apelin-13-peptide and diphenyl

The APJ receptor and its endogenous peptidic ligand apelin have been implicated as important modulators of cardiovascular function, and APJ receptor agonists may be beneficial in the treatment of heart failure. In this article, we describe the discovery of a series of biphenyl acid derivatives as potent APJ receptor agonists. Following the identification of initial high-throughput screen lead

Topics: Animals; Apelin Receptors; Biphenyl Compounds; Blood Pressure; Cardiovascular Agents; Dose-Response Relationship, Drug; Heart Rate; HEK293 Cells; High-Throughput Screening Assays; Humans; Intercellular Signaling Peptides and Proteins; Male; Rats, Sprague-Dawley; Small Molecule Libraries; Structure-Activity Relationship