ml-290

Description: ML-290, a 2-acetamido-N-phenylbenzamide analog, is a novel potent, selective and orally bioactive agonist of the relaxin/insulin-like family peptide receptor (RXFP1) and an activator of anti-fibrotic genes with an EC50 of 94 nM. It was identified from a dose responsive quantitative high throughput screen (qHTS) of > 350, 000 compounds against a human relaxin/insulin-like family peptide receptor (RXFP1) transfected HEK293?cell line. ML-290 has excellent in vivo PK properties with high levels of systemic exposure. ML-290 represents the first-in-class small-molecule agonists of RXFP1 and is a potent activator of anti-fibrotic genes.

References: Eur J Med Chem. 2018 Aug 5; 156:79-92.