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SML3814

Sigma-Aldrich

Firibastat

≥98% (HPLC)

Synonym(s):

QGC-001, (3S)-3-Amino-4-[[(2S)-2-amino-4-sulfobutyl]disulfanyl]butane-1-sulfonic acid, (3S,3′S)-4,4′-Dithiobis(3-aminobutane-1-sulfonic acid, QGC 001, QGC001, RB 150, RB-150, RB150

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About This Item

Empirical Formula (Hill Notation):
C8H20N2O6S4
CAS Number:
648927-86-0
Molecular Weight:
368.51
MDL number:
MFCD20921962
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

Firibastat (RB150; QGC001) is an orally active, blood-brain barrier-permeant prodrug composed of two molecules of disulfide-linked aminopeptidase A (APA; glutamyl aminopeptidase) active-site inhibitor EC33 (Ki = 300 nM) that are released via the action of brain reductase in the brain. Firibastat exhibits antihypertensive efficacy in vivo (Blood pressure reduction ED50 = 30 mg/kg via p.o. in spontaneously hypertensive rats).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000255770
0000269512
0000269510

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Brain ACE2 activation following brain aminopeptidase A blockade by firibastat in salt-dependent hypertension
Clinical Science (London, England : 1979), 135(6), 775-791 (2021)
Orally active aminopeptidase A inhibitors reduce blood pressure: a new strategy for treating hypertension
Hypertension, 51(5), 1318-1325 (2008)
Aminopeptidase A contributes to biochemical, anatomical and cognitive defects in Alzheimer's disease (AD) mouse model and is increased at early stage in sporadic AD brain
Acta Neuropathologica, 141(6), 823-839 (2021)
Effects of firibastat in combination with enalapril and hydrochlorothiazide on blood pressure and vasopressin release in hypertensive DOCA-salt rats
Biomedicine and Pharmacotherapy, 40, 111682-111682 (2021)
Brain renin-angiotensin system blockade by systemically active aminopeptidase A inhibitors: a potential treatment of salt-dependent hypertension
Proceedings of the National Academy of Sciences of the USA, 101(20), 7775-7780 (2004)
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