Description: ML221 is a potent apelin /APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 µM in the cAMP assay, and 1.75 µM in the beta-arrestin assay, and EC80 of 10 nM in both assays. Target: Apelin receptor, Arrestin. Smiles:...

ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 µM). It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 µM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and beta-arrestin recruitment assays (IC50s = 0.7 and 1.75 µM, respectively). It...