BQ-788 sodium salt

Chemical Structure : BQ-788 sodium salt

CAS No.: 156161-89-6

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货号: PC-23821Not For Human Use, Lab Use Only.

规格	价格	库存
1 mg	￥1280	In stock
5 mg	￥2780	In stock
10 mg	￥4580	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

BQ-788 sodium salt is a potent, selective endothelin-B receptor (ETB) antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, >1000-fold selective over ETA receptor.
BQ-788 poorly inhibits the binding to ETA receptors on human neuroblastoma cell line SK-N-MC cells (IC50, 1300 nM).
BQ-788 shows no agonist activity up to 10 microM in isolated rabbit pulmonary arteries.
BQ-788 competitively antagonizes the vasoconstriction induced by an ETB-selective agonist, BQ-3020 (pA2, 8.4).
BQ-788 (1 mg/kg, i.v.) abolishes the depressor response, resulting in a rapid onset of apparently enhanced pressor response in rats.

物理化学性质&存储条件

分子量	663.79
分子式	C34H50N5NaO7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Sodium (R)-2-((R)-2-((S)-2-((2R,6S)-2,6-dimethylpiperidine-1-carboxamido)-4,4-dimethylpentanamido)-3-(1-(methoxycarbonyl)-1H-indol-3-yl)propanamido)hexanoate

参考文献

1. Fukuroda T, et al. Biochem Biophys Res Commun. 1994 Mar 30;199(3):1461-5.

2. Ishikawa K, et al. Proc Natl Acad Sci U S A. 1994 May 24;91(11):4892-6.