Biochem/physiol Actions

SR9243 is a selective inverse agonist of the nuclear receptor liver-X-receptor (LXR) that targets the Warburg effect, inhibiting glycolysis and lipogenesis by reducing glycolytic and lipogenic gene expression. SR9243 is believed to enhance corepressor recruitment to LXRs at target-gene promoters, resulting in suppression of gene expression. SR9243 induced apoptosis in tumor cells without harming normal cells. SR9243 reduced prostate, colorectal, and lung cancer cell viability at nanomolar concentrations and also inhibited colon tumor xenograft growth.

SR9243 has the ability to reduce liver fibrosis stimulated by BDL (bile-duct ligation) and CCL4 (carbon tetrachloride). It stimulates apoptosis without promoting weight loss, hepatotoxicity and inflammation. SR9243 blocks the initiation of liver-X-receptor (LXR) by increasing LXR-corepressor recruitment.

Packaging

5, 25 mg in glass bottle