Aliskiren hemifumarate 173334-58-2

简要描述：Aliskiren hemifumarate 173334-58-2
Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.

产品咨询联系我们

产品分类

Product Category

查看全部

详细介绍

Aliskiren hemifumarate 173334-58-2

产品描述
描述	Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.
纯度	96%
储存/保存方法	Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性	Soluble in DMSO
生物活性
靶点	Renin
In vitro(体外研究)	Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans.
In vivo(体内研究)	Aliskiren hemifumarate ( Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension.
参考文献
参考文献	1. Nakamura Y, et al. ACS Med Chem Lett, 2012, 3(9), 754–758. 2. Buczko W, et al. Pharmacol Rep, 2008, 60(5), 623-631. 3. Wood JM, et al. Biochem Biophys Res Commun, 2003, 308(4), 698-705.

研究领域
研究领域	CardiovascularBloodBlood Pressure regulation CardiovascularBloodOther MetabolismPathways and ProcessesCofactors, Vitamins / mineralsVitamins / minerals NeuroscienceProcesses Signal TransductionMetabolismVitamins / Minerals Drug DiscoverySmall Molecule DrugLead Compound Discovery

Aliskiren hemifumarate 173334-58-2温馨提示：本产品仅作科研实验使用，不支持临床等研究

产品咨询