P450

Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that function as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compounds, as well as for hormone synthesis and breakdown. In plants, these proteins are important for the biosynthesis of defensive compounds, fatty acids, and hormones.CYPs are, in general, the terminal oxidase enzymes in electron transfer chains, broadly categorized as P450-containing systems. The term "P450" is derived from the spectrophotometric peak at the wavelength of the absorption maximum of the enzyme (450 nm) when it is in the reduced state and complexed with carbon monoxide. Most CYPs require a protein partner to deliver one or more electrons to reduce the iron (and eventually molecular oxygen).

Cat No.	product name
T0179	Ticagrelor	Ticagrelor is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation.
T0595	Naringin	Naringin, a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibiti...
T0603	Phthalic Acid Monooctyl Ester	Phthalic acid mono-2-ethylhexyl ester (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP), which inhibits the 17, 20 lyase activity of CYP17...
T0660	Beta-Tetralone	Beta-Tetralone is a ketone derivative of tetralin.
T0679	Ketoconazole	Ketoconazole, a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
T0792	(-)-Sparteine sulfate pentahydrate	Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker. It can chelate the bivalents calcium and magnesium.
T0920	Ambroxol	Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosol...
T1011	Itraconazole	Itraconazole is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
T10335	Antihistamine-1	Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4...
T10535	BI 653048	BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.
T10535L	BI 653048 phosphate	BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).
T10688	Casopitant mesylate	Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of ant...
T10891	CRTH2-IN-1	CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.
T10923	CYP17-IN-1	CYP17-IN-1 is an effective oral CYP17 inhibitor that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.
T11065	DMU2105	DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
T11066	DMU2139	DMU2139 is a potent and specific CYP1B1 inhibitor with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
T1149	Fenofibrate	Fenofibrate is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic...
T1187	Bifonazole	Bifonazole acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a ...
T11964	MCH-1 antagonist 1	MCH-1 antagonist 1 also inhibits CYP3A4 (IC50: 10μM).MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist (Ki: 2.6 nM).
T12146	N-Desmethyl Apalutamide	N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor, is an active Apalutamide metabolite.
T1274	Benzbromarone	Uricosuric is an effective inhibitor of CYP2C9 used in the treatment of gout.
T1415	Gemfibrozil	Gemfibrozil interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an in...
T1443	Memantine hydrochloride	Memantine hydrochloride is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.
T14678	BMS-819881	BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM and it also is selective and potent for CYP3...
T1597	Proadifen hydrochloride	Proadifen hydrochloride is an inhibitor of drug metabolism and cytochrome P-450 enzyme system activity.
T16111	ML604086	ML604086 suppresses CCL1 mediated chemotaxis and enhances intracellular Ca2 concentrations. ML604086 is a selective inhibitor of CCR8. It also inhibiting CCL1 b...
T16739	RG-12525	RG-12525 is a PPAR-gamma agonist (IC50: appr 60 nM) and a potent inhibitor of CYP3A4 (Ki: 0.5 µM). RG-12525 is a specific and competitive antagonist of the pep...
T1704	Diosmetin	Diosmetin has been found to act as a weak TrkB receptor agonist.
T2143	Bergapten	Bergapten, a psoralen, inhibits cell replication.
T2175	Apigenin	Chamomile is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothin...
T2532	Tauroursodeoxycholic Acid	Tauroursodeoxycholic acid is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans. Tauroursodeox...
T2753	Avasimibe	Avasimibe is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the ...
T2838	Naringenin	Naringenin is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate m...
T2944	Sodium Danshensu	Danshensu (sodium salt) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstrictio...
T2945	Germacrone	Germacrone, a major active component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antivirus activities. It also inhibits ...
T2946	Tanshinone IIA sulfonate sodium	Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator ...
T2949	Alizarin	Alizarin, a red dye derived from the roots of plants of the madder genus, inhibits P450 isoform CYP1A1( IC50 = 6.2 μM), CYP1A2 (IC50 =10.0 μM )and CYP1B1(IC50...
T2S0663	Humantenmine	1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.
T3002	Piperine	Piperine (1-Piperoylpiperidine), a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.
T3355	Naloxegol oxalate	Naloxegol oxalate is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.
T3401	Ginsenoside F1	Ginsenoside F1 is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of t...
T3411	Curdione	Curdione inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be ...
T3417	Amentoflavone	Amentoflavone, as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in ...
T3585	TMS	TMS is a very selective and potent competitive inhibitor of P450 1B1 (CYP1A1).
T3669	Curcumenol	Curcumenol, one of the major components of Zedoary turmeric oil, is an antibiotic drug which has anti-Y, anti-inflammation activity. Curcumenol may be safely us...
T3698	alpha-Asarone	Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
T3736	Olivetol	Olivetol (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses o...
T3768	Epifriedelanol	Epifriedelanol suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can ...
T3776	Rhapontigenin	Rhapontigenin is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic arom...
T3797	Isosilybin	Isosilybin and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.
T3811	Ginsenoside C-K	Ginsenoside C-K is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2.
T3886	Rosavin	Rosavin has antidepressant and anxiolytic actions, helps balance all the neurotransmitters.
T4188	SDZ285-428	NVP-VID-400 (SDZ285-428) is a CYP24A1 inhibitor.
T4498	Stiripentol	Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively)...
T4567	Sulfaphenazole	Sulfaphenazole 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/CYP2...
T4S0800	Demethyleneberberine	Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either...
T5594	Cedrol	Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respecti...
T5715	FLAVOKAVAIN A(P)	FLAVOKAVAIN A(P), a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-depende...
T5786	TETRAHYDROPIPERINE	TETRAHYDROPIPERINE is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.
T5953	1-Aminobenzotriazole	1-Aminobenzotriazole (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.
T5S0669	Bergamotine	1. Bergamotine can significantly reduce blood glucose and increase glucose tolerance and insulin sensitivity in KK-A<sup>y</sup>diabetic mice.
T5S2360	Corydaline	1. Corydaline, an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent. 2. Corydaline promotes gastric emptying a...
T6030	XL388	XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
T6215	Abiraterone Acetate	Abiraterone acetate is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic...
T6216	Abiraterone	Abiraterone (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor (IC50: 4 nM).
T6246	Cobicistat	Cobicistat is a carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with whic...
T6509	Galeterone	Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhib...
T6S0630	Hypaconitine	Hypaconitine, an active and highly toxic constituent derived from Aconitum species, has anti-inflammatory activity, is widely used to treat rheumatism.
T6S1894	Linderane	1. Linderane was characterized as a mechanism-based inactivator of CYP2C9.
T7088	Difubenzuron	Diflubenzuron is a benzoyl-urea insecticide, found to be a potent inhibitor of melanosome synthesis in mouse melanoma cells. Diflubenzuron has also been shown t...
T7190	Actein	Actein has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis, it also can prevent oxidative damage to osteoblas...
T7370	Talarozole	Talarozole is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.4...
T7410	Furafylline	Furafylline is a selective inhibitor of human cytochrome P450 (CYP)1A2 (IC50 : 0.07 μM),
T7427	1-Ethynylnaphthalene	1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 IB1
T7472	7-Hydroxyflavone	7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2.with anti-inflammat...
T7618	Pyributicarb	Pyributicarb is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
T8125	Quinidine sulfate	Quinidine sulfate dihydrate is a potent and selective cytochrome P450db inhibitor
T8182	Guan-fu base A	Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.
T9113	Myristicin	Myristicin has anti-cholinergic, antibacterial, and hepatoprotective effects, it also has anti-inflammatory properties related with its inhibition of NO, cytoki...
TC0039	Vasicinone	Vasicinone may act as a hepatoprotective agent. (±)-Vasicinone has significant antitussive, expectorant, and bronchodilating activities, which can be used to t...
TMA0164	15-Hydroxydehydroabietic acid	15-Hydroxydehydroabietic acid exhibits a promising alpha-glucosidase inhibitory activity, it also shows significant antibacterial activities.
TMA2106	(-)-Sparteine	Sparteine is a class 1a antiarrhythmic agent, a sodium channel blocker. The deficient debrisoquine hydroxylation of Sparteine is due to the absence of P-450IID1...
TN1011	Rhodionin	Rhodionin and rhodionin can inhibit cytochrome P450 2D6 non-competitively with high specificity which could have implications for interactions with co-administe...
TN1023	Miltirone	Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.
TN1027	beta-Amyrin	beta-Amyrin has antiviral, hepatoprotective, antinociceptive, anti-inflammatory, it retard acute inflammation in rat model of periodontitis.
TN1078	Seneciphylline	Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can signific...
TN1210	2-Hydroxy-1-Methoxyaporphine	2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone.
TN1343	8-Geranyloxypsoralen	8-Geranyloxypsoralen inhibits α²-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat a...
TN1372	alpha-Amyrin	Alpha-Amyrin is trypsin and chymotrypsin inhibitor,it has antineoplastic,it induces proliferation of human keratinocytes.Alpha-Amyrin can as a hepatomodulatory ...
TN1378	alpha-Viniferin	Alpha-viniferin is a prostaglandin H2 synthase inhibitor, which has anti-inflammatory, anti-oxidant, anti-arthritis, and anti-tumor activities.
TN1416	Ayanin	Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethyleth...
TN1482	Chamaechromone	Chamaechromone has anti-HBV and insecticidal activity. The hydroxylation of Chamaechromone is inhibited by α±-naphthoflavone, and predominantly catalyzed by r...
TN1526	Corydalmine	Corydalmine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains.1-Corydalmine significantly inhibits spo...
TN1691	Glabrol	Glabrol is a PTP1B inhibitor, it is also a CYP1B1 inhibitor, it shows inhibition of CYP1B1 in live cell assay with the IC50 value of 15uM.
TN1702	Glycycoumarin	Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.
TN1748	Humantenirine	Standard reference
TN1828	Kahweol	Kahweol has anticarcinogenic, anti-angiogenic,and anti-inflammatory activities, it can block the LPS-induced activation of NF-kappaB by preventing IkappaB degra...
TN1854	Lasiodin	Lasiokaurin has anti-oxidative, and antineoplastic activities, it also shows antibacterial activity, esp. against Sarcina lutea.
TN2144	Resveratroloside	Resveratroloside has cardioprotective effect, it exhibits α±-glucosidase inhibitory activity, it also can inhibit hydroxylation of testosterone by CYP3A4.
TN2147	Retrorsine	Retrorsine selectively inhibits hepatocyte proliferation and following liver injury evokes small hepatocyte-like progenitor cells.
TN2179	Saponarin	Saponarin shows in vitro and in vivo hepatoprotective and antioxidant activity against CCl4-induced liver damage.
TN2687	2,3',4,6-Tetrahydroxybenzophenone	2,3',4,6-Tetrahydroxybenzophenone possesses significant antioxidant activity.
TN3080	5,6,7-Trimethoxycoumarin	5,6,7-Trimethoxycoumarin shows moderate inhibitory activity against Micrococcus luteus, it also displays an intermediate cytotoxic effects against brine shrimp ...
TN3147	6',7'-Dihydroxybergamottin	6',7'-Dihydroxybergamottin(DHB), a well-known inhibitor of CYP3A4, the inhibition of CYP3A4 activity by DHB includes the inhibition of POR activity, DHB can inh...
TN3294	8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate	8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate shows inhibitory activity toward CYP2A6 and MAO-A and MAO-B enzymes.
TN3300	8alpha-Tigloyloxyhirsutinolide 13-O-acetate	8alpha-Tigloyloxyhirsutinolide 13-O-acetate shows inhibitory activity toward CYP2A6 and MAO-A and MAO-B enzymes. 8alpha-Tigloyloxyhirsutinolide 13-O-acetate has...
TN3379	Allocryptopine	Allocryptopine has certain effects on anti-injury for hepatocyte, ameliorating liver function, and prohibiting hepatic fibrosis; it increases mRNA levels of cyt...
TN3574	Canadine	Canadine has antioxidant activity with low-toxic effect.
TN3627	Chalepensin	Chalepensin behaves as an energy transfer inhibitor at low concentration, it inhibits multiple P450s and that epoxidation activity is crucial for the potential ...
TN3875	Dipterocarpol	Dipterocarpol is a dammarane-type triterpenoid, as are the major bioactive compounds of ginseng. Dipterocarpol A shows moderate acetylcholinesterase inhibitory ...
TN4130	Germacrone 4,5-epoxide	(4S,5S)-(+)-Germacrone-4,5-epoxide inhibits certain subtypes of cytochrome P450 (CYP).
TN4277	Isocupressic acid	Isocupressic acid induces abortion in pregnant cows when ingested primarily during the last trimester, it decrease affects the angiogenesis of the female reprod...
TN4424	Lecanoric acid	Lecanoric acid shows antioxidant activity with an IC50 value of 79-95 ug/ml, it at 100 ug/ml conc. shows high growth stimulating activity in terms of increased ...
TN4435	Licopyranocoumarin	Licopyranocoumarin could as a potent neuroprotective drug via markedly blocked MPP+-induced neuronal PC12D cell death and disappearance of mitochondrial membran...
TN4800	Pisatin	Pisatin is an isoflavonoid phytoalexin synthesized by pea (Pisum sativum L.).
TN4928	Rutacridone	Rutacridone has mutagenicity.
TN5278	Zederone	Zederone has anti-bacterial activity,it inhibits gram-positive bacteria activity. Zederone induces hepatotoxicity implicated the induction of Cyps, which leads ...
TQ0109	(-)-Cephaeline dihydrochloride	(-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM).
TQ0191	Dihydromethysticin	Dihydromethysticin is one kavalactone found in Piper methysticum. It has marked activity on the induction of CYP3A23.
TQ0217	Gomisin G	Gomisin G is a natural compound and exhibits potent anti-HIV activity (EC50: 0.006 μg/mL; therapeutic index: 300). It is a good substrate of CYP2C9.
TQ0276	Methysticin	Methysticin, a major kavalactone extracted from kava, can induce CYP1A1.
TQ0296	N-Nornuciferine	N-Nornuciferine, an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).