BMS-986331 is a highly potent and selective Formyl peptide receptor 2 (FPR2) agonist with EC50 of 0.5 nM (hFPR2).
BMS-986331 exhibits rat FPR2 cAMP EC50 of 1 nM, 220-fold selective over rFPR1.
BMS-986331 induces concentration-dependent modulation of bioluminescence resonance energy transfer (BRET) signals for Gαi2 (EC50=0.5 nM), GαoA (EC50=0.5 nM), Gα12 (EC50=16 nM), and Gα13 (EC50=13 nM) biosensors following FPR2 activation in in HEK293 cells transiently expressing human FPR2.
BMS-986331 exhibits excellent activity in inducing the expression and release of the pro-resolution cytokine IL-10 in isolated human whole blood and in an acute rat model of systemic inflammation, respectively.
BMS-986331 (0.1, 1, or 10 mg/kg/day, PEG 400/PG/TPGS/water, 40:10:10:40) preserves myocardial structure and improves cardiac function in the rat MI model.
