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.
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GC45239
δ4-Abiraterone
CB 7627, D4A
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)
Wy 45494
A minor active metabolite of venlafaxine -
GC12404
(+)-Ketoconazole
R 41400
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)-5-Ethyl-3-methyl-5-phenylhydantoin
S-Mephenytoin (5-phenyl-5-ethyl-N-methylhydantoin) is an anticonvulsive drug which is metabolized by N-demethylation and 4-hydroxylation (of the aromatic ring). - GC33073 1-Ethynylnaphthalene 1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
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GC13836
2,3-dihydrothieno-Thiadiazole Carboxylate
MTCC
CYP450 enzymes (CYP2E1 and CYP2B4) inhibitor -
GC12262
2-Phenyl-2-(1-piperidinyl)propane
1-(α,α-dimethylbenzyl)-Piperidine,PPP
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.
-
GC68544
4,5-Dimethoxycanthin-6-one
4,5-Dimethoxycanthin-6-one is an effective and non-competitive inhibitor of CYP1A2-mediated phenacetin O-deethylation, with an IC50 value of 1.7 μM and a Ki value of 2.6 μM. It is a bioactive alkaloid isolated from Picrasma quassioides BENNET (Simaroubaceae).
- GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes.
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GC11758
4-phenyl-5-methyl-1,2,3-Thiadiazole
NSC 358739
CYP2B4 and CYP2E1 inhibitor -
GN10241
5-Methoxypsoralen
5-Methoxypsoralen, 5-MOP, Heraclin, NSC 95437
- 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
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GC17645
Abiraterone
CB-7598
A CYP17A1 inhibitor and an active metabolite of abiraterone acetate -
GC11108
Abiraterone acetate
CB-7630
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.
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GC14781
ABT (1-Aminobenzotriazole)
ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987
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
CI-58000, NSC 7212
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.
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GN10150
Apigenin
Chamomile, Flavone, NSC 83244, Versulin
Apigenin (API), or 4′,5,7-trihydroxyflavone, is a bioactive flavonoid present in many plants, known for its anti-inflammatory, antioxidant, and anticancer properties. -
GC12945
Atazanavir
BMS 232632, CGP 73547
An inhibitor of HIV-1 protease - GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease
-
GC65088
Atovaquone-d5
Atavaquone-d5
-
GC10999
Avasimibe
Cl-1011, PD-148515
An ACAT inhibitor -
GC34132
Bergamottin (5-Geranoxypsoralen)
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
α-Cedrol
A sesquiterpene alcohol -
GC16751
Chlorzoxazone
NSC 26189
Muscle-relaxing drug -
GC68863
Cholesterol 24-hydroxylase-IN-1
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active and highly selective inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) with an IC50 of 8.5 nM. Cholesterol 24-hydroxylase-IN-1 can penetrate the blood-brain barrier.
- GC11170 Choline Fenofibrate
-
GC35692
Chrysosplenetin
Chrysosplenol B, Chrysosptertin B, EMD 20940, Polycladin
A flavonoid with diverse biological activities -
GC16754
Clarithromycin
A-56268, Antibiotic A 56268, TE 031
A macrolide antibiotic - GC38758 Clomethiazole Chlormethiazole is an potent and orally active GABAA?agonist.
-
GC14269
Cobicistat (GS-9350)
GS-9350
An inhibitor of CYP3A -
GN10338
Compound K
Ginsenoside Compound K, Ginsenoside IH901
-
GC41611
Curcumenol
(+)-Curcumenol
Curcumenol is a sesquiterpene that has been found in Curcuma species. - GC70725 CYP11B2-IN-1 CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM.
- 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
PF-00251802 hydrochloride
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. - GC71411 Dasatinib analog-1 Dasatinib analog-1 (compound 5826) inhibits CYP3A4 viability with a Ki value of 5.4 μM.
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GC49817
Desethoxy Quetiapine (hydrochloride)
O-Desalkylquetiapine
An active metabolite of quetiapine -
GC49866
Desmethyl Carvedilol
BM 14242, O-desmethyl Carvedilol
An active metabolite of carvedilol -
GC49842
Digoxigenin Bisdigitoxoside
Bisdigoxigenin
A Na+/K+-ATPase inhibitor -
GC30479
Dihydromethysticin ((+)-Dihydromethysticin)
NSC 112159
Dihydromethysticin ((+)-Dihydromethysticin) is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23. -
GC16550
Diosmetin
Diosmetol, Luteolin 4'-methyl ester
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.
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GC12892
Doxepin (hydrochloride)
Sinequan
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.
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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.
-
GN10137
Galangin
NSC 407229, 3,5,7-Trihydroxyflavone
-
GC14915
Gemfibrozil
CI719
PPARα activator -
GN10720
Gentiopicrin
Gentiopicroside, NSC 606402
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GN10032
Ginsenoside F1
GF1, Panaxoside A Progenin
- 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.
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GC49855
Harmalol (hydrochloride hydrate)
11-hydroxy Harmalan, Harmidol
A β-carboline alkaloid and an active metabolite of harmaline - GC71313 hCYP3A4 Fluorogenic substrate 1 hCYP3A4 Fluorogenic substrate 1 is a potrnt hCYP3A4 fluorogenic substrate with an Km value of 0.36 μM.
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GC11540
HET0016
N-hydroxy-N'-(4-n-butyl-2-methylphenyl)Formamidine
inhibitor of 20-HETE formation -
GC49832
Hydroxymetronidazole
hydroxy-MNZ
Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. -
GC16707
Isavuconazole
BAL4815, RO 0094815
triazole antifungal drug - GC36335 Isoglycycoumarin Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis.
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GN10568
Isosilybin
Isosilibinin, Isosilybinin, Silybin B
-
GC17337
Ketoconazole
R 41400
A triazole antifungal agent -
GC38554
Liarozole dihydrochloride
R75251 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
- GC70453 LY43578 LY43578 is an orally active aromatase inhibitor.
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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
Akatinol, Axura, Ebix, Namenda, NSC 102290, SUN Y7017
NMDA receptor antagonist -
GC41373
Methysticin
Kavatin, (+)-Methysticin, NSC 112158
Methysticin is a kavalactone isolated from the kava roots. -
GC17411
Metyrapone
NSC 25265, SU 4885
11-β hydroxylase (CYP11B1) inhibitor -
GC16423
Monoacetylphloroglucinol
MAPG,NSC 54927,Phloroacetophenone,2',4',6'-Trihydroxyacetophenone
Monoacetylphloroglucinol (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity. -
GC36754
N-Nornuciferine
Daechualkaloid E, (R)-Nornuciferine, (–)-Nornuciferine, Sanjoinine Ia
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
NSC 5548
-
GC49851
Norquetiapine
N-Desalkylquetiapine
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.
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GC30966
Olivetol
5-n-Amylresorcinol, 5-Pentylresorcinol
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
OMEP sulfone, OMP sulfone, OMZ sulfone
Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor. - GC71393 Opevesostat Opevesostat is a cholesterol side-chain cleavage enzyme (CYP11A1) inhibitor.
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GC36822
Oteseconazole
VT-1161
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
CYP3cide,PF-04981517,PF4981517
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
Remofovir 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).