MK-0974 |CAS:781649-09-0 Probechem Biochemicals

Chemical Structure : MK-0974

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MK-0974 (Telcagepant, MK0974)

货号: PC-45811Not For Human Use, Lab Use Only.

Telcagepant (MK-0974) is a potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM.

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生物&药学活性

Telcagepant (MK-0974) is a potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM.
Telcagepant (MK-0974) shows >10,000-fold selectivity in a panel of assays representing over 160 receptors, transporters, and enzymes.
Telcagepant (MK-0974) inhibits CGRP-stimulated cAMP production in E10 cells with IC50 of 2.2 nM.
Telcagepant (MK-0974) inhibits the capsaicin-induced increase in dermal blood flow in monkey models.

物理化学性质&存储条件

分子量	566.523
分子式	C26H27F5N6O3
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	1-Piperidinecarboxamide, N-[(3R,6S)-6-(2,3-difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-

参考文献

1. Paone DV, et al. J Med Chem. 2007 Nov 15;50(23):5564-7.

2. Salvatore CA, et al. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21.

3. Sinclair SR, et al. Br J Clin Pharmacol. 2010 Jan;69(1):15-22.

MK-0974 (Telcagepant, MK0974)

生物&药学活性

物理化学性质&存储条件

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MK-0974 (Telcagepant, MK0974)

生物&药学活性

物理化学性质&存储条件

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