p-450

Cytochrome P450 2C9 is a cytochrome P-450 subtype that possesses specificity for acidic xenobiotics. It oxidizes a wide range of important clinical drugs under the categories of nonsteroidal anti-inflammatory agents, anticoagulants, hypoglycemic agents, a

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Tegafur (FT 207) is a congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme.

Voriconazole (UK-109496) is a triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 [CYP3A].

Sulconazole mononitrate (Exelderm) is the nitrate salt form of sulconazole, a synthetic imidazole derivative with the antifungal property. Sulconazole mononitrate inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols and inhibition of the synthesis of ergosterol, an important component of the fungal cell membrane. Inhibition of ergosterol synthesis leads to a disruption of cell membrane permeability, and ultimately inhibition of cell wall synthesis. In addition, Sulconazole mononitrate seems to interfere with the autolytic degradation of fungal DNA and RNA.

Diniconazole (Rac-diniconazole) is a fungicide. It is known as a plant hormone abscisic acid (ABA) catabolic inhibitor, and acts as a potent competitive inhibitor of recombinant Arabidopsis ABA 8'-hydroxylase, CYP707A3.

Proadifen hydrochloride (RP-5171) is an inhibitor of drug metabolism and cytochrome P-450 enzyme system activity.

Zoxazolamine (NSC-24995) is a uricosuric and muscle relaxant. Zoxazolamine acts centrally as a muscle relaxant, but the mechanism of its action is not understood.

Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can significantly increased the activities of epoxide hydrase and glutathione-S-transferase but cause reduc

Valganciclovir, the L-valyl ester of ganciclovir, is a prodrug effectively converted to ganciclovir in the body, serving as an antiviral medication for cytomegalovirus (CMV) infections. In vitro studies demonstrate that valganciclovir inhibits glycylsarcosine transport mediated by PEPT1 and PEPT2 in Caco-2 and SKPT cells, respectively, with competitive inhibition K(i) values of 1.68±0.30 mM for PEPT1 and 0.043±0.005 mM for PEPT2. Clinical trials indicate valganciclovir's non-inferior efficacy to ganciclovir in pre-emptive therapy for CMV, exhibiting no significant difference in viral clearance rates or toxicity levels between the treatments. Specifically, 89.5% of patients treated with valganciclovir and 83% treated with ganciclovir achieved viral clearance at 28 days (P=0.030 for non-inferiority). Additionally, valganciclovir prophylaxis at 450 mg twice daily prevented CMV reactivation in patients on an alemtuzumab-containing regimen, with none of the 20 patients experiencing reactivation (P=0.004).

LY 43578 is an orally active aromatase inhibitor. LY43578 could inhibit O-demethylation of P-450-dependent p-nitroanisole and N-demethylation of ethylmorphine (IC50 of 0.3 and 5 μm, respectively) in rat liver microsomes. LY 43578 can be used to study neurological and cardiovascular diseases.

5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450) and a metabolite of Xanthotoxin. It is used in the treatment of psoriasis, eczema, vitiligo, and certain cutaneous lymphomas in combination with phototherapy involving exposure to sunlight.

p,p'-DDMS is a water soluble and highly specific inhibitor of cytochrome P-450 omega-hydroxylase.

Lab 170250F is a potent cytochrome P-450-obtusifoliol-14-demethylase inhibitor.

Flumecinol is a hepatic enzyme (cytochrome P-450 monooxygenases) inducer.

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg/kg prior to occlusion or reperfusion.[5] Reference：[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO/BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).

RPR132595A (NPC) hydrochloride, an active metabolite of CPT-11, is produced via cytochrome P-450 3A4 (CYP3A4) metabolism and is ultimately eliminated via urinary excretion [1].

M 79193 induces total hepatic microsomal cytochrome P-450.

UK 39671 is an inhibitor of cytochrome P-450(CAM) inhibitor.

Buthiobate is a fungicide which inhibits lanosterol 14 alpha-demethylation catalyzed by a cytochrome P-450.

Dehydro warfarin, a metabolite of (±)-warfarin, is formed by rat liver microsomes from (±)-warfarin.

Nicotelline, also known as Nicotellin, is an alkaloid associated with nicotine and acts as a modest inhibitor of the enzyme human cDNA-expressed cytochrome P-450 2A6 (CYP2A6), which is responsible for coumarin 7-hydroxylation. However, Nicotelline does not show inhibitory effects at a concentration of 300 μM. It serves as a tracer and biomarker for particulate matter (PM) originating from tobacco smoke [1] [2].

Bisfentidine is an H2 receptor antagonist that blocks H2 receptors on gastric parietal cells to reduce gastric acid secretion. It binds to cytochrome P-450 in liver microsomes, affecting drug metabolism. Bisfentidine is utilized in research on drug metabolism processes, lipid peroxidation, and peptic ulcers.

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM, exhibiting antimalarial activity by inducing developmental arrest of malaria parasites at the schizont stage[1][2].

RPR132595A is an active CPT-11 metabolite, it is generated by cytochrome P-450 3A4 (CYP3A4).

Itraconazole-d5 is a deuterated compound of Itraconazole. Itraconazole has a CAS number of 84625-61-6. Itraconazole is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.

Voriconazole-d3 is a deuterated compound of Voriconazole. Voriconazole has a CAS number of 137234-62-9. Voriconazole is a triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.

Fadrozole hydrochloride (CGS 16949A) is a model aromatase inhibitor that effectively suppresses estrogen production in fish ovaries.

Cytochrome P450 CYP1B1 (190-198) [Homo sapiens] is a peptide from Cytochrome c, which is a small heme protein found loosely associated with the inner membrane of the mitochondrion. Cytochromes c from certain eukaryotes, including plants and fungi but not higher animals, contains methylated lysine residues at specific positions1. Cytochrome c is a required cofactor for Apaf-1 function2.