ML-290

ML-290 is an allosteric agonist of relaxin family peptide receptor 1 (RXFP1; EC50 = 0.094 µM for the human receptor in a cAMP produciton assay). It is selective for RXFP1 over RXFP2 (EC50 = 1.5 µM). ML-90 (250 nM) induces expression of VEGF in THP-1 cells expressing human RXFP1. It stimulates cAMP release from HEK293 cells expressing the human, macaque, pig, or rabbit receptors, but not the guinea pig or mouse receptors. ML-290 (5 µM) increases the expression of MMP1 and PPARGC1A and decreases COL1A1 expression in primary human hepatic stellate cells. It reduces carbon tetrachloride-induced liver...