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.

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.

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.

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.

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.

DL-Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

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.

'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.

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

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 hydrochloride is a potent and orally available dual PI3K/mTOR inhibitor. Its IC₅₀ values against PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR are 8 nM, 24 nM, 74 nM, 77 nM and 0.42 nM respectively. It also exerts inhibitory activity against E545K and H1047R mutants with IC₅₀ values of 14 nM and 11 nM, and exhibits significant antitumor effects in in vivo models.

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.