P450
Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.
Products for P450
- Cat.No. Product Name Information
- GC66197 α-?Terpinyl acetate α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
- GC45239 δ4-Abiraterone δ4-Abiraterone is a major metabolite of abiraterone. δ4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
- GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine
- GC12404 (+)-Ketoconazole Potent inhibitor of cytochrome P450c17
- GC30424 (-)-Cephaeline dihydrochloride (NSC 32944) (-)-Cephaeline dihydrochloride (NSC 32944) is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
-
GC14486
(S)-Mephenytoin
S-Mephenytoin is an anticonvulsive drug which is metabolized by N-demethylation and 4-hydroxylation .
- GC33073 1-Ethynylnaphthalene 1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
- GC13836 2,3-dihydrothieno-Thiadiazole Carboxylate CYP450 enzymes (CYP2E1 and CYP2B4) inhibitor
- GC12262 2-Phenyl-2-(1-piperidinyl)propane mechanism-based inactivator of human cytochrome P450 (CYP) 2B6
- GC33071 4'-Methylchrysoeriol 4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
- GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes.
- GC11758 4-phenyl-5-methyl-1,2,3-Thiadiazole CYP2B4 and CYP2E1 inhibitor
- GN10241 5-Methoxypsoralen
- GC35201 8-Geranyloxypsoralen 8-Geranyloxypsoralen is a furanocoumarin isolated from grapefruit, acts as a potent inhibitor of P450 3A4 (CYP3A4) with an IC50 of 3.93 μM.
- GN10330 8-Methoxypsoralen
- GC17645 Abiraterone A CYP17A1 inhibitor and an active metabolite of abiraterone acetate
- GC11108 Abiraterone acetate A CYP17A1 inhibitor
- GC64010 Abiraterone decanoate Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.
- GC14781 ABT (1-Aminobenzotriazole) ABT (1-Aminobenzotriazole) is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).
- GC35236 Acetylshikonin Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity.
- GC16575 Alizarin A CYP450 inhibitor
- GC31141 Antihistamine-1 Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
- GN10150 Apigenin Apigenin (API) is a competitive CYP2C9 inhibitor with a Ki of 2 µM..
- GC12945 Atazanavir An inhibitor of HIV-1 protease
- GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease
- GC65088 Atovaquone-d5
- GC10999 Avasimibe An ACAT inhibitor
- GC34132 Bergamottin (5-Geranoxypsoralen) Bergamottin (5-Geranoxypsoralen) is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
- GC33909 Bergaptol (5-Hydroxypsoralen) Bergaptol (5-Hydroxypsoralen) is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
- GC65345 BI 653048 BI 653048 is a selective and orally active nonsteroidal?glucocorticoid (GC)?agonist with an IC50 value of 55 nM.
- GC32419 BI 689648 BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
- GC31479 BMS-819881 BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM.
- GC32257 Carbosulfan Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers).
- GC31464 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
- GC31460 CDD3506 CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
- GC32991 Cecropin B Cecropin B has high level of antimicrobial activity and is considered as a valuable peptide antibiotic.
- GC38681 Cedrol A sesquiterpene alcohol
- GC16751 Chlorzoxazone Muscle-relaxing drug
- GC11170 Choline Fenofibrate
- GC35692 Chrysosplenetin A flavonoid with diverse biological activities
- GC16754 Clarithromycin A macrolide antibiotic
- GC38758 Clomethiazole Chlormethiazole is an potent and orally active GABAA?agonist.
- GC14269 Cobicistat (GS-9350) An inhibitor of CYP3A
- GN10338 Compound K
- GC41611 Curcumenol Curcumenol is a sesquiterpene that has been found in Curcuma species.
- GC35788 CYP17-IN-1 CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
- GC35803 Dafadine-A Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
- GC63872 Dagrocorat hydrochloride Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor.
- GC49817 Desethoxy Quetiapine (hydrochloride) An active metabolite of quetiapine
- GC49866 Desmethyl Carvedilol An active metabolite of carvedilol
- GC49842 Digoxigenin Bisdigitoxoside A Na+/K+-ATPase inhibitor
- GC30479 Dihydromethysticin ((+)-Dihydromethysticin) Dihydromethysticin ((+)-Dihydromethysticin) is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23.
- GC16550 Diosmetin CYP1A1 inhibitor
- GC19415 DMU2105 DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
- GC19416 DMU2139 DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
- GC12892 Doxepin (hydrochloride) histamine, serotonin, adrenergic, and muscarinic receptors antagonist
- GC65260 EDP-305 EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells).
- GC35981 EMT inhibitor-2 EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes.
-
GC12250
Fenofibrate
PPARα agonist
- GC38623 Fraxinol Fraxinol is isolated from Lobelia chinensis.
-
GC32855
Furafylline
Furafylline, as a long-acting replacement for theophylline in the treatment of asthma, is a methylxanthine derivative[1].
- GN10137 Galangin
- GC14915 Gemfibrozil PPARα activator
- GN10720 Gentiopicrin
- GN10032 Ginsenoside F1
- GN10549 Ginsenoside Rd
- GC39168 GSK2945 hydrochloride GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively.
- GC49855 Harmalol (hydrochloride hydrate) A β-carboline alkaloid and an active metabolite of harmaline
- GC11540 HET0016 inhibitor of 20-HETE formation
- GC49832 Hydroxymetronidazole Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles.
- GC16707 Isavuconazole triazole antifungal drug
- GC36335 Isoglycycoumarin Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis.
- GN10568 Isosilybin
- GC17337 Ketoconazole A triazole antifungal agent
-
GC38554
Liarozole dihydrochloride
?Liarozole dihydrochloride is a P-450 inhibitor and retinoic acid (RA) metabolizing blocking agent inhibits RA metabolism and thereby increases intracellular RA levels in cells that actively produce RA.
- GC67933 LKY-047
-
GC31422
MCH-1 antagonist 1
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM.
- GC10198 Memantine hydrochloride NMDA receptor antagonist
- GC41373 Methysticin Methysticin is a kavalactone isolated from the kava roots.
- GC17411 Metyrapone 11-β hydroxylase (CYP11B1) inhibitor
- GC16423 Monoacetylphloroglucinol Monoacetylphloroglucinol (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity.
- GC36754 N-Nornuciferine N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits CYP2D6 with IC50 and Ki of 3.76 and 2.34 μM, respectively.
- GN10257 Naringin
- GC49851 Norquetiapine An active metabolite of quetiapine
-
GC69602
Obtusifoliol
Obtusifoliol is a specific CYP51 inhibitor, with Kd values of 1.2 μM and 1.4 μM for the affinity to Brucella melitensis (TB) and human CYP51, respectively.
- GC30966 Olivetol Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2.
- GC11155 Omeprazole sulfone Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
- GC36822 Oteseconazole Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51.
- GC12280 PF-4981517 A potent, selective inhibitor of CYP3A4
- GC38421 Phillyrin (Forsythin) Phillyrin (Forsythin) is isolated from Forsythia suspensa Vahl (Oleaceae), has antibacterial and anti-inflammatory activities.
- GN10649 Polygalaxanthone III
- GC19301 Pradefovir mesylate Pradefovir mesylate is a good substrate for liver CYP3A4.
- GC33862 Pyributicarb (TSH-888) Pyributicarb (TSH-888), a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
- GC37061 Quilseconazole Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
- GC30681 Revexepride Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.
- GC33780 RG-12525 (NID 525) RG-12525 (NID 525) is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 (NID 525) is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 μM.
- GC13470 Rhapontigenin inactivator of cytochrome P450 1A1 with antioxidant and anti-cancer activity
- GN10200 Salvianolic acid C
- GN10425 Schisandrin A
- GC37631 Seviteronel Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.