Atogepant CAS# 1374248-81-3

Atogepant, an oral calcitonin gene–related peptide (CGRP) receptor antagonist, demonstrated potent preclinical bioactivity with high selectivity for the human CGRP receptor. In vitro, it inhibited CGRP-stimulated cAMP production in SK-N-MC cells with nanomolar potency (Ki ≈ 0.07 nM; IC50 ≈ 0.16 nM) and showed >10,000-fold selectivity over related receptors. In animal migraine models, atogepant blocked CGRP-induced vasodilation and inhibited plasma protein extravasation in dura mater, correlating with dose-dependent suppression of migraine-like behaviors. Its favorable oral bioavailability, sustained receptor occupancy, and minimal off-target activity supported advancement into clinical trials for preventive migraine therapy.