1. Metabolic Enzyme/Protease
  2. Aminopeptidase
  3. Firibastat

Firibastat (Synonyms: QGC001; RB150)

Cat. No.: HY-109058
Handling Instructions

Firibastat (QGC001), an orally active brain penetrating prodrug 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.

For research use only. We do not sell to patients.

Firibastat Chemical Structure

Firibastat Chemical Structure

CAS No. : 648927-86-0

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Description

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

In Vivo

When given orally, Firibastat (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Normotensive and hypertensive DOCA-salt rats[1]
Dosage: 0.1-30 mg/kg
Administration: P.o.
Result: Resulting in a dose-dependent decrease in mean arterial blood pressure (MABP).
Molecular Weight

368.51

Formula

C₈H₂₀N₂O₆S₄

CAS No.

648927-86-0

SMILES

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

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

FiribastatQGC001 RB150QGC 001QGC-001RB150RB 150RB-150Aminopeptidasefirst-in-classangiotensinbrainhypertensivebloodpressureInhibitorinhibitorinhibit

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Firibastat
Cat. No.:
HY-109058
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