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.

Calcitriol (1,25-Dihydroxyvitamin D3) is a metabolite of vitamin D and a vitamin D receptor (VDR) agonist (IC50=0.4 nM). Calcitriol increases intestinal absorption of calcium and phosphorus, and increases bone resorption with parathyroid hormone.

Urolithin A is a natural product, a metabolite of ellagic acid, which inhibits DNA synthesis and induces apoptosis and autophagy. Urolithin A exhibits antioxidant, anti-inflammatory and antitumor activities.

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.

1. Berberrubine chloride (9-Berberoline Chloride) has antitumor activity. 2. Berberrubine has antidiabetic activity. 3. Berberrubine dose-dependently inhibits IL-8 and MCP-1 protein levels in the media and mRNA expression of the cells stimulated with IL-1beta or TNF-alpha.

Anhydrosimvastatin (Dehydro simvastatin) is an impurity of Simvastatin. Simvastatin is an HMG-CoA reductase inhibitor.

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.

Mycophenolic acid glucuronide is the glucuronide metabolite of mycophenolic acid in human plasma.

Clozapine N-oxide dihydrochloride, a derivative of Clozapine and an agonist of human muscarinic design receptors (DREADDs), crosses the blood-brain barrier and activates DREADD receptors hM3Dq and hM4Di.

beta-Nicotyrine is a tobacco alkaloids Metabolite in the liver.

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

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.

SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.

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

Duloxetine metabolite Para-Naphthol Duloxetine is an inactive metabolite of Duloxetine. Duloxetine is an antidepressant and a serotonin-norepinephrine reuptake inhibitor (SNRI).

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.

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

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.

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

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

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.

Florfenicol amine hydrochloride is a synthetic veterinary antibiotic with antimicrobial activity.Florfenicol amine hydrochloride is widely used in aquaculture and ranching for the study of diseases caused by Bartonella, Edwardsiella, Escherichia coli, and Salmonella.

Tetrabenazine Metabolite ((-)-β-HTBZ), a vesicles monoamine transporter 2 (VMAT2) inhibitor, is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite has a high affinity for VMAT2 with a Ki of 13.4 nM. Tetrabenazine Metabolite is often used to study chorea associated with Huntington's disease and other hyperactivity disorders.

24, 25-Dihydroxy VD2 (24,25-Dihydroxy vitamin D2) is a metabolite of vitamin D2, which is the isomer of vitamin D present in the body as 25-hydroxyvitamin D. PF-04957325 is used in the study of autoimmune encephalomyelitis.