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Chemical Structure : BMS-694153
Catalog No.: 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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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.
| M.Wt | 644.80 | |
| Formula | C35H45FN8O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Andrew P. Degnan, et al. Journal of Medicinal Chemistry 2008, 51, 16, 4858-4861.
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