APJ receptor agonist 1

APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Anti-infection >> HIV

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.

[1]. Su S, Clarke A, et al. Biphenyl Acid Derivatives as APJ Receptor Agonists. J Med Chem. 2019;62(22):10456-10465.