Telcagepant (MK-0974) | CGRP antagonist

Chemical Structure : Telcagepant

CAS No.: 781649-09-0

Telcagepant (MK-0974, MK0974)

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.

Packing	Price	Stock
10 mg	$98	In stock
10 mg	$98	In stock
25 mg	$158	In stock
50 mg	$258	In stock
100 mg		Get quote

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Biological Activity

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.

Physicochemical Properties

M.Wt	566.523
Formula	C26H27F5N6O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
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)-

References

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.

Telcagepant (MK-0974, MK0974)

Biological Activity

Physicochemical Properties

References

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