SML3814
Firibastat
≥98% (HPLC)
别名:
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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关于此项目
经验公式（希尔记法）:
C8H20N2O6S4
化学文摘社编号:
分子量:
368.51
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
H2O: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
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).
Orally active, brain-permeant precursor of the aminopeptidase A (APA; glutamyl aminopeptidase) active-site inhibitor EC33 with antihypertensive efficacy in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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)
Orally active aminopeptidase A inhibitors reduce blood pressure: a new strategy for treating hypertension
Hypertension, 51(5), 1318-1325 (2008)
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)
Central antihypertensive effects of chronic treatment with RB150: an orally active aminopeptidase A inhibitor in deoxycorticosterone acetate-salt rats
Journal of Hypertension, 36(3), 641-650 (2018)
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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