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 (551):

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-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-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-113472
    N-Methyl-4-pyridone-3-carboxamide is a metabolite of coffee pyridines.
  • HY-134240
    L-Threonic acid magnesium
    L-Threonic acid magnesium salt is the enantiomer of Threonic acid and a metabolite of vitamin C. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent.
  • HY-100638A
    RPR132595A hydrochloride
    RPR132595A (NPC) hydrochloride is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine.
  • HY-B0199
    Mycophenolate Mofetil
    Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent 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-15405
    Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
  • HY-129993
    Gemfibrozil 1-O-β-glucuronide
    Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM.
  • HY-112226
    VRT-043198, the agent 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-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-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-117433
    4-Hydroperoxy cyclophosphamide
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the proagent 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-W008772
    4-Hydroxymephenytoin is a metabolism of an antiepileptic agent mephenytoin, which is used as a CYP2C19 substrate.
  • 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-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-32350
    Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2.