MK-0974, CAS 781649-09-0

Formulation: A crystalline solid

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

Purity: ≥98%

Formula Markup: C26H27F5N6O3

Formula Weight: 566,5

Shelf life (days): 1460

CAS Number: 781649-09-0

Notes: 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}

• Artikelnummer: CAY23960-5
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 23960-5
• Green Labware: Nein
• Verpackungseinheit: 5 mg
• Mengeneinheit: STK