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MedKoo Cat#: 529017 | Name: Firibastat
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Firibastat, also known as QGC-001 and RB-150, is a glutamyl aminopeptidase antagonist potentially for the treatment of hypertension. Firibastat is an orally active prodrug of the specific and selective APA inhibitor, EC33.

Chemical Structure

Firibastat
Firibastat
CAS#648927-86-0 (free)

Theoretical Analysis

MedKoo Cat#: 529017

Name: Firibastat

CAS#: 648927-86-0 (free)

Chemical Formula: C8H20N2O6S4

Exact Mass: 368.0204

Molecular Weight: 368.49

Elemental Analysis: C, 26.08; H, 5.47; N, 7.60; O, 26.05; S, 34.80

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 330.00 Ready to ship
50mg USD 490.00 Ready to ship
100mg USD 850.00 Ready to ship
200mg USD 1,530.00 Ready to ship
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Related CAS #
648927-86-0 (free) 648927-86-0 (3hydrate) 1601301-47-6 (disodium)
Synonym
RB-150; RB150 RB 150; QGC 001; QGC 001; QGC001; Firibastat;
IUPAC/Chemical Name
(S)-3-amino-4-(((S)-2-amino-4-sulfobutyl)disulfaneyl)butane-1-sulfonic acid
InChi Key
HJPXZXVKLGEMGP-YUMQZZPRSA-N
InChi Code
InChI=1S/C8H20N2O6S4/c9-7(1-3-19(11,12)13)5-17-18-6-8(10)2-4-20(14,15)16/h7-8H,1-6,9-10H2,(H,11,12,13)(H,14,15,16)/t7-,8-/m0/s1
SMILES Code
O=S(CC[C@H](N)CSSC[C@@H](N)CCS(=O)(O)=O)(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Firibastat is a brain APA inhibitor (Ki=200 nM). When given orally, firibastat 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.
In vitro activity:
To be determined
In vivo activity:
In conscious hypertensive deoxycorticosterone acetate (DOCA)-salt rats, treatment with tritherapy with firibastat, enalapril and hydrochlorothiazide improves blood pressure control and arginine-vasopressin release in an experimental salt-dependent model of hypertension, indicating the development of new treatments for patients with currently difficult-to-treat or resistant hypertension. Reference: Biomed Pharmacother. 2021 Aug;140:111682. https://pubmed.ncbi.nlm.nih.gov/34020248/
Solvent mg/mL mM
Solubility
Water 33.3 90.45
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 368.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Marc Y, Hmazzou R, De Mota N, Balavoine F, Llorens-Cortes C. Effects of firibastat in combination with enalapril and hydrochlorothiazide on blood pressure and vasopressin release in hypertensive DOCA-salt rats. Biomed Pharmacother. 2021 Aug;140:111682. doi: 10.1016/j.biopha.2021.111682. Epub 2021 May 19. PMID: 34020248. 2. Alomar SA, Alghabban SA, Alharbi HA, Almoqati MF, Alduraibi Y, Abu-Zaid A. Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials. Avicenna J Med. 2021 Jan 5;11(1):1-7. doi: 10.4103/ajm.ajm_117_20. PMID: 33520782; PMCID: PMC7839263.
In vitro protocol:
To be determined
In vivo protocol:
1. Marc Y, Hmazzou R, De Mota N, Balavoine F, Llorens-Cortes C. Effects of firibastat in combination with enalapril and hydrochlorothiazide on blood pressure and vasopressin release in hypertensive DOCA-salt rats. Biomed Pharmacother. 2021 Aug;140:111682. doi: 10.1016/j.biopha.2021.111682. Epub 2021 May 19. PMID: 34020248. 2. Alomar SA, Alghabban SA, Alharbi HA, Almoqati MF, Alduraibi Y, Abu-Zaid A. Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials. Avicenna J Med. 2021 Jan 5;11(1):1-7. doi: 10.4103/ajm.ajm_117_20. PMID: 33520782; PMCID: PMC7839263.
1: Nesbitt SD. Firibastat: a Novel Treatment for Hypertension. Curr Hypertens Rep. 2021 Dec 24;23(12):46. doi: 10.1007/s11906-021-01163-4. PMID: 34950965. 2: Croasdell G. European Society of Cardiology (ESC) Congress 2021 (August 27-30, 2021 - Virtual Meeting). Drugs Today (Barc). 2021 Oct;57(10):639-643. doi: 10.1358/dot.2021.57.10.3365971. PMID: 34713872. 3: Marc Y, Hmazzou R, De Mota N, Balavoine F, Llorens-Cortes C. Effects of firibastat in combination with enalapril and hydrochlorothiazide on blood pressure and vasopressin release in hypertensive DOCA-salt rats. Biomed Pharmacother. 2021 Aug;140:111682. doi: 10.1016/j.biopha.2021.111682. Epub 2021 May 19. PMID: 34020248. 4: Gupta R, Alcantara R, Popli T, Tariq U, Sood A, Mahajan S, Ayele H, Rajeswaran Y, Vyas AV. Firibastat: A Novel Brain Aminopeptidase Inhibitor - A New Era of Antihypertensive therapy. Curr Probl Cardiol. 2021 Apr 3:100859. doi: 10.1016/j.cpcardiol.2021.100859. Epub ahead of print. PMID: 33994025. 5: Hmazzou R, Marc Y, Flahault A, Gerbier R, De Mota N, Llorens-Cortes C. Brain ACE2 activation following brain aminopeptidase A blockade by firibastat in salt- dependent hypertension. Clin Sci (Lond). 2021 Mar 26;135(6):775-791. doi: 10.1042/CS20201385. PMID: 33683322. 6: Alomar SA, Alghabban SA, Alharbi HA, Almoqati MF, Alduraibi Y, Abu-Zaid A. Firibastat, the first-in-class brain aminopeptidase a inhibitor, in the management of hypertension: A review of clinical trials. Avicenna J Med. 2021 Jan 5;11(1):1-7. doi: 10.4103/ajm.ajm_117_20. PMID: 33520782; PMCID: PMC7839263. 7: Khosla J, Aronow WS, Frishman WH. Firibastat: An Oral First-in-Class Brain Aminopeptidase A Inhibitor for Systemic Hypertension. Cardiol Rev. 2022 Jan-Feb 01;30(1):50-55. doi: 10.1097/CRD.0000000000000360. PMID: 33027067. 8: Couvineau P, De Almeida H, Leroux V, Roques B, Maigret B, Llorens-Cortes C, Iturrioz X. Structural insight into the catalytic mechanism and inhibitor binding of aminopeptidase A. Biochem J. 2020 Nov 13;477(21):4133-4148. doi: 10.1042/BCJ20200307. PMID: 32955085. 9: Marc Y, Boitard SE, Balavoine F, Azizi M, Llorens-Cortes C. Targeting Brain Aminopeptidase A: A New Strategy for the Treatment of Hypertension and Heart Failure. Can J Cardiol. 2020 May;36(5):721-731. doi: 10.1016/j.cjca.2020.03.005. Epub 2020 Mar 6. PMID: 32389345. 10: Aronow WS. Approaches for the Management of Resistant Hypertension in 2020. Curr Hypertens Rep. 2020 Jan 8;22(1):3. doi: 10.1007/s11906-019-1013-0. PMID: 31916065. 11: Llorens-Cortes C, Touyz RM. Evolution of a New Class of Antihypertensive Drugs: Targeting the Brain Renin-Angiotensin System. Hypertension. 2020 Jan;75(1):6-15. doi: 10.1161/HYPERTENSIONAHA.119.12675. Epub 2019 Dec 2. PMID: 31786978. 12: Keck M, Hmazzou R, Llorens-Cortes C. Orally Active Aminopeptidase A Inhibitor Prodrugs: Current State and Future Directions. Curr Hypertens Rep. 2019 May 21;21(7):50. doi: 10.1007/s11906-019-0957-4. PMID: 31115779. 13: Keck M, De Almeida H, Compère D, Inguimbert N, Flahault A, Balavoine F, Roques B, Llorens-Cortes C. NI956/QGC006, a Potent Orally Active, Brain- Penetrating Aminopeptidase A Inhibitor for Treating Hypertension. Hypertension. 2019 Jun;73(6):1300-1307. doi: 10.1161/HYPERTENSIONAHA.118.12499. PMID: 31067198. 14: Ferdinand KC, Balavoine F, Besse B, Black HR, Desbrandes S, Dittrich HC, Nesbitt SD. Efficacy and Safety of Firibastat, A First-in-Class Brain Aminopeptidase A Inhibitor, in Hypertensive Overweight Patients of Multiple Ethnic Origins. Circulation. 2019 Jul 9;140(2):138-146. doi: 10.1161/CIRCULATIONAHA.119.040070. Epub 2019 Apr 24. PMID: 31014072. 15: Azizi M, Courand PY, Denolle T, Delsart P, Zhygalina V, Amar L, Lantelme P, Mounier-Vehier C, De Mota N, Balavoine F, Llorens-Cortes C. A pilot double-blind randomized placebo-controlled crossover pharmacodynamic study of the centrally active aminopeptidase A inhibitor, firibastat, in hypertension. J Hypertens. 2019 Aug;37(8):1722-1728. doi: 10.1097/HJH.0000000000002092. PMID: 30882604. 16: Boitard SE, Marc Y, Keck M, Mougenot N, Agbulut O, Balavoine F, Llorens- Cortes C. Brain renin-angiotensin system blockade with orally active aminopeptidase A inhibitor prevents cardiac dysfunction after myocardial infarction in mice. J Mol Cell Cardiol. 2019 Feb;127:215-222. doi: 10.1016/j.yjmcc.2018.12.008. Epub 2018 Dec 30. PMID: 30599150. 17: Leenen FHH, Ahmad M, Marc Y, Llorens-Cortes C. Specific Inhibition of Brain Angiotensin III Formation as a New Strategy for Prevention of Heart Failure After Myocardial Infarction. J Cardiovasc Pharmacol. 2019 Feb;73(2):82-91. doi: 10.1097/FJC.0000000000000638. PMID: 30531435. 18: Marc Y, Hmazzou R, Balavoine F, Flahault A, Llorens-Cortes C. Central antihypertensive effects of chronic treatment with RB150: an orally active aminopeptidase A inhibitor in deoxycorticosterone acetate-salt rats. J Hypertens. 2018 Mar;36(3):641-650. doi: 10.1097/HJH.0000000000001563. PMID: 28968260. 19: Gao J, Marc Y, Iturrioz X, Leroux V, Balavoine F, Llorens-Cortes C. A new strategy for treating hypertension by blocking the activity of the brain renin- angiotensin system with aminopeptidase A inhibitors. Clin Sci (Lond). 2014 Aug;127(3):135-48. doi: 10.1042/CS20130396. PMID: 24697296. 20: Balavoine F, Azizi M, Bergerot D, De Mota N, Patouret R, Roques BP, Llorens- Cortes C. Randomised, double-blind, placebo-controlled, dose-escalating phase I study of QGC001, a centrally acting aminopeptidase a inhibitor prodrug. Clin Pharmacokinet. 2014 Apr;53(4):385-95. doi: 10.1007/s40262-013-0125-y. PMID: 24337978.