Telcagepant-d8

Telcagepant-d8 (MK-0974-d8) is deuterium labeled 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

[1132641-75-8]

Product Name Alternative

MK-0974-d8

UNSPSC

12352005

Target

CGRP Receptor; Isotope-Labeled Compounds

Related Pathways

GPCR/G Protein; Neuronal Signaling; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=C1N(C2C([2H])([2H])C([2H])([2H])N(C([2H])([2H])C2([2H])[2H])C(N[C@H]3C(N(C[C@H](C4=C(C(F)=CC=C4)F)CC3)CC(F)(F)F)=O)=O)C5=CC=CN=C5N1

Molecular Formula

C26H19D8F5N6O3

Molecular Weight

574.57

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.|[4]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.