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抑制剂 & 化合物

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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
	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
	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)
	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
	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 ...
T36920	16α-hydroxy Dehydroepiandrosterone
	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...
T36561	(3S)-hydroxy Quinidine
	(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...
T37064	6β-hydroxy Eplerenone
	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

PF-4981517

Cat.No: T21548

Synonym: CYP3cide

Target: P450

Dehydro Nifedipine

Cat.No: T36665

Synonym: BAY-b 4759

Target:

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

Synonym:

Target:

N-Desmethyl Sildenafil (citrate)

16α-hydroxy Dehydroepiandrosterone

Cat.No: T36920

Synonym:

Target:

(3S)-hydroxy Quinidine

Cat.No: T36561

Synonym:

Target:

6β-hydroxy Eplerenone

Cat.No: T37064

Synonym:

Target:

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

Cletoquine

Cat.No: T10835

Synonym: Desethylhydroxychloroquine

Target: Parasite, Antifection

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