KYLO-0603 is an orally active and selective THR-beta agonist with an EC50 of 31.07 nM. It effectively reduces serum cholesterol and low-density lipoprotein cholesterol levels. By activating THR-beta receptors, KYLO-0603 enhances the expression of THR-regulated genes like iodothyronine deiodinase 1 (Dio1), malic enzyme 1 (Me1), and thyroid hormone-responsive (Thrsp) gene, while it inhibits the expression of inflammatory and fibrosis-related genes, including low-density lipoprotein receptor (LDL-R) gene. This compound is applicable for the study of metabolic associated steatohepatitis (MASH) and liver fibrosis.
