Cytochrome P-450 Inhibitors and Inducers

1-Aminobenzotriazole
A suicide substrate for cytochrome P-450 and chloroperoxidase, shown to inhibit oxidative drug metabolism in vivo and block ω-oxidation of arachidonic acid but not epoxidation.
Katalog # CAS Nummer Summenformel Menge
sc-200600 1614-12-6 C₆H₆N₄ 20 mg/100 mg
(±)11(12)-EET
Biosynthesized in rat and rabbit liver microsomes by CYP450. Has been shown, along with (±)8(9)-EET, to play a role in the recovery of depleted Ca²⁺ pools in cultured smooth muscle cells.
Katalog # CAS Nummer Summenformel Menge
sc-220579 81276-02-0 C₂₀H₃₂O₃ 25 µg/50 µg
(±)14(15)-EET
Biosynthesized in rat and rabbit liver microsomes by CYP450.1,2 Dramatic increases in urinary (±)14,15-DiHETrE, which is a (±)14(15)-EET metabolite, have been documented by GC/MS in pregnancy induced hypertension.3
Katalog # CAS Nummer Summenformel Menge
sc-220610 n.n. C₂₀H₃₂O₃ 25 µg/50 µg
(±)14(15)-EET Ethanolamide
An endogenous lipid neurotransmitter with cannabinergic activity, binding to both the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. Fatty acid amide hydrolase (FAAH) is the enzyme responsible for the hydrolysis and inactivation of AEA. Metabolism of AEA by cyclooxygenase-2, leading to formation of prostaglandin ethanolamides and by lipoxygenases has also been documented. (±)14(15)-EET ethanolamide is a potential cytochrome P450 (CYP450) metabolite of AEA, although specific stereochemistry rather than a racemic mixture would likely ensue from enzymatic metabolism. CYP450 metabolism of AEA may be particularly relevant under conditions of FAAH inhibition. Evidence for the formation of (±)14(15)-EET ethanolamide in vivo has not been documented.
Katalog # CAS Nummer Summenformel Menge
sc-220611 n.n. C₂₂H₃₇NO₃ 25 µg/50 µg
16(17)-EpDPE
An unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as 14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) have been little studied relative to arachidonate epoxygenase metabolites. Is the DHA homolog of 14(15)-EpETrE, derived via epoxidation of the 16,17-double bond of docosahexaenoic acid (DHA). The EDHF activity of 16(17)-EpDPE has not yet been determined and the epoxygenase metabolites of DHA have also been detected in a murine inflammation model.
Katalog # CAS Nummer Summenformel Menge
sc-220642 n.n. C₂₂H₃₂O₃ 25 µg/50 µg
2,3-dihydrothieno-Thiadiazole Carboxylate
1,2,3-Thiadiazoles are used in agriculture and medicine applications, such as bactericides, fungicides, and antiviral agents. 2,3-dihydrothieno-Thiadiazole carboxylate (MTCC), 100 µM, inactivates and inhibits certain microsomal CYP450 enzymes (CYP2E1 and CYP2B4), but not others (CYP1A2), with inactivation occurring in a mechanism-based manner.
Katalog # CAS Nummer Summenformel Menge
sc-220770 n.n. C₆H₄N₂O₂S₂ 50 mg/100 mg
4,5-diphenyl-1,2,3-Thiadiazole
Has diverse applications in medicine and agriculture, including as bactericides, fungicides, and antiviral agents. At 100 μM, an inhibitor of some CYP450 enzymes (CYP2B4, CYP1A2), but not others (CYP2E1), with inhibition occurring in a mechanism-based manner.
Katalog # CAS Nummer Summenformel Menge
sc-205127 5393-99-7 C₁₄H₁₀N₂S 250 mg/500 mg
6',7'-dihydroxy Bergamottin
A potent inhibitor of CYP3A4; appears to be the primary compound in grapefruit juice that is responsible for inhibition of testosterone 6β-hydrolase activity.
Katalog # CAS Nummer Summenformel Menge
sc-205162 145414-76-2 C₂₁H₂₄O₆ 1 mg/10 mg
7-Ethoxyresorufin
Fluorimetric substrate and suicide inhibitor for cytochrome P450, nitric oxide synthesis inhibitor, NADPH-P450 inhibitor, with demonstrated inhibition of vasorelaxant responses to acetylcholine.
Katalog # CAS Nummer Summenformel Menge
sc-200606 5725-91-7 C₁₄H₁₁NO₃ 2 mg/10 mg
Benzylimidazole
Found to induce various cytochrome P-450 isozymes and to inhibit thromboxane A₂ synthase.
Katalog # CAS Nummer Summenformel Menge
sc-200530 4238-71-5 C₁₀H₁₀N₂ 1 g/5 g
β-Naphthoflavone
Cytochrome P450 enzyme system inducer. Protects chemical-induced carcinogenesis by enhancing the detoxification of carcinogens.
Katalog # CAS Nummer Summenformel Menge
sc-205597 6051-87-2 C₁₉H₁₂O₂ 1 g/5 g
Clofibrate
A ligand agonist for peroxisome proliferator-activated receptor α (PPARα) and influences expression of cytochromes P450IVA1 and IVA3 in studies with rat liver.
Katalog # CAS Nummer Summenformel Menge
sc-200721 637-07-0 C₁₂H₁₅ClO₃ 1 g
Feprazone
A non-steroidal, anti-inflammatory compound reported to induce the cytochrome P-450 II B family of cytochromes.
Katalog # CAS Nummer Summenformel Menge
sc-279162 30748-29-9 C₂₀H₂₀N₂O₂ 200 mg
Furafylline
A methyl xanthine derivative with an expanded duration of action than theophylline and it is an inhibitor of cytochrome P4501A2.
Katalog # CAS Nummer Summenformel Menge
sc-215061 80288-49-9 C₁₂H₁₂N₄O₃ 5 mg
HET-0016
A potent and selective inhibitor of the biosynthesis of 20-HETE in human renal microsomes with an IC₅₀ of 8.9 nM, selectively inhibiting CYP4A and 4F isoforms.
Katalog # CAS Nummer Summenformel Menge
sc-200673 339068-25-6 C₁₂H₁₈N₂O 5 mg/25 mg
Ketoconazole
An inhibitor of thromboxane synthetase and 5-lipoxygenase. Suppresses 5-lipoxygenase-mediated production of leukotrienes. Reduces production of thromboxane A₂. Inhibits adrenocorticoid biosynthesis.
Katalog # CAS Nummer Summenformel Menge
sc-200496 65277-42-1 C₂₆H₂₈Cl₂N₄O₄ 50 mg/500 mg
Methoxsalen (8-Methoxypsoralen)
A potent tricyclic fumocoumarin suicide inhibitor of cytochrome P-450.
Katalog # CAS Nummer Summenformel Menge
sc-200505 298-81-7 C₁₂H₈O₄ 1 g
Metyrapone
Inhibits the biosynthesis of corticosteroid. Reported to rapidly oxidize endogenous NADPH, improve oxidation of cortisol, and inhibit the reduction of cortisone.
Katalog # CAS Nummer Summenformel Menge
sc-200597 54-36-4 C₁₄H₁₄N₂O 200 mg
MS-PPOH
A selective inhibitor of the epoxygenation reactions catalyzed by specific CYP450 isozymes.
Katalog # CAS Nummer Summenformel Menge
sc-205392 206052-02-0 C₁₆H₂₁NO₄S 1 mg/5 mg
Muscone
Has been shown to induce CYP4F3 and contain antiinflammatory effects by reducing proinflammatory cytokines. Also reported to be weakly estrogenically active in vitro.
Katalog # CAS Nummer Summenformel Menge
sc-200528 541-91-3 C₁₆H₃₀O 100 mg/500 mg
Naringenin-4'-O-beta-D-Glucuronide
Naringenin is a flavanone. Naringenin-4'-O-β-D-Glucuronide is the metabolite of the flavonoid naringin, which has been shown to have an inhibitory effect on the human cytochrome P450 isoform CYP1A2.
Katalog # CAS Nummer Summenformel Menge
sc-295905 158196-35-1 C₂₁H₂₀O₁₁ 100 µg/500 µg
Rutaecarpine
An alkaloid isolated from the chinese herb Evodia rutaecarpa which has vasorelaxing effect andinhibits platelet aggregation and COX-2. This compound is a selective inhibitor of cytochrome P450 1A.
Katalog # CAS Nummer Summenformel Menge
sc-205846 84-26-4 C₁₈H₁₃N₃O 10 mg/25 mg
SKF-525A HCl (Proadifen)
Exhibits a wide array of activity, including: inhibition of NOS1, AChR, CYP4, transmembrane Ca²⁺ influx, and platelet thromboxane synthesis, as well as blockage of KIR6.1, and stimulation of endothelial cell prostacyclin production.
Katalog # CAS Nummer Summenformel Menge
sc-200492 62-68-0 C₂₃H₃₂ClNO₂ 250 mg/1 g
YM 511
Katalog # CAS Nummer Summenformel Menge
sc-361413 148869-05-0 C₁₆H₁₂BrN₅ 10 mg/50 mg