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

Drug Metabolite

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.

Drug Metabolite Related Products (311):

Cat. No. Product Name Effect Purity
  • HY-17366
    Clozapine N-oxide
    Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
  • HY-13318
    Oseltamivir acid
    Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses.
  • HY-100599
    Urolithin A
    Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
  • HY-126303C
    GS-443902 trisodium
    GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).
  • HY-17366A
    Clozapine N-oxide dihydrochloride
    Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
  • HY-142122
    Imipramine N-oxide
    Imipramine N-oxide is the metabolite of Imipramine. Imipramine is a tertiary amine tricyclic antidepressant.
  • HY-B0199
    Mycophenolate Mofetil
    Mycophenolate mofetil (RS 61443) is the morpholinoethylester prodrug of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.
  • HY-137316A
    Phosphoramide mustard (cyclohexanamine)
    Phosphoramide mustard cyclohexanamine is a biologically active metabolite of Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA damage.
  • HY-112226
    VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.
  • HY-117433
    4-Hydroperoxy cyclophosphamide
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide has the potential for lymphomas and autoimmune disorders.
  • HY-B0300
    Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine increases free copper and enhances oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria.
  • HY-103252
    Monomethyl fumarate
    Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.
  • HY-B1417
    Nortriptyline hydrochloride
    Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride), the main active metabolite of Amitriptyline, is a tricyclic antidepressant used to relieve the symptoms of depression. Nortriptyline hydrochloride is a potent autophagy inhibitor.
  • HY-B0794B
    AZ7550 Mesylate
    AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  • HY-128669
    Abemaciclib metabolite M2
    Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s of 1.2 and 1.3 nM, respectively. Anti-cancer activity.
  • HY-14798
    Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.
  • HY-18719B
    Endoxifen hydrochloride
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
  • HY-136303
    GS-704277 is an alanine metabolite of Remdesivir. Remdesivir, a nucleoside analogue with effective antiviral activity, is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.
  • HY-103638
    3-Methoxytyramine hydrochloride
    3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1).
  • HY-32350
    Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.