Firibastat, 氨基肽酶 A 抑制剂

非利巴司他

Firibastat

F656797-1ml

1ml

10mM in Water

-80℃储存

超低温冰袋运输

Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor ( K i =200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Normotensive and hypertensive DOCA-salt rats Dosage: 0.1-30 mg/kg Administration: P.o. Result: Resulting in a dose-dependent decrease in mean arterial blood pressure (MABP).

菲瑞巴司他（QGC001）是一种口服活性脑穿透原药 EC33，是第一类脑氨肽酶 A（APA）抑制剂（K i =200 nM）。非利巴司他能选择性地特异抑制脑血管紧张素-II 向血管紧张素-III a 的转化。

648927-86-0(Water)

C8H20N2O6S4

368.51 g/mol

C(CS(=O)(=O)O)C(CSSCC(CCS(=O)(=O)O)N)N

抑制剂

氨基肽酶 A 抑制剂