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Search Results for " cyp3a5 "

Targets Recommended: P450

12

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21548	PF-4981517 CYP3cide	P450	Metabolism
	PF-4981517 (CYP3cide) 是一种高效，特异性和时间依赖性细胞色素P4503A4 (CYP3A4)抑制剂。对于CYP3A4，CYP3A5 和 CYP3A7，抑制CYP3A 活性的IC50值分别为 0.03 μM，17 μM 和 71μM。PF-4981517 可用于区分CYP3A4和 CYP3A5 对于药物代谢的作用。
T36665	Dehydro Nifedipine BAY-b 4759	Others	Others
	Dehydro Nifedipine (BAY-b 4759) 是人血浆中硝苯地平的主要代谢物。Dehydro Nifedipine 抑制PC-12细胞葡萄糖摄取，IC50值为130 μM，硝苯地平是一种钙通道阻滞剂，用于治疗高血压和心绞痛。当硝苯地平被细胞色素P450 (CYP)异构体CYP3A4和CYP3A5代谢时形成脱氢硝苯地平。
T1561	Clobetasol propionate Dermovate,Clobetasol 17-propionate,CGP9555,Temovate,丙酸氯倍他索,CCl 4725	Glucocorticoid Receptor; P450	Endocrinology/Hormones; Metabolism
	Clobetasol propionate (CGP9555) 是CYP3A5的选择性抑制剂(IC50:0.206 μM)，而对 CYP3A4 或其他主要 CYP 无抑制作用。它是皮质类固醇，对于牛皮癣和其他皮肤病具有潜在的研究价值。
T35714	N-Desethyl Vardenafil	Others	Others
	N-Desethyl vardenafil is a metabolite of vardenafil , a phosphodiesterase 5 inhibitor, that is formed by the action of cytochrome P450 (CYP)3A4 and CYP3A5.
T36062	N-Desmethyl Sildenafil (citrate)	Others	Others
	N-Desmethyl sildenafil is a major metabolite of sildenafil . N-Desmethyl sildenafil is formed via oxidative metabolism of sildenafil by the cytochrome (CYP) P450 isoforms CYP3A4, CYP3A5, and CYP3A7.
T36039	16α-Hydroxyestrone	Others	Others
	The naturally-occurring estrogens are estrone , estradiol , and estriol . 16α-hydroxy Estrone (16α-OHE1) is a hydroxylated metabolite of E1 as well as an interconversion product with E2. E1 is 16α-hydroxylated by cytochrome P450 (CYP) isoforms, including CYP1A1, CYP3A5, CYP3A4, and CYP3A7, with CYP3A5 being breast-specific. 16α-OHE1 is sulphatized or glucuronidated before excretion. It is increased in rheumatoid arthritis and decreased by physical activity. Unlike the parent estrogens and other ...
T84930	6β-hydroxy Prednisolone	Others	Others
	6β-Hydroxy Prednisolone, the active metabolite of prednisone and a derivative of prednisolone, is predominantly synthesized via the cytochrome P450 (CYP) isoform CYP3A4 and, to a lesser extent, CYP3A5.
T84531	6β-hydroxy Testosterone 4-Androsten-6β,17β-diol-3-one	Others	Others
	6β-Hydroxy Testosterone, primarily metabolized from testosterone by CYP3A4 and CYP3A5 enzymes, represents 75-80% of testosterone's metabolites. Both cytochrome P450 enzymes, induced by glucocorticoids and various xenobiotics (including drugs and chemical carcinogens), facilitate the metabolism of xenobiotics and certain endobiotics like steroid hormones. However, the biological effects of 6β-hydroxy testosterone remain poorly understood.
T36561	(3S)-hydroxy Quinidine	Others	Others
	(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-depe...
T84947	Desethoxy Quetiapine hydrochloride O-Desalkylquetiapine	Others	Others
	Desethoxy quetiapine, an active metabolite of the atypical antipsychotic quetiapine, primarily forms through the action of the cytochrome P450 (CYP) isoform CYP3A5. This compound binds to dopamine D2 receptors with an IC50 value of 1,330 nM. In vivo, desethoxy quetiapine at dosages of 20 and 40 mg/kg mitigates dopamine receptor agonist apomorphine-induced climbing behavior and ameliorates swimming deficits in mice, showcasing its potential modulatory effects on dopamine-mediated behaviors.
T36920	16α-hydroxy Dehydroepiandrosterone	Others	Others
	16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone .116α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosteronevia16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol .2 1.Miller, K.K.M., Cai, J., Ripp, S.L., et al.Stereo- and regioselectivity account for the diversity of dehydro...
T37064	6β-hydroxy Eplerenone	Others	Others
	6β-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone .1 It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4. \|1. Cook, C.S., Berry, L.M., Kim, D.H., et al. Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: Differential metabolism by CYP3A4 and CYP3A5. Drug Metab. Dispos. 30(12), 1344-1351 (2002).

化合物

Cat.No: T21548

Synonym: CYP3cide

Target: P450

Dehydro Nifedipine

Cat.No: T36665

Synonym: BAY-b 4759

Target: Others

Clobetasol propionate

Cat.No: T1561

Synonym: Dermovate,Clobetasol 17-propionate,CGP9555,Temovate,丙酸氯倍他索,CCl 4725

Target: Glucocorticoid Receptor, P450

N-Desethyl Vardenafil

Cat.No: T35714

Target: Others

N-Desmethyl Sildenafil (citrate)

Cat.No: T36062

Target: Others

16α-Hydroxyestrone

Cat.No: T36039

Target: Others

6β-hydroxy Prednisolone

Cat.No: T84930

Target: Others

6β-hydroxy Testosterone

Cat.No: T84531

Synonym: 4-Androsten-6β,17β-diol-3-one

Target: Others

(3S)-hydroxy Quinidine

Cat.No: T36561

Target: Others

Desethoxy Quetiapine hydrochloride

Cat.No: T84947

Synonym: O-Desalkylquetiapine

Target: Others

16α-hydroxy Dehydroepiandrosterone

Cat.No: T36920

Target: Others

6β-hydroxy Eplerenone

Cat.No: T37064

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T10835	Cletoquine Desethylhydroxychloroquine	Parasite; Antifection	Microbiology/Virology
	Cletoquine 是 Hydroxychloroquine 的主要活性代谢物。 Cletoquine 具有对抗基孔肯雅病毒 (CHIKV) 的能力。 Cletoquine 具有抗疟作用，并具有治疗自身免疫性疾病的潜力。

天然产物

Cat.No: T10835

Synonym: Desethylhydroxychloroquine

Target: Parasite, Antifection

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