ML-290 is an allosteric agonist of relaxin family peptide receptor 1 (RXFP1; EC₅₀ = 94 nM for human RXFP1).^1,2 It displays >15-fold selectivity for RXFP1 over RXFP2.² ML-290 activates human, rhesus macaque, pig, and rabbit RXFP1 but is weak or inactive at mouse or guinea pig RXFP1.^2,3 Through RXFP1, ML-290 increases intracellular cAMP and induces VEGF expression (2.8-fold at 250 nM).² ML-290 is metabolically stable and displays excellent in vivo pharmacokinetics.²

≥95%

Store at -20℃

RXFP1 Agonist 8​​;

1.Diepenhorst, N.A.,Petrle, E.J.,Chen, C.Z., et al. Investigation of interactions at the extracellular loops of the relaxin family peptide receptor 1 (RXFP1). J. Biol. Chem. 289(50), 34938-34952 (2014).

2.Xiao, J.,Chen, C.Z.,Huang, Z., et al. Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1). Probe Reports from the NIH Molecular Libraries Program (2012).

3.Huang, Z.,Myhr, C.,Bathgate, R.A.D., et al. Activation of relaxin family receptor 1 from different mammalian species by relaxin peptide and small-molecule agonist ML290. Front. Endocrinol. (Lausanne) 6, 128 (2015).