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).¹ 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.² ML-290 (5 µM) increases the expression of MMP1 and PPARGC1A and decreases COL1A1 expression in primary human hepatic stellate cells.³ It reduces carbon tetrachloride-induced liver fibrosis in transgenic mice expressing human RXFP1 when administered at a dose of 37 mg/kg.

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1. 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).

2. 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).

3. Kaftanovskaya, E.M., Ng, H.H., Soula, M., et al. Therapeutic effects of a small molecule agonist of the relaxin receptor ML290 in liver fibrosis. The FASEB Journal 33(11), 12435-12446 (2019).