BMS-665053

BMS-665053 is a potent and selective CRF1 receptor antagonist with an IC50 of 1.0 nM, effectively inhibiting CRF-stimulated cAMP production in vitro (IC50 = 4.9 nM in Y-79 cells) . It demonstrates in vivo efficacy in rodent models of anxiety, such as the Defensive Withdrawal test, and exhibits favorable pharmacokinetic properties including low clearance and a long half-life in rats.