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Metabolism P450

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...
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.
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 ...
T1274 Benzbromarone Uricosuric is an effective inhibitor of CYP2C9 used in the treatment of gout.
T1597 Proadifen hydrochloride Proadifen hydrochloride is an inhibitor of drug metabolism and cytochrome P-450 enzyme system activity.
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...
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...
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.
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.
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.
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...
T2S0663 Humantenmine 1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.
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...
T6S1894 Linderane 1. Linderane was characterized as a mechanism-based inactivator of CYP2C9.
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...
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...
T3768 Epifriedelanol Epifriedelanol suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can ...
T4S0800 Demethyleneberberine Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either...
T2945 Germacrone Germacrone, a major active component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antivirus activities. It also inhibits ...
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...
T6S0630 Hypaconitine Hypaconitine, an active and highly toxic constituent derived from Aconitum species, has anti-inflammatory activity, is widely used to treat rheumatism.
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...
T5786 TETRAHYDROPIPERINE TETRAHYDROPIPERINE is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.
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...
T5953 1-Aminobenzotriazole 1-Aminobenzotriazole (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.
Ticagrelor
T0179CAS 274693-27-5
Ticagrelor is an inhibitor of platelet aggregation. Unlike clopidogrel, ticagrelor is not a prodrug required metabolic activation.
Naringin
T0595CAS 10236-47-2
Naringin, a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibiti...
Beta-Tetralone
T0660CAS 530-93-8
Beta-Tetralone is a ketone derivative of tetralin.
Ketoconazole
T0679CAS 65277-42-1
Ketoconazole, a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
(-)-Sparteine sulfate pentahydrate
T0792CAS 6160-12-9
Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker. It can chelate the bivalents calcium and magnesium.
Ambroxol
T0920CAS 18683-91-5
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...
Itraconazole
T1011CAS 84625-61-6
Itraconazole is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
Fenofibrate
T1149CAS 49562-28-9
Fenofibrate is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic...
Bifonazole
T1187CAS 60628-96-8
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 ...
Benzbromarone
T1274CAS 3562-84-3
Uricosuric is an effective inhibitor of CYP2C9 used in the treatment of gout.
Proadifen hydrochloride
T1597CAS 62-68-0
Proadifen hydrochloride is an inhibitor of drug metabolism and cytochrome P-450 enzyme system activity.
Diosmetin
T1704CAS 520-34-3
Diosmetin has been found to act as a weak TrkB receptor agonist.
Bergapten
T2143CAS 484-20-8
Bergapten, a psoralen, inhibits cell replication.
Apigenin
T2175CAS 520-36-5
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...
Tauroursodeoxycholic Acid
T2532CAS 14605-22-2
Tauroursodeoxycholic acid is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans. Tauroursodeox...
Avasimibe
T2753CAS 166518-60-1
Avasimibe is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the ...
Naringenin
T2838CAS 480-41-1
Naringenin is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate m...
Sodium Danshensu
T2944CAS 67920-52-9
Danshensu (sodium salt) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstrictio...
Alizarin
T2949CAS 72-48-0
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...
Naloxegol oxalate
T3355CAS 1354744-91-4
Naloxegol oxalate is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.
Ginsenoside F1
T3401CAS 53963-43-2
Ginsenoside F1 is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of t...
Curdione
T3411CAS 13657-68-6
Curdione inhibits CYP3A4 activity and the production of prostaglandin E2. Curdione inhibits proliferation of MCF-7 cells by inducing apoptosis. Curdione may be ...
Amentoflavone
T3417CAS 1617-53-4
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 ...
TMS
T3585CAS 24144-92-1
TMS is a very selective and potent competitive inhibitor of P450 1B1 (CYP1A1).
Curcumenol
T3669CAS 19431-84-6
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...
alpha-Asarone
T3698CAS 2883-98-9
Alpha-Asarone is a psychoactive compound with antidepressant-like activity in mice.
Rhapontigenin
T3776CAS 500-65-2
Rhapontigenin is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic arom...
Isosilybin
T3797CAS 72581-71-6
Isosilybin and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.
Rosavin
T3886CAS 84954-92-7
Rosavin has antidepressant and anxiolytic actions, helps balance all the neurotransmitters.
SDZ285-428
T4188CAS 174262-13-6
NVP-VID-400 (SDZ285-428) is a CYP24A1 inhibitor.
XL388
T6030CAS 1251156-08-7
XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
Abiraterone Acetate
T6215CAS 154229-18-2
Abiraterone acetate is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic...
Abiraterone
T6216CAS 154229-19-3
Abiraterone (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17,20-lyase (CYP17) inhibitor (IC50: 4 nM).
Cobicistat
T6246CAS 1004316-88-4
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...
Galeterone
T6509CAS 851983-85-2
Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhib...
Humantenmine
T2S0663CAS 82354-38-9
1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.
Corydaline
T5S2360CAS 518-69-4
1. Corydaline, an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent. 2. Corydaline promotes gastric emptying a...
Linderane
T6S1894CAS 13476-25-0
1. Linderane was characterized as a mechanism-based inactivator of CYP2C9.
Stiripentol
T4498CAS 49763-96-4
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively)...
Sulfaphenazole
T4567CAS 526-08-9
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...
Difubenzuron
T7088CAS 35367-38-5
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...
Epifriedelanol
T3768CAS 16844-71-6
Epifriedelanol suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can ...
Demethyleneberberine
T4S0800CAS 25459-91-0
Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either...
Germacrone
T2945CAS 6902-91-6
Germacrone, a major active component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antivirus activities. It also inhibits ...
Phthalic Acid Monooctyl Ester
T0603CAS 4376-20-9
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...
Hypaconitine
T6S0630CAS 6900-87-4
Hypaconitine, an active and highly toxic constituent derived from Aconitum species, has anti-inflammatory activity, is widely used to treat rheumatism.
Cedrol
T5594CAS 77-53-2
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...
TETRAHYDROPIPERINE
T5786CAS 23434-88-0
TETRAHYDROPIPERINE is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.
FLAVOKAVAIN A(P)
T5715CAS 37951-13-6
FLAVOKAVAIN A(P), a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-depende...
1-Aminobenzotriazole
T5953CAS 1614-12-6
1-Aminobenzotriazole (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.