A CGRP receptor antagonist (Ki = 0.77 μM); binds selectively to the human CGRP receptor complex over the adrenomedullin receptor complexes in HEK293 cells (Kis = >100 and 29 μM for CRLR with RAMP2 and 3

MK-0974 – 10 mg

Brand:
Cayman
CAS:
781649-09-0
Storage:
-20
UN-No:
Non-Hazardous - /

MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 μM), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).{38703} MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 μM, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 μM) reduces CGRP-induced vasodilation in isolated human meningeal arteries.{38704} MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).{38703}  

 

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SKU: 23960 - 10 mg Category:

Description

A CGRP receptor antagonist (Ki = 0.77 μM); binds selectively to the human CGRP receptor complex over the adrenomedullin receptor complexes in HEK293 cells (Kis = >100 and 29 μM for CRLR with RAMP2 and 3, respectively); inhibits CGRP-induced cAMP accumulation in HEK293 cells expressing the CGRP receptor complex (IC50 = 2.2 nM); reduces CGRP-induced vasodilation in isolated human meningeal arteries; inhibits vasodilation induced by topical application of capsaicin in rhesus monkeys (EC50 = 127 nM)

Formal name: 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

Synonyms: 

Molecular weight: 566.5

CAS: 781649-09-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cardiovascular System|Vasculature|Vasoconstriction

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