CYP2 Selective Inhibitors | Chemicals

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S0721	Ticlopidine	Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina,PCR 5332) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.	Selective	CYP2B6, Ki: 0.2 μM
S0922	Salvianolic acid C	Salvianolic acid C is a non-competitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2).	Selective	CYP2C8, Ki: 4.82 μM; CYP2J2, Ki: 5.75 μM
S9241	Polygalaxanthone III	Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.	Selective	CYP2E1, IC50: 50.56 μM
S5658	Omeprazole Sodium	Omeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19.	Selective
S1952	Methoxsalen	Methoxsalen (Xanthotoxin, NCI-C55903) is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.	Selective
S3777	Gentiopicroside	Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.	Selective
S4221	Benzbromarone	Benzbromarone(Desuric) is a CYP2C9 inhibitor, it binds to CYP2C9 with K_i value of 19.3 nM.	Pan	CYP2C9, Ki: 19.3 nM
S1794	Fenofibrate	Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.	Pan	CYP2C19, IC50: 0.2 μM; CYP2B6, IC50: 0.7 μM; CYP2C9, IC50: 9.7 μM
S3673	Sulfaphenazole	Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).	Pan	CYP2C9, Ki: 0.3 μM
S4938	Cedrol	Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.	Pan	CYP2B6, Ki: 0.9 μM
S2046	Pioglitazone HCl	Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent	Pan	CYP2C8, Ki: 1.7 μM; CYP2C9, Ki: 32.1 μM
S2262	Apigenin (LY 080400)	Apigenin (NSC 83244, LY 080400) is a potent P450 inhibitor for CYP2C9 with K_i of 2 μM.	Pan	CYP2C9, Ki: 2 μM
S2187	Avasimibe	Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.	Pan	CYP2C9, IC50: 2.9 μM; CYP2C19, IC50: 26.5 μM
S0110	APD597	APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).	Pan	CYP2C9, IC50: 5.8 μM
S4741	Danshensu	Danshensu (Salvianic acid A), a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects. Danshensu inhibits CYP2E1 and CYP2C9 with IC50 of 36.63 and 75.76 μm, respectively.	Pan	CYP2E1, IC50: 36.63 μM; CYP2C9, IC50: 75.76 μM
S3931	Ginsenoside Rd	Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP	Pan	CYP2D6, IC50: 58.0 μM; CYP2C9, IC50: 85.1 μM
S2268	Baicalein	Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.	Pan