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 fibrosis in transgenic mice expressing human RXFP1 when administered at a dose of 37 mg/kg.Formal Name: 2-[[2-(1-methylethoxy)benzoyl]amino]-N-[3-[(trifluoromethyl)sulfonyl]phenyl]-benzamide. CAS Number: 1482500-76-4. Synonyms: RXFP1 Agonist 8. Molecular Formula: C24H21F3N2O5S. Formula Weight: 506.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml, DMSO: 25 mg/ml, Ethanol: 0.14 mg/ml. lambdamax: 212, 263 nm. SMILES: O=S(C1=CC=CC(NC(C2=CC=CC=C2NC(C3=C(OC(C)C)C=CC=C3)=O)=O)=C1)(C(F)(F)F)=O. InChi Code: InChI=1S/C24H21F3N2O5S/c1-15(2)34-21-13-6-4-11-19(21)23(31)29-20-12-5-3-10-18(20)22(30)28-16-8-7-9-17(14-16)35(32,33)24(25,26)27/h3-15H,1-2H3,(H,28,30)(H,29,31). InChi Key: RSYHJSDOGMSLDH-UHFFFAOYSA-N.