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Chemical Structure : MK-0974
Catalog No.: 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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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.
| M.Wt | 566.523 | |
| Formula | C26H27F5N6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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