cyp2c8

Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatment.

Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil, is a potent and competitive inhibitor of P450 (CYP) isoform CYP2C8, with an IC50 of 4.07 μM.

N-Desmethyl-Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.

MS-PPOH is a potent and selective inhibitor of cytochrome P450 (CYP) epoxygenase, specifically inhibiting CYP2C8 and CYP2C9 with IC50 values of 15 and 11 µM, respectively.

Fenofibrate (Lipanthyl) is a PPARα agonist (EC50=30 μM) and is selective. Fenofibrate also inhibits cytochrome P450 isoforms, such as CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4. Fenofibrate exhibits antihyperlipidemic activity.

'3'-Hydroxy Repaglinide, a primary CYP2C8 metabolite of Repaglinide, is derived from carbamoylmethyl benzoic acid and is used in the treatment of type II diabetes.

4-Hydroxytolbutamide is a sulfonylurea and drug metabolite derived from the metabolism of Tolbutamide by CYP2C8 and CYP2C9 Tolbutamide (HLS 831) is a sulfonylurea hypoglycemic agent.

Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Clopidogrel-β-D-glucuronide is a metabolite of Clopidogrel. It directly interacts with the CYP2C8 enzyme and strongly inhibits the hepatic enzyme CYP2C8.

Lesinurad sodium (RDEA594 sodium) is a selective inhibitor of uric acid reabsorption and is used in the study of cardiovascular diseases.

Salvianolic Acid C is extracted from the root of Salvia miltiorrhiza, a perennial plant in the genus Salvia.

rac-trans-4-hydroxy Glyburide, an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide, is formed by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. It inhibits glyburide binding to rat brain synaptosomes at high and low affinity sites of SUR1/Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.

N-desmethyl Rosiglitazone is a major metabolite of rosiglitazone , a potent and selective PPARγ ligand present in formulations that have been used to treat type 2 diabetes. Rosiglitazone is metabolized by the cytochrome P450 (CYP) isoform CYP2C8 to form N-desmethyl rosiglitazone.

Olmesartan medoxomil impurity C is an impurity of Olmesartan medoxomil, a potent and selective angiotensin (AT1 receptor) inhibitor with an IC50 of 66.2 μM.

PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.

Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine. It is formed by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes from HepG2 cells expressing CYP3A4 or CYP2C8, respectively. Carbamazepine 10,11-epoxide exhibits anticonvulsant activity against maximal electroshock-induced seizures in mice and has been detected in wastewater effluent [1][2][3].

Sulfaphenazole (Plisulfan) is an inhibitor of CYP2C9 (Ki: 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 μM for CYP2C8/CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). At 10 μM, sulfaphenazole has been shown to inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis.

BAY-0069 is a potent and selective PPARγ transactivator, inhibiting human PPARγ and murine PPARγ with IC50 values of 6.3 nM and 24 nM, respectively. BAY-0069 can be used in cancer research.

BMS-986339 is an orally active, potent FXR agonist that engages His298 and ASN287 residues via H-bond formation. It is employed in research on primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH) due to its anti-fibrosis properties.

2-Phenyl-2-(1-piperidinyl)propane (PPP), an analog of phencyclidine, is a chemical compound.

mTOR Inhibitor-14 (compound 14c) is a potent inhibitor of mTOR with minimal inhibition of CYP2C8 and has demonstrated the capability to inhibit tumor growth [1].

BKIDC-1553, an orally active antiglycolytic agent and bumped kinase inhibitor-derived compound, has a predicted half-life of approximately 17 hours in humans. It inhibits CYP2C8 and Angiotensin Converting Enzyme, making it suitable for cancer research [1].