FiribaSTAT 是一种具有口服活性的 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),选择性地抑制高血压大鼠脑血管紧张素 II 转化为血管紧张素 III,降低血压。
产品描述
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[1][2].
体内活性
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[2].
Cas No.
648927-86-0
分子式
C8H20N2O6S4
分子量
368.51
别名
QGC 001;QGC001;QGC-001;RB-150;RB 150;RB150
储存和溶解度
H2O:30mg/mL (81.41mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years