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Anti-Monkey/Human CD28 Antibody (CD28.2) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to monkey/human CD28. Anti-Monkey/Human CD28 Antibody (CD28.2) can block CD28 signaling. Anti-Monkey/Human CD28 Antibody (CD28.2) can be used for the research of immunology .
Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to monkey/human MHC class II. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can inhibits tumor cells proliferation and induce apoptosis. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) increases cellular reactive oxygen species (ROS) and loss of mitochondrial membrane potential in human endothelial cells. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can be used for the researches of cancer and infection, such as lymphoma .
Anti-Monkey/Human CD40L/CD154 Antibody (5C8) is a mouse-derived IgG2a type antibody inhibitor, targeting to monkey/human CD40L/CD154. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) blocks the interactionbetween CD154 and CD40. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) can be used for the researches of inflammation and immunology, such as colitis and transplant .
Anti-Monkey/Human CD20 Antibody (2H7) is a mouse-derived IgG2b κ type antibody inhibitor, targeting to monkey/human CD20. Anti-Monkey/Human CD20 Antibody (2H7) specifically deplete B cells. Anti-Monkey/Human CD20 Antibody (2H7) can be used for the researches of inflammation and metabolic disease, such as diabetes and experimental autoimmune encephalomyelitis .
Type II Collagen, T Cell Grade, from Monkey is a T-cell dependent antigen with unique immunological features. Type II Collagen, T Cell Chick, from Monkey can be used as a stimulating antigen for T-cells in in vitro culture systems .
ATP6V1A Monkey Pre-designed siRNA Set A contains three designed siRNAs for ATP6V1A gene (Monkey), as well as a negative control, a positive control, and a FAM-labeled negative control.
Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) is a Armenian hamster-derived IgG type antibody inhibitor, targeting to mouse/rat/monkey/human ICOS/CD278.
NPRA agonist-11 (Example 161) is an NPRA (NPR1) agonist, with AC50 values of 1.681 μM and 0.989 μM for humans and monkeys, respectively. NPRA agonist-11 can be used in the research of cardiovascular diseases and other disorders .
DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey .
Tiospirone (MJ 13859-1) hydrochloride is an orally active antipsychotic agent that reduces or eliminates tardive dyskinesia (TD) in Cebus apella monkeys with persistent TD .
Adrogolide hydrochloride (ABT-431 hydrochloride) is a chemically stable prodrug that can convert to the dopamine D1 receptor agonist A-86929. Adrogolide hydrochloride ameliorates the MPTP (HY-15608)-induced Parkinson's Disease in marmoset model, reduces the dyskinesias tendency. Adrogolide hydrochloride reverses Risperidone (HY-11018)-induced cognitive deficits in monkey .
SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys .
Ruzasvir (MK-8408) is an orally active inhibitor for genotypic HCV nonstructural protein 5A (NS5A), which inhibits the replication of NS5A mutants GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a and GT4a with EC90 ranging from 0.003 to 0.067 nM. Ruzasvir exhibits good pharmacokinetic characters in rhesus monkey model .
5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus .
Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)
formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys .
SAR441255 TFA is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 TFA displays high potency with balanced activation of all three target receptors.?SAR441255 TFA shows positive acute glucoregulatory effectss in diabetic obese monkeys .
DS79932728 is an orally active inhibitor for G9a and GLP with IC50 of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models .
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .
HbF inducer 3 (Compound dWIZ-2) is an orally active molecular glue, which degrades the WIZ transcription factor (DC50=13 nM in primary human erythroid precursor cell) and induces the expression of fetal hemoglobin (HbF) (EC50=100 nM). HbF inducer 3 exhibits good pharmacokinetic characteristics in cynomolgus monkeys .
Dersimelagon phosphate is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon phosphate shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon phosphate can be used for the research of skin pigmentation .
Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation .
Maridebart cafraglutide (AMG 133) is an antibody-peptide conjugate acting as a GLP-1 receptor agonist and an antagonist of the GIP receptor. Maridebart cafraglutide reduces body weight and improve metabolic markers in male obese mice and cynomolgus monkeys. Maridebart cafraglutide is promising for research of obesity .
GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent .
PD-134672 (CI-992) is a renin inhibitor containing a 2-amino-4-thiazolyl substituent. PD-134672 potently inhibits monkey renin in vitro and only weakly inhibits the related aspartic protease bovine feline hepsin D. The compound exhibits oral hypotensive activity in hyperreninemic normotensive monkeys. Based on its superior efficacy and long-lasting effects in vitro and in the normotensive macaque model, PD-134672 was selected for further evaluation in renal hypertensive monkeys.
Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
PGF2α 1,15-lactone (Prostaglandin F2α 1,15-lactone) is a lipid-soluble internal ester of PGF2α. PGF2α 1,15-lactone decreases menstrual cycle lengths in non-pregnant rhesus monkeys. PGF2α 1,15-lactone terminates early pregnancy in the monkey .
ABBV-154 is an anti-TNF antibody-drug conjugate (ADC). ABBV-154 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-137883). ABBV-154 can be used in studies of rheumatoid arthritis, Crohn's disease and polymyalgia rheumatica .
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
MB-07729 is a potent fructose 1,6-bisphosphatase (FBPase) noncompetitive inhibitor with IC50 values of 31, 121, and 189 nM for human, monkey, and rat, respectively.
RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively .
7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity .
Mirincamycin (hydrochloride) (U-24729 A), a compound used to inhibit malaria, has a protective effect against the early liver stages of Plasmodium but fails to kill dormant liver stages of Plasmodium in a rhesus monkey model.
Hyzetimibe is a cholesterol absorption inhibitor. Hyzetimibe blocks the intestinal absorption of cholesterol and phytol. Hyzetimibe is well tolerated in animal models, with an LDmax 2000 mg/kg in rats and an LDmax 500 mg/kg in rhesus monkeys .
GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT .
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
FCE 28654 is an inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
WR-27653 (RC-12) is a derivative of Catechol with good activity against hypnozoites in the gold-standard Plasmodium cynomolgi-rhesus monkey (Macaca mulatta) model. WR-27653 has antimalarial activity .
CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys .
Fluoroclebopride binds reversibly to dopamine receptors. 18F labeled fluoroclebopride has been used as a probe for studying D2/D3 receptor availability via PET in various monkey models .
MB-07344 is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
MB-07344 sodium is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 sodium has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC50 of 4.2 μM for monkey kidney Vero E6 cells.
Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma .
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
Salvinorin B is a salvinorin, and its analog Salvinorin A is a selective full agonist of κ-opioid receptor (KOPr). Salvinorin A derivative β-tetrahydropyran Salvinorin B also has KOPr agonist activity, activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response, and has central penetrability. Salvinorin B can be used for the study of neuropathic pain (such as paclitaxel-induced pain) and inflammatory diseases[1][2].
LSN3353871 is a potent inhibitor of lipoprotein(a) (Lp(a)) that can binds to Kringle IV (KIV) 8, KIV7–8 and KIV5–8, with Kd of 756 nM, 605 nM and 423 nM, respectively. LSN3353871 disrupts the formation of Lp(a) with the IC50 of 1.69 µM. LSN3353871 has oral bioactivity .
Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
GLP-1R agonist 28 (Compound 19) is an orally active GLP-1R agonist. GLP-1R agonist 28 can increase insulin secretion and can be used in the research of GLP-1R-related diseases .
Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis .
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly .
(R)-RS 56812 hydrochloride is a 5-HT3 receptor antagonist that enhances performance in monkeys on a delayed matching task. The (R) isomer produces more systematic improvements than the (S) isomer and has potential inhibitory effects in diseases involving cognitive decline.
(R)-RS 56812 is a 5-HT3 receptor antagonist that enhances performance in monkeys on a delayed matching task. The (R) isomer produces more systematic improvements than the (S) isomer and has potential inhibitory effects in diseases involving cognitive decline.
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
5-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP .
H-0104 dihydrochloride is a ROCK inhibitor with significant intraocular pressure (IOP)-lowering activity. H-0104 dihydrochloride effectively reduces IOP when administered to monkey eyes. There may not be a direct relationship between the Iop-lowering effect of H-0104 dihydrochloride and ROCK inhibition .
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
Rev 6207 (free base) is a potent non-thiol angiotensin I converting enzyme inhibitor. Rev 6207 (free base) has comparable antihypertensive activity to Enalapril (HY-B0331) in awake monkeys with high renin activity and can be used in the study of hypertensive diseases .
MK-0668 mesylate is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 mesylate exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
MK-0668 is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
Isoxepac (Standard) is the analytical standard of Isoxepac. This product is intended for research and analytical applications. Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
Cevoglitazar (LBM-642) is an orally active and highly potent PPARα and PPARγ dual agonist. Cevoglitazar can reduce food intake, body weight, and fasting plasma insulin in obese mice and cynomolgus monkeys. Cevoglitazar has the potential for diabetes and obesity-related disorders research .
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels .
Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete .
Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete .
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
9-Keto Travoprost is a derivative of Fluprostenol (HY-108560). 9-Keto Travoprost is an EP receptor agonist. 9-Keto Travoprost can be used in endocrine-related research .
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guinea pigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough .
Auranofin (Standard) is the analytical standard of Auranofin. This product is intended for research and analytical applications. Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC50 of 4.2 μM for monkey kidney Vero E6 cells.
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively . Apilimod is a potent and highly selective PIKfyve inhibitor.
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 .
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively . Apilimod is a potent and highly selective PIKfyve inhibitor.
L-751788 is a selective inhibitor of type I of 5α-reductase. L-751788 does not have a significant impact on the differentiation of the external genitalia in animals. When administered orally to pregnant rhesus monkeys, L-751788 (2, 10 mg/kg) did not cause abnormalities in fetal external genitalia .
BMS-351 (compound 18) is a potent, oral active, nonsteroidal CYP17A1 lyase inhibitor with the IC50 values of 19 nM and 4 nM aganist human CYP17A1 and cynomolgus monkeys CYP17A1,respectively. BMS-351 can be used for the study of castration-resistant prostate cancer .
JBSNF-000028 is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 can be used for the research of metabolic disorders .
H-0106 dihydrochloride is a ROCK inhibitor with potent intraocular pressure (IOP)-lowering activity. H-0106 dihydrochloride can effectively inhibit ROCK enzyme. H-0106 dihydrochloride demonstrated significant IOP-lowering effects in monkey eyes. Studies with H-0106 dihydrochloride suggest that there may not be a direct relationship between ROCK inhibition and IOP reduction .
CJB-090 dihydrochloride is a partial agonist with activity at dopamine D3 receptors. CJB-090 exhibits partial agonist characteristics in vitro. CJB-090 elicits yawning responses only in monkeys with an extensive history of cocaine use. CJB-090 reduces the reinstatement effects of cocaine in reinstatement behaviors induced by cocaine .
NW-1172 (free base) (compound 22b) is a 5-HT3 receptor antagonist with performance-enhancing activity in a delayed matching task in monkeys, with the (R) isomer producing more systematic improvements than the (S) isomer, a difference paralleled by the higher affinity of the (R) enantiomer for the 5-HT3 receptor.
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
JBSNF-000028 hydrochloride is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 hydrochloride can be used for the research of metabolic disorders .
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension .
Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels .
Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels .
JBSNF-000028 TFA is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 TFA can be used for the research of metabolic disorders .
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
JNJ-70218902 is a bispecific antibody that binds to human TMEFF2 on cancer cells and to human CD3 on T cells. JNJ-70218902 induces an exposure-dependent proinflammatory response and targeted tumor cell lysis, and promotes T cell-mediated tumor cell killing (EC50: 1.4 nM). JNJ-70218902 has a promising potential for prostate cancer research. The recommended isotype control is human IgG4 kappa, isotype control (HY-P99003) .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Antileishmanial agent-17 is a coumarin hybrid compound with antileishmanial effects (IC50 <0.78 μM). Antileishmanial agent-17 is safe to normal VERO cells. Antileishmanial agent-17 binds to folate pathway enzymes pteridine reductase and DHFR-TS. And Antileishmanial agent-17 shows the most potent with IC50 value of 0.40 μM against promastigote and 0.68 μM against amastigote, respectivley.
Etripamil (MSP-2017) is a short-acting, L-type calcium-channel antagonist. Etripamil inhibits calcium influx through slow calcium channels, thereby slowing AV node conduction and prolonging the AV node refractory period. Etripamil increases heart rate and decreases systolic blood pressure. Etripamil can be used in the study of paroxysmal supraventricular tachycardia (PSVT) .
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
AGN 191976 is a potent and selective thromboxane A2-sensitive (TP) receptor agonist with EC50 values of 0.23 nM and 24 nM in rat aorta and human platelets, respectively. AGN 191976 has potent IOP-lowering effects in dogs and monkeys. AGN 191976 can be used to study vascular biology and the role of thromboxane A2 in vascular function .
Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
(rac)-AL-37350A ((rac)-4,5-DHP-AMT) is a 5-HT2 receptor agonist with intraocular pressure-lowering activity. (rac)-AL-37350A has high affinity and selectivity for the 5-HT2 receptor and effectively reduces intraocular pressure in conscious hypertensive cynomolgus monkeys.
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
Ubrogepant (Standard) is the analytical standard of Ubrogepant. This product is intended for research and analytical applications. 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 .
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
TC-1698 dihydrochloride is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 dihydrochloride improves memory and has neuroprotective effects. TC-1698 dihydrochloride can be used for Alzheimer's disease research .
TC-1698 is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 improves memory and has neuroprotective effects. TC-1698 can be used for Alzheimer's disease research .
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
Gentulizumab (Gensci-059) is a humanized IgG4 antibody that targets CD47. Gentulizumab displays strong binding to CD47 in both human and monkey, and effectively inhibits the CD47-SIRPα interaction. Gentulizumab exhibits a potent antitumor activity. The isotype control for Gentulizumab can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer .
15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
MK-6240 is a blood-brain barrier-permeable positron emission tomography (PET) tracer targeting neurofibrillary tangles (NFTs) (Kd = 0.42 nM). MK-6240 can be used for imaging neurofibrillary tangle pathology in Alzheimer's disease and hereditary frontotemporal dementia .
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkeyIL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .
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 .
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
ALS-I-41 is a novel, potent and selective oxytocin receptor antagonist with the potential to modulate biological activities related to social behavior and mental disorders. ALS-I-41 is being evaluated for behavioral pharmacology experiments in non-human primates and can be administered via intranasal or intramuscular injection. The central nervous system penetration and metabolic rate of ALS-I-41 were studied by mass spectrometry analysis in cerebrospinal fluid and plasma of macaque monkeys .
PPACK TFA is potent, selective and irreversible thrombin inhibitor. PPACK TFA can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK TFA is also a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit the binding of rt-PA to plasma protease inhibitors .
7-Ethoxycoumarin (Standard) is the analytical standard of 7-Ethoxycoumarin. This product is intended for research and analytical applications. 7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN, HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection .
7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
Ganciclovir triphosphate (GCV-TP) disodium is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate disodium is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate disodium has an IC50 of 0.01 μM against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate disodium has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
Ambenoxan hydrochloride is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
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 .
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
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 .
Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases .
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
15(S)-Latanoprost (Standard) is the analytical standard of 15(S)-Latanoprost. This product is intended for research and analytical applications. 15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. 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 .
LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.
Bofanglutide (GZR18) is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression .
DA-302168S is an orally active and selective agonist targeting the GLP-1R, with EC50 value of 1.32 nM. DA-302168S stimulates insulin secretion and shows hypoglycemic effects. DA-302168S decreases food intake. DA-302168S mainly activates GLP-1R of monkeys and humans, and exhibits little excitatory effect on GLP-1R of rats, mice, and dogs. DA-302168S can be used for type 2 diabetes and obesity study .
TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3. TP0463518 competitively inhibits human PHD1 (IC50=18 nM), PHD2 (Ki=5.3 nM), and PHD3 (IC50=63 nM), and targets monkeyPHD2 with an IC50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia .
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
A-86929 is a highly potent and selective dopamine D1 receptor agonist with a pKi value of 7.3. In the 6-OHDA (HY-B1081)-induced unilateral nigrostriatal lesion rat model, A-86929 significantly induces rotational behavior. It also improves motor function in the MPTP (HY-15608)-induced Parkinson's disease marmoset model. Additionally, A-86929 demonstrates potential therapeutic value in reducing cocaine-seeking behavior in rats and reversing Haloperidol (HY-14538)-induced cognitive deficits in rhesus monkeys. A-86929 can be used for research in neurological disorders .
AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research .
Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targeting ICOSL. Prezalumab inhibits T cell activation and related immune responses by binding to ICOSL and blocking the interaction between ICOS and ICOSL. Prezalumab can be used in the research of autoimmune diseases and inflammatory diseases such as systemic lupus erythematosus. Recommend Isotype Controls: Human IgG2 kappa, Isotype Control (HY-P99002) .
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells .
15-keto-17-phenyl trinor Prostaglandin F2α (15-keto-17-phenyl trinor PGF2α) is an F-series prostaglandin (PG) analog. The potential metabolite of 15-keto-17-phenyl trinor Prostaglandin F2α in animals is 15-keto PG. 15-keto PG can slightly reduce the intraocular pressure (1 mm Hg) in normal cynomolgus monkeys when administered at a dose of 1 μg/eye. 15-keto-17-phenyl trinor Prostaglandin F2α is a miotic agent in cats, reducing the pupil diameter by 8 mm at a dose of 5 μg/eye.
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- ( )-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
Pafuramidine (maleate) (DB289 (maleate)) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine (maleate) (DB289 (maleate)) is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion .
Pafuramidine (Standard) is the analytical standard of Pafuramidine. This product is intended for research and analytical applications. Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria[1][2][3].
Molidustat (Standard) is the analytical standard of Molidustat. This product is intended for research and analytical applications. Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia .
Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
15-keto Latanoprost is a potential metabolite of latanoprost (HY-B0577) when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye.1 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm Hg reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type prostaglandins; for example, prostaglandin F2α will produce this degree of miosis at a dose of less than 1 μg/eye.
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease .
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
15(R)-17-phenyl trinor Prostaglandin F2α isopropyl ester (15(R)-17-phenyl trinor PGF2α isopropyl ester) is the latanoprost-related isomer containing both a double bond at 13,14 and an inverted (β) hydroxyl group at C-15. Similar to 15(S)-latanoprost, 15(R)-17-phenyl trinor PGF2α isopropyl ester is a potential impurity in most commercial preparations of the latanoprost bulk drug product. The IC50 values for the free acid forms of 15(S)-17-phenyl trinor PGF2α and 15(R)-17-phenyl trinor PGF2α were determined to be 0.71 nM and 30 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle.1 A 3 μg dose of 15(R)-17-phenyl trinor PGF2α caused a 1.9 mmHg reduction of IOP in normotensive cynomolgus monkeys.
17-phenyl trinor PGF2α N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.1 The N-ethyl amide prostaglandin prodrugs are converted to the active free acid more slowly than the analogous prostaglandin ester prodrugs such as latanoprost.2 This product is the isopropyl ester of the free acid prostaglandin which corresponds to Bimatoprost. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist.3 In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. The 17-phenyl trinor PGF2α isopropyl ester derivative is examined for IOP-lowering activity during the development of latanoprost.4 At the dose of 3 μg/eye in the monkey, 17-phenyl trinor PGF2α isopropyl ester is the most potent analog tested in reducing IOP, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost. However, this derivative is also significantly more irritating to the eye than latanoprost.
NX-2127 (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
Cholesterol (Excipient, GMP Like) is the GMP Like class Cholesterol (HY-N0322), and can be used as pharmaceutical excipients. Cholesterol is a component of the cell membrane and a precursor of some hormones, vitamin D and bile acid, with oral activity.
In Vitro: Cholesterol (200 μg/mL; 40 h) increases the production of newly synthesized β-amyloid protein and enhances the secretion of Aβ1-40 in HEK cells transfected with APP .
In Vivo: Cholesterol (0.5% cholesterol in diet; oral; once daily; 7 days) increases plasma cholesterol in the hamster model, while the cholesterol absorption inhibitor SCH 48461 (10 mg/kg; oral gavage; once daily; 7 days) inhibits cholesterol absorption and reduces plasma cholesterol . Cholesterol (1% cholesterol + 0.5% bile acid in diet; oral; once daily; 7 days) increases plasma cholesterol levels in the male CD rat model, while SCH 48461 (2 mg/kg; oral; once daily; 7 days) reduces hepatic cholesterol ester accumulation . Cholesterol (0.25% cholesterol + 22% saturated fat diet; oral; once daily; 3 weeks) increases VLDL+LDL cholesterol levels in the rhesus monkey model, while SCH 48461 (0.2 mg/kg; oral; once daily; 3 weeks) maintains baseline levels and inhibits cholesterol absorption .
Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, KD=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
Type II Collagen, T Cell Grade, from Monkey is a T-cell dependent antigen with unique immunological features. Type II Collagen, T Cell Chick, from Monkey can be used as a stimulating antigen for T-cells in in vitro culture systems .
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- ( )-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys .
SAR441255 TFA is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 TFA displays high potency with balanced activation of all three target receptors.?SAR441255 TFA shows positive acute glucoregulatory effectss in diabetic obese monkeys .
Peptide M is a synthetic amino acid (18 amino acids in length which correspond to the amino acid positions 303-322 of bovine S-antigen: DTNLASSTIIKEGIDKTV), is capable of inducing experimental autoimmune uveitis in monkeys and Hartley guinea pigs as well as Lewis rats .
β-MSH (monkey) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
CBLB 612 is an anti-radiation agent. CBLB 612 can be used in the propagation of mouse and monkey moderate stimulation hematopoietic stem cell (HSC), and lure that they are passed to peripheral blood from bone marrow into. CBLB 612 is an important auxiliary agent for cancer .
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
PPACK TFA is potent, selective and irreversible thrombin inhibitor. PPACK TFA can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK TFA is also a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit the binding of rt-PA to plasma protease inhibitors .
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
Bofanglutide (GZR18) is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
Anti-Monkey/Human CD28 Antibody (CD28.2) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to monkey/human CD28. Anti-Monkey/Human CD28 Antibody (CD28.2) can block CD28 signaling. Anti-Monkey/Human CD28 Antibody (CD28.2) can be used for the research of immunology .
Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to monkey/human MHC class II. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can inhibits tumor cells proliferation and induce apoptosis. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) increases cellular reactive oxygen species (ROS) and loss of mitochondrial membrane potential in human endothelial cells. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can be used for the researches of cancer and infection, such as lymphoma .
Anti-Monkey/Human CD40L/CD154 Antibody (5C8) is a mouse-derived IgG2a type antibody inhibitor, targeting to monkey/human CD40L/CD154. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) blocks the interactionbetween CD154 and CD40. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) can be used for the researches of inflammation and immunology, such as colitis and transplant .
Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma .
Anti-Monkey/Human CD20 Antibody (2H7) is a mouse-derived IgG2b κ type antibody inhibitor, targeting to monkey/human CD20. Anti-Monkey/Human CD20 Antibody (2H7) specifically deplete B cells. Anti-Monkey/Human CD20 Antibody (2H7) can be used for the researches of inflammation and metabolic disease, such as diabetes and experimental autoimmune encephalomyelitis .
Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) is a Armenian hamster-derived IgG type antibody inhibitor, targeting to mouse/rat/monkey/human ICOS/CD278.
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis .
JNJ-70218902 is a bispecific antibody that binds to human TMEFF2 on cancer cells and to human CD3 on T cells. JNJ-70218902 induces an exposure-dependent proinflammatory response and targeted tumor cell lysis, and promotes T cell-mediated tumor cell killing (EC50: 1.4 nM). JNJ-70218902 has a promising potential for prostate cancer research. The recommended isotype control is human IgG4 kappa, isotype control (HY-P99003) .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
Gentulizumab (Gensci-059) is a humanized IgG4 antibody that targets CD47. Gentulizumab displays strong binding to CD47 in both human and monkey, and effectively inhibits the CD47-SIRPα interaction. Gentulizumab exhibits a potent antitumor activity. The isotype control for Gentulizumab can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkeyIL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN, HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection .
Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases .
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research .
Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targeting ICOSL. Prezalumab inhibits T cell activation and related immune responses by binding to ICOSL and blocking the interaction between ICOS and ICOSL. Prezalumab can be used in the research of autoimmune diseases and inflammatory diseases such as systemic lupus erythematosus. Recommend Isotype Controls: Human IgG2 kappa, Isotype Control (HY-P99002) .
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion .
7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity .
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
Salvinorin B is a salvinorin, and its analog Salvinorin A is a selective full agonist of κ-opioid receptor (KOPr). Salvinorin A derivative β-tetrahydropyran Salvinorin B also has KOPr agonist activity, activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response, and has central penetrability. Salvinorin B can be used for the study of neuropathic pain (such as paclitaxel-induced pain) and inflammatory diseases[1][2].
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
Isoxepac (Standard) is the analytical standard of Isoxepac. This product is intended for research and analytical applications. Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
7-Ethoxycoumarin (Standard) is the analytical standard of 7-Ethoxycoumarin. This product is intended for research and analytical applications. 7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
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 .
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 .
Human, Mouse, Monkey, Goat, Hamster, Rat, Chlamydomonas Reinhardtii
Beta Tubulin Antibody (YA839) is a non-conjugated and Mouse origined monoclonal antibody about 50-55 kDa, targeting to Tubulin beta chain (TUBB). It can be used for WB,ICC/IF assays in the background of Human, Mouse, Monkey, Goat, Hamster, Rat, Chlamydomonas Reinhardtii.
A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
Cholesterol (Excipient, GMP Like) is the GMP Like class Cholesterol (HY-N0322), and can be used as pharmaceutical excipients. Cholesterol is a component of the cell membrane and a precursor of some hormones, vitamin D and bile acid, with oral activity.
In Vitro: Cholesterol (200 μg/mL; 40 h) increases the production of newly synthesized β-amyloid protein and enhances the secretion of Aβ1-40 in HEK cells transfected with APP .
In Vivo: Cholesterol (0.5% cholesterol in diet; oral; once daily; 7 days) increases plasma cholesterol in the hamster model, while the cholesterol absorption inhibitor SCH 48461 (10 mg/kg; oral gavage; once daily; 7 days) inhibits cholesterol absorption and reduces plasma cholesterol . Cholesterol (1% cholesterol + 0.5% bile acid in diet; oral; once daily; 7 days) increases plasma cholesterol levels in the male CD rat model, while SCH 48461 (2 mg/kg; oral; once daily; 7 days) reduces hepatic cholesterol ester accumulation . Cholesterol (0.25% cholesterol + 22% saturated fat diet; oral; once daily; 3 weeks) increases VLDL+LDL cholesterol levels in the rhesus monkey model, while SCH 48461 (0.2 mg/kg; oral; once daily; 3 weeks) maintains baseline levels and inhibits cholesterol absorption .
ATP6V1A Monkey Pre-designed siRNA Set A contains three designed siRNAs for ATP6V1A gene (Monkey), as well as a negative control, a positive control, and a FAM-labeled negative control.
