Firibastat

Firibastat (QGC001), an orally active brain penetrating proagent 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].

Product Specifications

CAS Number

[648927-86-0]

Product Name Alternative

QGC001; RB150

UNSPSC

12352211

Hazard Statement

H302, H312, H315, H319, H332, H335

Target

Aminopeptidase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/firibastat.html

Concentration

10mM

Purity

98.0

Solubility

H2O : 25 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C8H20N2O6S4

Molecular Weight

368.51

Precautions

H302, H312, H315, H319, H332, H335

References & Citations

[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.