| Identification | Back Directory | [Name]
(3S,3'S)-4,4'-disulfanediylbis(3-aMinobutane-1-sulfonic acid) | [CAS]
648927-86-0 | [Synonyms]
RB 150
QGC-001
RB150 RB 150
Firibastat 648927-86-0
1-Butanesulfonic acid, 4,4'-dithiobis[3-amino-, (3S,3'S)-
(3S,3'S)-4,4'-disulfanediylbis(3-aMinobutane-1-sulfonic acid) | [Molecular Formula]
C8H20N2O6S4 | [MDL Number]
MFCD20921962 | [MOL File]
648927-86-0.mol | [Molecular Weight]
368.51 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
H2O: 2 mg/mL, clear (Warmed) | [form ]
Solid | [color ]
White to off-white | [Water Solubility ]
Water : 41.67 mg/mL (113.08 mM; ultrasonic and warming and heat to 60°C) |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Firibast at (RB150; QGC001) is an orally activeblood-brain barrier-permeant prodrug composed of two molecules of disulfide-linked aminopeptidase A (APA; glutamyl aminopeptidase) active-site inhibitor EC33 (Ki = 300 nM) th at are released via the action of brain reductase in the brain. Firibast at exhibits antihypertensive efficacy in vivo (Blood pressure reduction ED50 = 30 mg/kg via p.o. in spontaneously hypertensive rats). | [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]. | 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).
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| [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. DOI:10.1161/CIRCULATIONAHA.119.040070
[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. DOI:10.1007/s11906-019-0957-4 |
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Lynnchem
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Novachemistry
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https://www.novachemistry.com/ |
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