产品名称

阿利克仑半富马酸盐(Aliskiren heMifuMarate)

一般描述

Aliskiren Hemifumarate(阿利克仑半富马酸盐) is an orally active nonpeptide renin inhibitor with antihypertensive activity.

别 称

(2S,4S,5S,7S)-N-(2-Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate

纯 度

≥98.0%(HPLC)

CAS   NO.

173334-58-2

分子式

C³²H⁵⁵N³O⁸

分子量

609.804

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

≥50mg/mL

l  生物学信息

生物活性/药理作用

Aliskiren Hemifumarate is an orally active nonpeptide renin inhibitor with antihypertensive activity. Aliskiren selectively binds to the S3 sub-pocket of renin, an enzyme in the renin-angiotensin-aldosterone system (RAAS) that is responsible for converting angiotensinogen to angiotensin I (AT I). By inhibiting the activity of renin, the conversion to AT I is prevented, which in turn prevents the conversion of AT I to AT II. This prevents arterial vasoconstriction by AT II and inhibits the production of aldosterone by AT II. As aldosterone causes re-uptake of sodium and water and eventually an increase in extracellular volume, aliskiren is able to prevent the effects that contribute to an increase in blood pressure.

l  包装与存储

包 装

100mg; 250mg; 1g

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov