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Telcagepant

Catalog No. T16093 CAS 781649-09-0

Synonyms: MK-0974

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

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Telcagepant, CAS 781649-09-0

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Telcagepant is an orally active antagonist of calcitonin gene-related peptide (CGRP) receptor (Kis: 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively).
Targets&IC50	CGRP (human):(ki)0.77 nM, CGRP (rhesus):1.2 nM(ki)
In vitro	Telcagepant shows affinity (Ki) for the canine and rat receptors, with values of 1204 nM and 1192 nM (n=10), respectively. Telcagepant displays saturable binding to SK-N-MC membranes with a KD of 1.9 nM and Bmax of 479 fmol/mg protein. Telcagepant effectively blocks human α-CGRP-stimulated cAMP responses in the human CGRP receptor-expressing HEK293 cells (IC50: 2.2 nM)[1]. Telcagepant also displays saturable binding to rhesus cerebellum homogenate (KD: 1.3 nM and Bmax of 20 fmol/mg)[2].
In vivo	Telcagepant (MK-0974) exhibits linear pharmacokinetics within a 0.5-10 mg/kg intravenous dosage range in monkeys. However, when administered orally at doses between 5-30 mg/kg, the area under the plasma concentration-time curve (AUC) increases in a manner that is 15-fold over dose-proportional. Furthermore, administering Telcagepant as an intravenous bolus at 1 mg/kg highlights the time-dependent nature of the antagonist’s efficacy, which aligns with plasma concentrations[1][3].

Synonyms	MK-0974
Molecular Weight	566.52
Formula	C26H27F5N6O3
CAS No.	781649-09-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (88.26 mM)

References and Literature

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.

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Keywords

Telcagepant 781649-09-0 Others MK 0974 MK-0974 MK0974 inhibitor inhibit

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