ML-290 (ML290) is a potent and selective small-molecule agonist of hRXFP1 with EC50 of 94 nM.
ML-290 displays >15-fold selectivity over RXFP2 (IC50>15 uM).
ML-290 shows similar efficacy as the natural hormone in functional assays, and increases intracellular cAMP and induces VEGF expression (2.8-fold at 250 nM).
ML-290 has as excellent in vitro ADME profile and in vivo PK properties; a very useful tool for the study of RXFP1 activation in pre-clinical disease models of heart failure and other diseases.
