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首页-小分子抑制剂&激动剂-GPCR-Urotensin Receptor-SB-706375
SB-706375

Chemical Structure : SB-706375

CAS No.: 733734-61-7

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SB-706375 (SB706375)

货号: PC-28274Not For Human Use, Lab Use Only.

SB-706375 is a potent, selective nonpeptidic urotensin-II receptor (U-II) antagonist, potently inhibits [(125)I]hU-II binding to both mammalian recombinant UT receptors (Ki=4.7-20.7 nM at rodent, feline and primate recombinant UT receptors) and Ki 5.4 nM at the endogenous UT receptor in SJRH30 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SB-706375 is a potent, selective nonpeptidic urotensin-II receptor (U-II) antagonist, potently inhibits [(125)I]hU-II binding to both mammalian recombinant UT receptors (Ki=4.7-20.7 nM at rodent, feline and primate recombinant UT receptors) and Ki 5.4 nM at the endogenous UT receptor in SJRH30 cells.
SB-706375 is a potent, competitive hU-II antagonist across species with pK(b) 7.29-8.00 in HEK293-UT receptor cells (inhibition of [Ca(2+)](i)-mobilization) and pK(b) 7.47 in rat isolated aorta (inhibition of contraction).
SB-706375 also reversed tone established in the rat aorta by prior exposure to hU-II (K(app) approximately 20 nM).

物理化学性质&存储条件

分子量 539.36
分子式 C20H22BrF3N2O5S
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

(R)-2-Bromo-4,5-dimethoxy-N-(3-((1-methylpyrrolidin-3-yl)oxy)-4-(trifluoromethyl)phenyl)benzenesulfonamide

参考文献

1. Douglas SA, et al. Br J Pharmacol. 2005 Jul;145(5):620-35.

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