LXRα Agonist

Ginsenoside C-K hexapropionate ester (Structure 2) is a selective agonist of LXRα, with no significant activation effect on LXRβ. Ginsenoside C-K hexapropionate ester upregulates the expression of downstream genes such as ABCA1 by activating LXRα, promoting reverse cholesterol transport, and reducing lipid deposition in macrophage-derived foam cells. It can be used in the research of atherosclerosis. Ginsenoside C-K hexapropionate ester is a derivative synthesized from ginsenoside Compound K, an active metabolite of Panax notoginseng saponins, by modification with propionic anhydride.

LXRα agonist 1 is a selective LXRα agonist, with EC₅₀ values of 42 nM and 266 nM against purified LXRα and LXRβ, respectively. LXRα agonist 1 acts as a lipotoxicity inducer, triggering the production of toxic saturated fatty acids in tumor cells, and induces lipotoxicity-mediated cancer cell death when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the research of hepatocellular carcinoma.