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.
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Drug Metabolite Related Products (1952)
Related Products (1952)
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Antibodies (1)
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Related Compound Screening Libraries (1)
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Clozapine N-oxide
0 ImagesClozapine 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't cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
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SN-38
0 ImagesSynonyms: 7-Ethyl-10-hydroxycamptothecinSN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
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Calcitriol
0 ImagesSynonyms: 1,25-Dihydroxyvitamin D3Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.
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4-Hydroperoxy cyclophosphamide
0 Images4-Hydroperoxy cyclophosphamide is the active metabolite form of the precursor Cyclophosphamide. 4-Hydroperoxy cyclophosphamide cross-links DNA to induce T cell apoptosis independent of caspase receptor activation, and can activate the mitochondrial death pathway by producing reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide can be used in the study of rheumatoid arthritis and autoimmune diseases.
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S-D-Lactoylglutathione
0 ImagesSynonyms: S-Lactylglutathione; (R)-S-LactoylglutathioneS-D-Lactoylglutathione is a crucial intermediate metabolite of the glyoxalase (Glo) system. S-D-Lactoylglutathione acts as a "bridge molecule" for the conversion of methylglyoxal (MGO) into non-toxic D-lactic acid by continuous catalysis from Glo1 to Glo2, preventing cell damage caused by the accumulation of MGO.
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1-Aminoindan
0 ImagesSynonyms: 1-Indanamine; 2,3-Dihydro-1H-inden-1-amine1-Aminoindan (1-Indanamine) is a Rasagiline (HY-14605A) metabolite. 1-aminoindan is shown to bind directly to α-Syn, thereby promoting a neuroprotective “loop” conformation that attenuates the α-Syn misfolding and aggregation. 1-Aminoindan is shown to be neuroprotective. 1-Aminoindan can be used in the research of Parkinson's disease.
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Dihydroartemisinin
0 ImagesSynonyms: Dihydroqinghaosu; β-Dihydroartemisinin; ArtenimolDihydroartemisinin is an orally active metabolite of rtemisinin (HY-B0094) and antimalarial agent. Dihydroartemisinin induces Autophagy by inhibiting NF-κB activation. Dihydroartemisinin promotes ROS accumulation. Dihydroartemisinin exhibits anticancer activity in esophageal cancer cells. Dihydroartemisinin shows schistosomicidal activity against juvenile and adult worms of Schistosoma japonicum, reduces worm burden, and displays antiparasitic activity. Dihydroartemisinin can be used in research related to multiple myeloma, promyelocytic leukemia, esophageal cancer, and Schistosoma japonicum infection.
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Clozapine N-oxide dihydrochloride
0 ImagesClozapine 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 cannot cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
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Oseltamivir acid
0 ImagesSynonyms: GS 4071; Ro 64-0802; Oseltamivir carboxylateOseltamivir 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. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions.
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Teriflunomide
0 ImagesSynonyms: A77 1726Teriflunomide 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.
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(E/Z)-4-Hydroxytamoxifen
0 ImagesSynonyms: Afimoxifene; 4-OHT(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity.
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Mycophenolate Mofetil
0 ImagesSynonyms: RS 61443; TM-MMFMycophenolate 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.
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Trimethylamine N-oxide
0 ImagesTrimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
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Phosphoramide mustard cyclohexanamine
0 ImagesPhosphoramide mustard cyclohexanamine is a biologically active metabolite of Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA damage.
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Gemfibrozil 1-O-β-glucuronide
0 ImagesGemfibrozil 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.
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Pyocyanin
0 ImagesPyocyanin (Pyocyanine) is a toxic, quorum sensing (QS) controlled metabolite produced by Pseudomonas aeruginosa. Pyocyanin is a REDOX active compound that promotes the production of reactive oxygen species (ROS). Pyocyanin has antibacterial and anti-inflammatory activity.
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Monomethyl fumarate
0 ImagesMonomethyl 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.
