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Firibastat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Firibastat图片
CAS NO:648927-86-0
包装与价格:
包装价格(元)
10mM (in 1mL Water)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Firibastat (QGC001) 是一种口服活性的 EC33 前体药物。Firibastat 是一种首创的脑氨基肽酶 A (APA) 抑制剂 (Ki=200 nM),选择性和特异性地抑制高血压大鼠脑血管紧张素 II 转化为血管紧张素 III,并降低血压。
Cas No.648927-86-0
别名QGC001; RB150
分子式C8H20N2O6S4
分子量368.51
溶解度Water : 41.67 mg/mL (113.08 mM; ultrasonic and warming and heat to 60°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats[1][2].

When given orally, Firibastat (0.1-30 mg/kg; p.o.) crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats[2].

[1]. Ferdinand KC, et al. Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins. Circulation. 2019;140(2):138-146.
[2]. Keck M, et al. Orally Active Aminopeptidase A Inhibitor Prodrugs: Current State and Future Directions. Curr Hypertens Rep. 2019;21(7):50. Published 2019 May 21.