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

Chemical Structure : Rimegepant

CAS No.: 1289023-67-1

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Rimegepant (BMS-927711, BMS 927711)

货号: PC-21792Not For Human Use, Lab Use Only.

Rimegepant (BMS-927711) is a potent, selective and orally active calcitonin gene-related peptide (CGRP) antagonist with Ki of 0.027 nM, inhibits CGRP-stimulated cAMP production in SK-N-MC cells with EC50 of 0.14 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Rimegepant (BMS-927711) is a potent, selective and orally active calcitonin gene-related peptide (CGRP) antagonist with Ki of 0.027 nM, inhibits CGRP-stimulated cAMP production in SK-N-MC cells with EC50 of 0.14 nM.
Rimegepant (BMS-927711) shows no significant potential for off-target liabilities in a panel of 45 receptor and ion channel binding and enzyme activity assays.
Rimegepant (BMS-927711) inhibits hαCGRP-induced increases in marmoset facial blood flow upon subcutaneous (SC) dosing.
Rimegepant (BMS-927711) shows good metabolic stability, acceptable CYP inhibition profile, good animal PK, and a favorable predictive toxicological profile.

物理化学性质&存储条件

分子量 534.57
分子式 C28H28F2N6O3
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

[(5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl] 4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate

参考文献

1. Luo G, et al. J Med Chem. 2012 Dec 13;55(23):10644-51.

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