Firibastat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

QGC-001 是一种谷氨酰氨肽酶拮抗剂，也是一种口服活性的 EC33 脑穿透前药。它是一流的脑氨肽酶 A (APA) 抑制剂，Ki 为 200 nM。

QGC-001 is a glutamyl aminopeptidase antagonist and an orally active brain penetrating prodrug of EC33. It is a first-in-class brain aminopeptidase A (APA) inhibitor with a Ki of 200 nM. QGC-001 selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.(In Vivo):Oral administration of QGC-001(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.

——

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).

RB-150 | RB150 | QGC001 | RB 150 | QGC 001 | QGC-001

Metabolic Enzyme/Protease

Aminopeptidase

Nucleoside Antimetabolite/Analog

——

——

648927-86-0

368.5

C8H20N2O6S4

>98% (HPLC)

In Vitro:?H2O : 33.33 mg/mL (90.45 mM)

N[C@@H](CCS(O)(=O)=O)CSSC[C@@H](N)CCS(O)(=O)=O

——

(-20℃)

With Ice Pack

≥ 2 years