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Telcagepant

Telcagepant structure

CAS No:
781649-09-0
Formula:
C26H27F5N6O3
Chemical Name:
Telcagepant
Synonyms:
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)-;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)-1-piperidinecarboxamide;MK 0974;Telcagepant
Categories:
Pharmaceutical Intermediates > Heterocyclic Compound

Description

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

Telcagepant has been investigated for the treatment of Migraine. It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine. CGRP and its receptors are found in areas of the central and peripheral nervous system that are important for the transmission of migraine pain. During migraine attacks, CGRP activates these receptors and facilitates the transmission of pain impulses.

Telcagepant Basic Attributes

Molecular Weight：

566.528

Exact Mass：

566.52

UNII：

D42O649ALL

Characteristics

PSA：

103.33000

XLogP3：

2.59

Density：

1.54

Refractive Index：

1.613

Drug Information

Drug Indication：

Migraine with or without aura

Mechanism of Action：

Telcagepant blocks the binding of CGRP to receptors within the areas of the central and peripheral nervous system that are important for the transmission of migraine pain and thereby is believed to inhibit the transmission of pain signals that lead to migraine headaches.

MeSH Entry Terms：

MK 0974

Telcagepant Use and Manufacturing

Use Classification：

Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:566.5
XLogP3:3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:4
Exact Mass:566.20647955
Monoisotopic Mass:566.20647955
Topological Polar Surface Area:97.9
Heavy Atom Count:40
Complexity:948
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes