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首页-小分子抑制剂&激动剂-GPCR-CGRP Receptor-BMS-694153
BMS-694153

Chemical Structure : BMS-694153

CAS No.: 1050381-35-5

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BMS-694153 (BMS 694153)

货号: PC-21156Not For Human Use, Lab Use Only.

BMS-694153 is a potent, selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 0.013 nM for hCGRP (inhibition of 125I-CGRP binding in SK-N-MC cell membranes).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BMS-694153 is a potent, selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 0.013 nM for hCGRP (inhibition of 125I-CGRP binding in SK-N-MC cell membranes).
BMS-694153 is a full, competitive antagonist, potently inhibits CGRP-stimulated cAMP production in SK-N-MC cells with EC50 of 0.0345 nM.
BMS-694153 show species-specific differences with relatively poor activity against nonprimate receptors, shows no inhibition of CGRP binding to the rat receptor at 1 uM.
BMS-694153 displays >10000-fold selectivity for CGRP over adrenomedullin receptors 1 and 2, calcitonin, and amylin receptors 1 and 3.
BMS-694153 shows no significant potential for off-target liabilities in a broad panel of receptor and ion channel binding and enzyme activity assays.
BMS-694153 potently reverses CGRP-induced dilation with EC50 of 0.06 nM in ex vivo human intracranial arteries.
BMS-694153 has good intranasal bioavailablity in rabbits and shows dose-dependent activity in validated in vivo and ex vivo migraine models.

物理化学性质&存储条件

分子量 644.80
分子式 C35H45FN8O3
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)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide

参考文献

1. Andrew P. Degnan, et al. Journal of Medicinal Chemistry  2008, 51, 16, 4858-4861.

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