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- Aliskiren hemifumarate 173334-58-2

- Aliskiren hemifumarate 173334-58-2
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 ReninIn 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 regulationCardiovascularBloodOtherMetabolismPathways and ProcessesCofactors, Vitamins / mineralsVitamins / mineralsNeuroscienceProcessesSignal TransductionMetabolismVitamins / MineralsDrug DiscoverySmall Molecule DrugLead Compound DiscoveryAliskiren 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
