Firibastat

Research use only, not for human use.

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 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.

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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

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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

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(-20℃)

With Ice Pack

≥ 2 years