Firibastat

SKU: orb1304935

Description

Firibastat (RB150) is an orally active, brain-penetrating prodrug of EC33 and a first-in-class aminopeptidase A (APA) inhibitor (Ki=200 nM). It selectively blocks the conversion of angiotensin-II to angiotensin-III in the brain, demonstrating antihypertensive effects in rodent models of hypertension and serving as a key research tool for studying the brain renin-angiotensin system.

Research Area

Metabolism Research

Key Properties

• CAS Number: 648927-86-0
• MW: 368.51
• Purity: 99.88%
• Formula: C₈H₂₀N₂O₆S₄
• SMILES: N[C@@H](CCS(O)(=O)=O)CSSC[C@@H](N)CCS(O)(=O)=O
• Target: Aminopeptidase
• Solubility: H2O:30 mg/mL (81.41 mM)

Bioactivity

• Target IC50:
  Aminopeptidase A:200 Nm(ki)
• 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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

QGC 001, QGC001, QGC-001, Inhibitor, inhibit, hypertensive, Firibastat, Aminopeptidase A, Aminopeptidase, angiotensin, brain, blood, RB150, RB-150, RB 150, pressure

Compound Identifiers

PubChem CID

24851355