Fully inhibits forskolin-mediated cAMP production, with an EC50 for human APJ of 0.02 nM, BMS-986224. BMS-986224 (0-100 nM) fully stimulates β-arrestin recruitment, ERK phosphorylation, and APJ internalization in Chinese hamster ovary-K1 or HEK293 ZF cells. BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13.

In the RHR model, BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily) increased stroke volume and cardiac output to levels seen in healthy animals, but without preventing cardiac hypertrophy and fibrosis. These effects are differentiated from enalapril[1].