APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research.

The S-atropisomer APJ receptor agonist 1 (compound 15a) is 200-fold more potent than the corresponding R-atropisomer.[1].

APJ receptor agonist 1 (10-100 μg/min/kg; intravenous infusion) induces a 10% increase in CO with minimal impact on blood pressure (<5% transient blood pressure drop)[1]. Animal Model: Isoflurane-anesthetized male Sprague Dawley rats[1]Dosage: 10, 100, 1000 μg/kg/min Administration: IV; infused into the jugular vein for 15 min Result: Showed a dose-dependent improvement in the cardiac output in male Sprague Dawley rats with no significant changes in either mean arterial blood pressure or heart rate.