Telcagepant

Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

Product Specifications

CAS Number

[781649-09-0]

Product Name Alternative

MK-0974

UNSPSC

12352005

Target

CGRP Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/MK-0974.html

Concentration

10mM

Purity

98.63

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C1NC2=C(N1C3CCN(C(N[C@@H]4CC[C@@H](C5=CC=CC(F)=C5F)CN(CC(F)(F)F)C4=O)=O)CC3)C=CC=N2

Molecular Formula

C26H27F5N6O3

Molecular Weight

566.52

References & Citations

[1]Salvatore CA, et al. Pharmacological characterization of MK-0974 [N-[ (3R,6S) -6- (2,3-difluorophenyl) -2-oxo-1- (2,2,2-trifluoroethyl) azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl) piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther. 2008 Feb;324 (2) :416-21. Epub 2007 Nov 26.|[2]Moore EL, et al. Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment of migraine. Eur J Pharmacol. 2009 Jan 14;602 (2-3) :250-4.|[3]Roller S, et al. Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP) -receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica. 2009 Jan;39 (1) :33-45.