LXRα Agonist

22 (R)-Hydroxycholesterol (Narthesterol) is a natural oxysterol, acting as a LXRα agonist that inhibits cancer cell proliferation. 22 (R)-Hydroxycholesterol activates LXRα-mediated upregulation of downstream ABCA1 expression, enhances apolipoprotein-dependent cholesterol efflux, reduces intracellular cholesterol content, and decreases the production of β-amyloid peptide. 22 (R)-Hydroxycholesterol induces the differentiation of human mesenchymal stem cells into functional dopaminergic neurons. 22 (R)-Hydroxycholesterol is applicable to research related to cancer, Alzheimer's disease, and Parkinson's disease.

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.