2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Drug Metabolite

Drug Metabolite

Drug Metabolite

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Drug metabolite results when a drug is metabolized into a modified form which continues to produce effects. Drug metabolism redox reactions such as heteroatom dealkylations, hydroxylations, heteroatom oxygenations, reductions, and dehydrogenations can yield active metabolites, and in rare cases even conjugation reactions can yield an active metabolite.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W009538
    5'-Deoxy-5-fluorocytidine
    		99.91%
    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.
    5'-Deoxy-5-fluorocytidine
  • HY-135731
    4-Methylamino antipyrine
    		99.80%
    4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic agent and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
    4-Methylamino antipyrine
  • HY-100431A
    IMR-1A
    		98.01%
    IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
    IMR-1A
  • HY-122489
    DL-Laudanosine
    		99.53%
    DL-Laudanosine, an Atracurium and Cisatracurium metabolite, crosses the blood–brain barrier and may cause excitement and seizure activity.
    DL-Laudanosine
  • HY-111177
    Pheneturide
    		99.20%
    Pheneturide (Ethylphenacemide, M 551), a decarboxylation product of Phenobarbital, can be used to prevent psychomotor seizures.
    Pheneturide
  • HY-N2013
    Aristolactam I
    		99.31%
    Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis.
    Aristolactam I
  • HY-W052508
    Norquetiapine
    		99.95%
    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.
    Norquetiapine
  • HY-114794
    Desglymidodrine
    Desglymidodrine (ST 1059), the active metabolite of Midodrine (HY-12749), is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure.
    Desglymidodrine
  • HY-131669
    Dasatinib metabolite M6
    		99.64%
    Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib (HY-10181). Dasatinib is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor.
    Dasatinib metabolite M6
  • HY-23093
    L-Aspartyl-L-phenylalanine
    		≥98.0%
    L-Aspartyl-L-phenylalanine is a metabolite of aspartame that can inhibit angiotensin converting enzyme (ACE) purified from rabbit lungs with a Ki of 11 μM.
    L-Aspartyl-L-phenylalanine
  • HY-136578
    RP101988
    		98.80%
    RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
    RP101988
  • HY-135746
    OR-1896
    		99.04%
    OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
    OR-1896
  • HY-W016393
    Dihydroconiferyl alcohol
    		99.91%
    Dihydroconiferyl alcohol is a cell division factor that can be found in pring sap of Acer pseudoplatanus L. Dihydroconiferyl alcohol can stimulate growth of soybean callus.
    Dihydroconiferyl alcohol
  • HY-W010031
    1-Methyluric acid
    		≥99.0%
    1-Methyluric acid acts on the urinary bladder mucosa and increases the blood glucose, insulin, triglyceride, and cholesterol levels.
    1-Methyluric acid
  • HY-116513
    Adrenochrome
    		98.66%
    Adrenochrome (Adraxone) is an oxidation product of Epinephrine. Adrenochrome is a potent coronary constricting agent in the rat heart. Adrenochrome can be used for neurological disorder research.
    Adrenochrome
  • HY-A0111
    Cefetamet
    		99.42%
    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.
    Cefetamet
  • HY-G0007
    Omeprazole sulfone
    		99.23%
    Omeprazole sulfone is one of the major metabolites of Omeprazole (HY-B0113). Omeprazole sulfone is generated via sulfoxidation mediated by cytochrome P450 3A4 (CYP3A4).
    Omeprazole sulfone
  • HY-N7781
    (-)-(E)-Guggulsterone
    		99.27%
    (-)-(E)-Guggulsterone ((E)-Guggulsterone) is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
    (-)-(E)-Guggulsterone
  • HY-108869
    Fodipir
    		99.81%
    Fodipir is an active metabolite of mangafodipir, involved in mangafodipir-mediated cytoprotection against 7β-hydroxycholesterol-induced cell death.
    Fodipir
  • HY-W008567
    N-Deschlorobenzoyl indomethacin
    N-Deschlorobenzoyl indomethacin (Compound 18), the primary metabolite of indomethacin (HY-14397), lacks the N-p-chlorobenzoyl group in its structure. Consequently, N-Deschlorobenzoyl indomethacin loses inhibitory activity against AKR1C2 and AKR1C3 (AKR1C2 IC50 =100 μM, AKR1C3 IC50 >100 μM), exhibiting no selectivity.
    N-Deschlorobenzoyl indomethacin
Cat. No. Product Name / Synonyms Application Reactivity