 13C, 15N2 (5,6-Dihydrouracil- 13C, 15N2) is the 13C- and 15N-labeled Dihydrouracil (HY-W012926). Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient .
2-(4-Bromophenoxy)-N,N-dimethylethanamine-d6 (2-(N,N-Dimethylamino)ethyl 4-bromophenyl ether-d6) is the deuterium labeled 2-(4-Bromophenoxy)-N,N-dimethylethanamine (HY-W013927).
Oxypurinol- 13C, 15N2-1 (Oxipurinol- 13C, 15N2-1) is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol, the major active metabolite of Allopurinoll (HY-B0219), is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
Betrixaban-d4(PRT054021-d4) is deuterium labeled Betrixaban. Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
Floxuridine- 13C, 15N2 (5-Fluorouracil 2'-deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled Floxuridine (HY-B0097). Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
Benzyl alcohol-α- 13C-α,α-d2 is the 13C-labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
N-Cyclohexyl-1,3-benzothiazol-2-amine- 13C6 (N-Cyclohexylbenzothiazole-2-amine- 13C6) is the 13C-labeled N-Cyclohexyl-1,3-benzothiazol-2-amine (HY-W200757).
1-Methyl-5-(3-pyridinyl)-2-pyrrolidinone- 13C,d3 (rac-Cotinine- 13C,d3) is the deuterium and 13C-labeled 1-Methyl-5-(3-pyridinyl)-2-pyrrolidinone (HY-W588192).
6-Amino-3-methylpyrimidine-2,4(1H,3H)-dione-d3 (6-Amino-3-methyluracil-d3) is the deuterium labeled 6-Amino-3-methylpyrimidine-2,4(1H,3H)-dione (HY-W038777).
H-N-Me-Ala-OH- 13C,d3 (N-Methyl-L-alanine- 13C,d3) is the deuterium and 13C labeled H-N-Me-Ala-OH (HY-W015926). H-N-Me-Ala-OH is an alanine derivative .
5,6-Diaminopyrimidine-2,4-diol hydrochloride- 13C3 (5,6-Diaminouracil hydrochloride- 13C3) is the 13C-labeled5,6-Diaminopyrimidine-2,4-diol (HY-W002107).
Fmoc-Gly-OH- 13C2, 15N (Fmoc glycine- 13C2, 15N) is a 15N-labeled and 13C-labled Fmoc-Gly-OH (HY-Y1250). Fmoc-Gly-OH (Fmoc glycine) is a Fmoc-protected glycine derivative, can be used for the synthesis of compounds .
Diethyl itaconate,98% (stabilized with TBC)- 13C5 (Itaconic Acid Diethyl Ester (stabilized with TBC)- 13C5) is the 13C-labeled Diethyl itaconate,98% (stabilized with TBC) (HY-W143131).
N-Ethyl-3,4-(methylenedioxy)aniline-d5 (N-Ethyl-3H-1,2-benzodioxol-6-amine-d5) is the deuterium labeled N-Ethylbenzo[d][1,3]dioxol-5-amine (HY-W015360).
2-Bromo-3'-methoxyacetophenone- 13C,d3 (α-Bromo-3'-methoxyacetophenone- 13C,d3) is the deuterium and 13C labeled 2-Bromo-3'-methoxyacetophenone (HY-W004800).
(R)-4-Benzyl-3-propionyloxazolidin-2-one-d3(N-3-propionyl-(4R)-benzyl-2-oxazolidinone-d3) is the deuterium labeled (R)-4-Benzyl-3-propionyloxazolidin-2-one (HY-W008773).
Meldrum's acid- 13C3 (2,2-Dimethyl-1,3-dioxane-4,6-dione- 13C3) is the 13C-labeled Meldrum's acid (HY-Y0232). Meldrum's acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Regorafenib N-oxide and N-desmethyl (M5)-d3-1 (N-Desmethyl regorafenib N-oxide-d3-1) is the deuterium labeled Regorafenib N-oxide and N-desmethyl (M5) (HY-108226). Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4 .
5-Bromo-2,4-di-tert-butoxypyrimidine- 13C, 15N2 (IFLAB-BB F1371-0151- 13C, 15N2) is the 13C- and 15N-labeled 5-Bromo-2,4-di-tert-butoxypyrimidine (HY-W128969).
5-Methyl cytosine- 13C, 15N2 hydrochloride (5-Methylcytosine hydrochloride- 13C, 15N2) is the 13C- and 15N-labeled 5-Methylcytosine hydrochloride (HY-W008091A). 5-Methylcytosine hydrochloride plays a crucial role in regulating gene expression, facilitating genomic imprinting, and suppressing transposable elements, while also being intricately linked to translational fidelity and tRNA recognition.
L-Alanine- 13C2, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Acetobromo-a-D-glucuronic acid- 13C6 methyl ester (Methyl acetobromo-α-D-glucuronate- 13C6 methyl ester) is 13C labeled Acetobromo-α-D-glucuronic acid methyl ester, 98% (HY-W008125). Acetobromo-α-D-glucuronic acid methyl ester, 98% is an intermediate. Acetobromo-α-D-glucuronic acid methyl ester, 98% can be used to synthesize HMR1098-S-Glucuronide Methyl Ester. HMR1098 is a novel KATP blocker that is metabolized to S-glucuronide in rat and dog bile. Acetobromo-α-D-glucuronic acid methyl ester, 98% can be used in the research of sudden cardiac death .
3-Hydroxykynurenine- 13C3, 15N (3-Hydroxy-DL-kynurenine- 13C3, 15N) is the 13C and 15N labeled 3-Hydroxykynurenine (HY-113294) . 3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis .
(S)-4-Benzyl-3-propionyloxazolidin-2-one-d3 (2-Oxazolidinone, 3-(1-oxopropyl)-4-(phenylmethyl)-, (4S)-d3) is the deuterium labeled (S)-4-Benzyl-3-propionyloxazolidin-2-one (HY-W008304).
L-Alanine- 13C3, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N-Acetyl-D-glucosamine- 13C6 (N-Acetyl-2-amino-2-deoxy-D-glucose- 13C6) is the 13C labled N-Acetyl-D-glucosamine (HY-A0132) . N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of glucose.
Quinolinic acid- 13C3, 15N (2,3-Pyridinedicarboxylic Acid- 13C3, 15N) is the 13C- and 15N-labeled Quinolinic acid (HY-100807). Quinolinic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway and thereby has the potential of mediating N-methyl-D-aspartate neuronal damage and dysfunction .
3,4-Dihydronaphthalen-1-one- 13C6 (3,4-Dihydro-1(2H)-naphthalenon- 13C6) is the 13C-labeled 3,4-Dihydronaphthalen-1(2H)-one (HY-76194). 3,4-Dihydronaphthalen-1(2H)-one is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
D-Glutamic acid- 13C5, 15N ((R)-Glutamic acid- 13C5, 15N) is 13C and 15N labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
N2,9-Diacetylguanine- 13C2, 15N (N-(9-Acetyl-6,9-dihydro-6-oxo-1H-purin-2-yl)acetamide- 13C2, 15N) is the 13C- and 15N-labeled N2,N9-Diacetylguanine (HY-41619).
N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine-d3 (Methyl N-acetyl-S-(3-hydroxypropyl)-L-cysteinate-d3) is the deuterium labeled N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine.
D-Mannosamine-d2(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal-d2) hydrochloride is a deuterium labeled D-Mannosamine hydrochloride (HY-W021425). D-Mannosamine ((2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal) hydrochloride is a six-carbon amino sugar and an amino derivative of D-mannose. D-Mannosamine hydrochloride can block mannose receptors.
Dinoprost- 13C5 is 13C labeled Dinoprost (HY-12956). Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
Exendin-4 (Leu- 13C6, 15N) (Exenatide (Leu- 13C6, 15N)) TFA is the 13C- and 15N-labeled Exendin-4 TFA (HY-13443). Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM .
γ-Glu-(Phe- 13C9, 15N) is the 13C and 15N labeled isotope of γ-Glu-Phe(HY-101399).γ-Glu-Phe or the postenzymatic reaction mixture enhanced the umami intensity of commercial soy sauce and model chicken soup.
Cyclic GMP- 13C, 15N2 is 13C and 15N labeled Cyclic GMP (HY-113469). Cyclic GMP (cGMP), an important second messenger, is a major intracellular mediator of extracellular signals such as nitric oxide (NO) and natriuretic peptides (NPs). Effects of Cyclic GMP occur through three main groups of cellular targets: cGMP-dependent protein kinases (PKGs), cGMP-gated cation channels, and PDEs. Cyclic GMP can inhibit both platelet adhesion and aggregation. cGAMP (Cyclic-GMP-AMP) (HY-12512), a conjugate of Cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses [4].
L-Phenylalanine- 13C9, 15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals [4].
2-Chloropropane-1,3-diyl dioleate-d5 (1,1′-(2-Chloro-1,3-propanediyl) di-(9Z)-9-octadecenoate-d5) is the deuterium labeled 2-Chloropropane-1,3-diyl dioleate (HY-W705777). 2-Chloropropane-1,3-diyl dioleate (1,1′-(2-Chloro-1,3-propanediyl) di-(9Z)-9-octadecenoate) is an ester product.
1-(3,4-Dimethylphenyl)ethan-1-ol- 13C,d3 (1-(3,4-Dimethylphenyl)ethanol- 13C,d3) is the deuterium labeled and 13C-labeled 1-(3,4-Dimethylphenyl)ethan-1-ol (HY-W340128).
4-Amino-TEMPO-d17,15N (4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl-d17,15N) is the deuterium labeled 4-Amino-TEMPO-d17 (HY-W002004S1). 4-Amino-TEMPO (4-Amino-2,2,6,6-tetramethylpiperidine-1-oxyl) is a stable nitroxide radical and N-nucleophile based on TEMPO. 4-Amino-TEMPO has superoxide dismutase-mimetic activity, can protect cells from oxidative damage, and has radioprotective effects. 4-Amino-TEMPO is widely used in fields such as biomedicine, materials science, and industrial production. 4-Amino-TEMPO can be used as a spin label to detect free radicals, an oxidation catalyst in industrial production, and an antioxidant stabilizer for polymers, among others .
5'-Hydroxyphenyl carvedilol-d5(3-(2-((3-((9H-carbazol-4-yl)oxy)-2-hydroxypropyl)amino)ethoxy)-4-methoxyphenol-d5) is the deuterium labeled 3-(2-((3-((9H-carbazol-4-yl)oxy)-2-hydroxypropyl)amino)ethoxy)-4-methoxyphenol (HY-W334664).
8-Hydroxy-2'-deoxyguanosine- 13C, 15N2 is 13C and 15N labeled 8-Hydroxy-2'-deoxyguanosine. 8-Hydroxy-2'-deoxyguanosine is a critical biomarker of oxidative stress and carcinogenesis .
Ile-(Leu-13C6,15N)-OH (TFA) is 13C- and 15N-labeled L-Isoleucyl-L-leucine (HY-W269700). L-Isoleucyl-L-leucine has a role as a metabolite and can be used to inhibit movement-induced muscle damage and muscle defective condition.
(S)-2-Amino-3-(4-nitrophenyl)propan-1-ol-d6((2S)-2-Amino-3-(4-nitrophenyl)-1-propanol-d6) is the deuterium labeled (S)-2-amino-3-(4-nitrophenyl)propan-1-ol (HY-W270163).
Diacetone-β-D-fructose- 13C6 (2,3:4,5-Di-O-isopropylidene-β-D-fructopyranose- 13C6) is the 13C-labeled Diacetone-β-D-fructose (HY-W011792). Diacetone-β-D-fructose is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
(Leu-13C6,15N)-Ile-OH (L-Leucyl-13C6,15N-L-isoleucine) TFA is the deuterium labeled Leu-Ile-OH. Leu-Ile-OH protects against neuronal death by inducing brain-derived neurotrophic factor (BDNF) and glial cell line-derived neurotrophic factor (GDNF) synthesis .
1,3-Dipalmitin-d6 (Glyceryl 1,3-dipalmitate-d6) is deuterium labeled 1,3-Dipalmitin. 1,3-Dipalmitin (1,3-Dipalmitoylglycerol) is a cerebroside that can be found in Typhonium giganteum Engl .
(3S,6S)-3,6-Dimethyl-1,4-dioxane-2,5-dione- 13C2 (L-Lactide- 13C2) is the 13C-labeled L-Lactide (HY-W020691A). (3S,6S)-3,6-Dimethyl-1,4-dioxane-2,5-dione is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Uridine diphosphate glucuronic acid- 13C, 15N2 (UDP-α-D-glucuronic acid- 13C, 15N2) is the 13C- and 15N-labeled Uridine diphosphate glucuronic acid (HY-125954). Uridine diphosphate glucuronic acid (UDP-α-D-glucuronic acid) is a cofactor that is formed by the catalytic activity of UDP-glucose dehydrogenase. Uridine diphosphate glucuronic acid is a central precursor in sugar nucleotide biosynthesis and common substrate for C4-epimerases and decarboxylases releasing UDP-galacturonic acid (UDP-GalA) and UDP-pentose products, respectively. Uridine diphosphate glucuronic acid as a glucuronic acid donor, can be used for for the research of the conjugation of bilirubin in the endoplasmic recticulum .
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
3a,4,7,7a-Tetrahydro-1H-isoindole-1,3(2H)-dione-d6 (1,2,3,6-Tetrahydrophthalimide-d6) is the deuterium labeled 3a,4,7,7a-Tetrahydro-1H-isoindole-1,3(2H)-dione (HY-W068988).
3',5'-Di-O-benzyl Entecavir- 13C2, 15N (The intermediate of Entecavir hydrate- 13C2, 15N) is the 13C- and 15N-labeled 2-Amino-9-((1S,3R,4S)-4-(benzyloxy)-3-((benzyloxy)methyl)-2-methylenecyclopentyl)-1H-purin-6(9H)-one (HY-W105415).
2,4-Dichloro-5-methylpyrimidine- 15N2, 13C (Pyrimidine, 2,4-dichloro-5-methyl- 15N2, 13C) is the 13C- and 15N-labeled 2,4-Dichloro-5-methylpyrimidine (HY-W002132).
Eicosapentaenoic acid 1,2,3,4,5- 13C5 (EPA 1,2,3,4,5- 13C, FA 20:5- 13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation [4].
N-Acetyl-D-glucosamine- 13C3, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc .
N-Acetyl-D-glucosamine- 13C8, 15N is 13C and 15N labeled N-Acetyl-D-glucosamine (HY-A0132). N-Acetyl-D-glucosamine is a monosaccharide derivative of glucose.
N-Acetyl-D-glucosamine- 13C2, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc .
2-(5-tert-Butyl-2-hydroxyphenyl)benzotriazole-d9(2-(2H-Benzo[d][1,2,3]triazol-2-yl)-4-(tert-butyl)phenol-d9) is the deuterium labeled 2-(2H-Benzo[d][1,2,3]triazol-2-yl)-4-(tert-butyl)phenol (HY-W440436).
Citrinin- 13C13 (NSC 186- 13C13) is the 13C labeled Citrinin (HY-N6746). Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity [4] .
N2-Acetyl-O6-diphenylcarbamoylguanine- 13C2, 15N (2-Acetamido-9H-purin-6-yl diphenylcarbamate- 13C2, 15N) is the 13C- and 15N-labeled 2-Acetamido-9H-purin-6-yl diphenylcarbamate (HY-W143802).
2,5,6-Triaminopyrimidin-4(3H)-one- 13C2, 15N (6-Hydroxy-2,4,5-triaminopyrimidine- 13C2, 15N) is the 13C- and 15N-labeled 2,5,6-Triaminopyrimidin-4(3H)-one (HY-W018560).
N-Boc-S-Bzl-L-Cys-Gly-OBzl- 13C2, 15N (Benzyl S-benzyl-N-(tert-butoxycarbonyl)-L-cysteinylglycinate- 13C2, 15N) is the 13C- and 15N-labeled Benzyl S-benzyl-N-(tert-butoxycarbonyl)-L-cysteinylglycinate (HY-W699579).
1,2-Dioleoyl-3-lauroyl-rac-glycerol- 13C3 is the 13C-labeled 1,2-Dioleoyl-3-lauroyl-rac-glycerol (HY-165089), 1,2-Dioleoyl-3-lauroyl-rac-glycerol (1,2-Olein-3-laurin) is a triglyceride identified by specific analytical methods in human milk, infant formula, other mammalian milk, and vegetable oils, with specific structural and distribution characteristics.
Tenuazonic acid-(acetyl- 13C2) (mixture of diastereomers) in methanol (3-(Acetyl- 13C2)-5-((S)-sec-butyl)-4-hydroxy-1,5-dihydro-2H-pyrrol-2-one) is 13C labeled Tenuazonic acid-(acetyl) (mixture of diastereomers) in methanol .
((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methanol-d2 ((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizine-7a(5H)-methanol-d2) is the deuterium labeled ((2S,7aR)-2-Fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methanol.
MRP4; MOATB; MOAT-B; EST170205; ABCC 4 antibody;
ABCC4 antibody;
ATP binding cassette sub family C (CFTR/MRP) member 4 antibody;
ATP binding cassette sub family C member 4 antibody
IHC-P, FC, ELISA
Human
MRP4 Antibody (YA3530) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to MRP4.
ABC42 antibody; Abcd1 antibody; ABCD1_HUMAN antibody; Adrenoleukodystrophy protein antibody; ALD antibody; Aldgh antibody; ALDP antibody; AMN antibody; ATP binding cassette, sub family D (ALD), member 1 antibody; ATP-binding cassette sub-family D member 1 antibody; ABC42 antibody; Abcd1 antibody; ABCD1_HUMAN antibody; Adrenoleukodystrophy protein antibody; ALD antibody; Aldgh antibody; ALDP antibody; AMN antibody; ATP binding cassette, sub family D (ALD), member 1 antibody; ATP-binding cassette sub-family D member 1 antibody; OTTHUMP00000025960 antibody; OTTMUSP00000019283 antibody; RGD1562128 antibody; RP23 373N8.2 antibody; X linked adrenoleukodystrophy (ALD) gene homolog antibody;
WB, ICC/IF
Human, Mouse, Rat
ABCD1/ALD Antibody (YA6452) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ABCD1/ALD.
ABC20; ABCB1; ATP binding cassette, sub family B(MDR/TAP), member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; PGY1.
IHC-P, IF-Tissue, IHC-F, WB
Human, Mouse, Rat
P Glycoprotein Antibody (YA6354) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to P Glycoprotein.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, WB, ICC/IF, ELISA
Human, Mouse,
P Glycoprotein Antibody (YA5626) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to P Glycoprotein.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
IHC-P, ELISA
Human, Mouse,
P Glycoprotein Antibody (YA5747) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to P Glycoprotein.
ABC20; ABCB1; ATP binding cassette, sub family B; MDR/TAP; , member 1; ATP-binding cassette sub-family B member 1; CD243; CLCS; Colchicin sensitivity; Doxorubicin resistance; GP170; MDR1; MDR1_HUMAN; Multidrug resistance 1; Multidrug resistance protein 1; P glycoprotein 1; P gp; P-glycoprotein 1; PGY1
WB, IHC-P, ICC/IF, IP, ELISA
Human
P Glycoprotein Antibody (YA6028) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to P Glycoprotein.
Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Erlotinib-d6 hydrochloride a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM . Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Zidovudine-d3 is the deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR . Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive . Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Erlotinib- 13C6 hydrochloride is the 13C labeled Erlotinib Hydrochloride . Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM . Erlotinib- 13C6 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives . Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ethynyl Estradiol- 13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor . Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
N-Desmethyl Selegiline-dd5 hydrochloride is the deuterium labeled N-Desmethyl Selegiline hydrochloride . N-Desmethyl Selegiline-d5 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Norethindrone acetate-d8 is the deuterium labeled Norethindrone acetate. Norethindrone acetate is a female hormone used for the research of endometriosis . Norethindrone acetate-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
Sub1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sub1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
SUB1 Human Pre-designed siRNA Set A contains three designed siRNAs for SUB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Sub1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sub1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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