[CAS NO. 648927-86-0] Firibastat
PRODUCTS SPECIFICATIONS [648927-86-0]
DESCRIPTION [648927-86-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 368.51 |
| Molecular Formula | C8H20N2O6S4 |
| SMILES | O=S(CC[C@H](N)CSSC[C@@H](N)CCS(=O)(O)=O)(O)=O |
Summary
Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor ( K i =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). |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04277884 | Quantum Genomics SA |
Hypertension
|
June 25, 2020 | Phase 3 |
| NCT02322450 | Quantum Genomics SA |
Essential Hypertension
|
January 2015 | Phase 2 |
| NCT02780180 | Quantum Genomics SA |
Heart Failure
|
June 2016 | Phase 2 |
| NCT03198793 | Quantum Genomics SA |
Hypertension
|
October 13, 2017 | Phase 2 |
| NCT03714685 | Quantum Genomics SA|Quotient Sciences |
Healthy Males
|
February 15, 2019 | Phase 1 |
| NCT04792333 | Quantum Genomics SA|Eurofins Optimed |
Healthy Volunteers|Renal Failure
|
September 17, 2019 | Phase 1 |
| NCT03715998 | Quantum Genomics SA |
Myocardial Infarction
|
June 4, 2019 | Phase 2 |
| NCT04857840 | Quantum Genomics SA|PRA Health Sciences |
Hypertension (HTN)
|
August 5, 2021 | Phase 3 |
| NCT01900184 | Quantum Genomics SA |
Essential Hypertension
|
December 2012 | Phase 1 |
| NCT01900171 | Quantum Genomics SA |
Essential Hypertension
|
February 2012 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
H 2 O : 33.33 mg/mL ( 90.45 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7136 mL | 13.5682 mL | 27.1363 mL |
| 5 mM | 0.5427 mL | 2.7136 mL | 5.4273 mL |
| 10 mM | 0.2714 mL | 1.3568 mL | 2.7136 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (271.36 mM); Clear solution; Need ultrasonic
References
- [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.
