Catalog No.: PC-38139Not For Human Use, Lab Use Only.
CMF-019 (CMF019) is the first G protein biased small molecule Apelin receptor (APJ, APLNR) agonist, potent benzimidazole-derived apelin peptidomimetic, binds to APLNR with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse APLNR, respectively.
CMF-019 (CMF019) is the first G protein biased small molecule Apelin receptor (APJ, APLNR) agonist, potent benzimidazole-derived apelin peptidomimetic, binds to APLNR with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse APLNR, respectively.
CMF-019 caused dose-dependent vasodilatation in vivo, rescues human pulmonary artery endothelial cells from apoptosis induced by tumor necrosis factor α and cycloheximide.
CMF-019 displays remarkable bias at the apelin receptor, recapitulates all aspects of the cardiovascular responses to the endogenous ligand, [Pyr1]apelin-13, in vivo.
CMF-019 is suitable as a tool compound and provides the basis for design of biased agonists with improved pharmacokinetics for treatment of cardiovascular conditions such as pulmonary arterial hypertension.
