Drug Metabolite

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

Hydroxy Itraconazole (R63373) is a triazole compound with antifungal activity for the study of malignant tumors.

Oseltamivir acid (GS4071) is a potent influenza virus neuraminidase inhibitor and the prodrug of GS4071.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

Mycophenolate Mofetil (TM-MMF), an immunosuppressive agent, is the 2-morpholinoethyl ester of mycophenolic acid (MPA), and an inhibitor of inosine monophosphate dehydrogenase (IMPDH).

Phosphoramide mustard is a toxic metabolite of cyclophosphamide with anticancer activity and ovarian toxicity that induces DNA damage.

Niraparib metabolite M1 (Niraparib carboxylic acid metabolite M1) is the carboxylic acid metabolite of Niraparib. Niraparib is a novel poly (ADP-ribose) polymerase (PARP) inhibitor used in cancer research.

7-Hydroxymethotrexate is the major metabolite of Methotrexate.Methotrexate is an inhibitor of folic acid, inhibiting dihydrofolate reductase, which prevents the conversion of folic acid to tetrahydrofolate, and inhibiting DNA synthesis.Methotrexate is also an inhibitor of metabolism.

4-Hydroxymephenytoin ((+ -)-4'-Hydroxymephenytoin) is the metabolism of an antiepileptic drug mephenytoin. Mephenytoin is used as a CYP2C19 substrate.

4-hydroperoxy cyclophosphamide (4-OOH-CY) is an active metabolite of Cyclophosphamide that induces hepatotoxicity.4-Hydroperoxy cyclophosphamide increases levels of glutaminase and aspartate aminotransferase, enhances inflammatory factors and oxidative markers, and Inhibits oxidoreductase activity.4-Hydroperoxy cyclophosphamide is used in the study of cancer and autoimmune diseases.

CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.

S-methyl-KE-298 is the second main metabolite in plasma,is a methyl conjugate of deacetyl-KE-298.KE-298 inhibits matrix metalloproteinase (MMP-1) production from  rheumatoid arthritis (RA) synovial cells.

Linsidomine hydrochloride (SIN-1 chloride) is considered as a metabolite of moxidomine, with vasodilation, inhibition of platelet aggregation, and antiangina activity. In myocardial ischemia-reperfusion models, Linsidomine hydrochloride to reduce myocardial necrosis and reperfusion induced endothelial dysfunction is associated with the cavernosal mechanism of action involved in nitric oxide release.

p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate) is the ethyl ester of p-Coumaric acid. p-Coumaric Acid is a common dietary polyphenol and also a potent immunosuppressive agent in treating autoimmune inflammatory diseases like rheumatoid arthritis.

Desmethyl Erlotinib (CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

Dehydro Nifedipine (BAY-b 4759) is the main metabolite of nifedipine in human plasma. Dehydro Nifedipine inhibits glucose uptake in PC-12 cells with an IC50 value of 130 μM. Nifedipine is a calcium channel blocker used in the treatment of hypertension and angina. Dehydronifedipine is formed when it is metabolized by cytochrome P450 (CYP) isomers CYP3A4 and CYP3A5.

Didesethyl chloroquine (Bisdesethylchloroquine) is an effective myocardial inhibitor. Didesethyl chloroquine (Bisdesethylchloroquine) is the main metabolite of the antimalarial drug chloroquine.

Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias associated with reentry mechanisms. It inhibits the Na-K-ATPase membrane pump, increasing intracellular sodium and calcium concentrations.

3-Sulfopropanoic acid, a major metabolite of treprostinil and its prodrug ALZ-801, is an endogenous molecule present in the cerebrospinal fluid (CSF) of AD patients that inhibits the formation of Aβ42 oligomers.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP ligand via a linker to form SNIPER. N-Deshydroxyethyl Dasatinib is used in the study of cancer and immune diseases.

DL-Laudanosine (Laudanosine) is a recognized metabolite of atracurium and cisatracurium.

N-Desmethyl imatinib (Imatinib metabolite N-Desmethyl imatinib) is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.

N-Desmethylclozapine (Desmethylclozapine) is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors.

Clofibric acid (Chlorofibrinic acid) is an antilipemic agent that is the biologically active metabolite of CLOFIBRATE.

meta-Fexofenadine (meta-MDL-16455) is an isomer of Fexofenadine.

Ferulic acid 4-O-sulfate (Ferulic acid 4-sulfate) is a metabolite of Ferulic acid.Ferulic acid 4-O-sulfate relaxes arteries, lowers blood pressure, and resists oxidative stress under conditions of iron overload in mice and HepG2 cells.Ferulic acid 4-O-sulfate is a metabolite of Ferulic acid.

Clopidogrel Carboxylic Acid hydrochloride (SR 26334) is a major inactive metabolite of clopidogrel, accounting for 85% of circulating clopidogrel, and is produced by hydrolysis by esterases. CLPM is commonly used as a reference standard for metabolic analysis of clopidogrel.

Regorafénib N-oxyde M2 is an active metabolite of Regorafenib, a multi-target inhibitor for VEGFR1 2 3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13 4.2 46, 1.5, 22, 7, and 2.5 nM).

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of atorvastatin calcium salt, a potent HMG-CoA reductase inhibitor (IC50 = 8 nM).

N-Acetylprocainamide (NAPA), the N-acetylated metabolite of Procainamide, is a Class III antiarrhythmic agent, while procainamide is a Class Ia antiarrhythmic drug.

Monobutyl phthalate, the main metabolite of dibutyl phthalate, is an embryotoxin with antiandrogenic properties.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

(E)-10-Hydroxynortriptyline (E-10-OH-NT) is an active metabolite of Nortriptyline with anxiolytic activity and affinity for muscarinic acetylcholine receptors, which can be used in the study of neurological disorders.

5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole, a gastric proton-pump inhibitor used to treat various peptic diseases. Lansoprazole is metabolized through CYP2C19, resulting in the formation of 5-Hydroxylansoprazole[1][2].

Monoethyl phthalate, a metabolite of diethyl phthalate, serves as a urinary biomarker for phthalate exposure and indicates potential risks of thyroid cancer and benign nodules.

Desmethyl Erlotinib hydrochloride (OSI 420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for human EGFR and EGFR autophosphorylation in tumor cells.

Homovanillyl alcohol, a biological metabolite of Hydroxytyrosol, is a phenolic compound found in virgin olive oil (VOO) and wine. It exhibits high scavenging activities, protects red blood cells from hemolysis in a dose-dependent manner, and has a protective effect on cardiovascular disease and total mortality.

Palifosfamide (Isophosphamide mustard) lysine (ZIO-201) is a stable form of palifosfamide. Palifosfamide lysine has broad activity in sarcoma lines in vitro. The IC50 ranges from 2.25 to 6.75 μM for most cell lines except OS222 (IC50=31.5 μM).

6'-hydroxydihydrocinchonidine is a metabolite of quinine, with antimicrobial and antitumor activity, and inhibitory effect on Trypanosoma brucei and Streptococcus pneumoniae.

4-Methylamino antipyrine, an active metabolite of Metamizole, a pyrazolone non-steroidal anti-inflammatory drug (NSAID) that inhibits COX, possesses analgesic, antipyretic, and relatively weak anti-inflammatory properties.

MTIC is the active metabolite of Temozolomide (TMZ) with anticancer and antitumor activity and is used in the study of melanoma.3'-Sialyllactose (3'-SL) sodium is a prebiotic with anti-inflammatory activity.

Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.

Ampyrone (4-Aminoantipyrine) is a reagent for glucose determination in the presence of peroxidase and phenol.

N-Desethyl Sunitinib hydrochloride (SU-12662 hydrochloride) is an active metabolite of Sunitinib with potential anti-cancer activity for the study of cancer.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.