Rimegepant CAS# 1289023-67-1

Rimegepant (BMS-927711) is a potent, orally bioavailable small-molecule antagonist of the calcitonin gene–related peptide (CGRP) receptor. In preclinical binding assays, it inhibited human CGRP receptor activity with a Ki of ~0.027 nM and blocked CGRP-induced cAMP accumulation with an IC50 of ~0.1 nM. In animal models of migraine, rimegepant effectively prevented CGRP-mediated vasodilation and reduced neurogenic plasma protein extravasation in the dura mater. It demonstrated high selectivity over related receptors and showed good oral bioavailability and central nervous system penetration in rodents. These findings supported its development as a highly potent, selective, and long-acting CGRP receptor antagonist for migraine treatment.