MK-3207

MK-3207 is an antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 22 pM for the recombinant human receptor).1 It is selective for the CGRP receptor over adrenomedullin receptor 1 (AM1) and AM2, calcitonin (CT) receptor, and amylin 3 receptor (AMY3; Kis = 16.5, 0.156, 1.9, and 0.128 µM, respectively) but does inhibit AMY1 to a lesser extent (Ki = 750 pM). MK-3207 inhibits CGRP-induced cAMP production in HEK293 cells expressing the human CGRP receptor (IC50 = 120 pM). It decreases capsaicin-induced forearm dermal vasodilation in rhesus monkeys in a dose-dependent manner.WARNING This product is not for human or veterinary use.

A CGRP receptor antagonist

557.6

≥98%

Biochemicals/Receptor Pharmacology/Antagonists

Formal_Name:8R-(3,5-difluorophenyl)-10-oxo-N-[(2R)-1,1',2',3-tetrahydro-2'-oxospiro[2H-indene-2,3'-[3H]pyrrolo[2,3-b]pyridin]-5-yl]-6,9-diazaspiro[4.5]decane-9-acetamide

O=C1[C@]2(CC3=CC(NC(CN4[C@H](C5=CC(F)=CC(F)=C5)CNC6(CCCC6)C4=O)=O)=CC=C3C2)C7=CC=CN=C7N1

957118-49-9

≥ 4 years

Acetonitrile: Slightly Soluble: 0.1-1 mg/ml DMSO: Sparingly Soluble: 1-10 mg/ml