LXRβ agonist-2

LXRβ agonist-2 is an orally active and selective LXRβ agonist. LXRβ agonist-2 increases high-density lipoprotein cholesterol levels without elevating plasma triglyceride levels. LXRβ agonist-2 decreases lipid accumulation area in the aortic arch. LXRβ agonist-2 can be used for the research of atherosclerosis^[1]. IC50 & Target:EC50: 7 nM (LXRβ), 200 nM (LXRα)^[1] In Vitro:LXRβ agonist-2 (0.01-10 μM; 24 h) potently and selectively activates LXRβ in GAL4-LXR luciferase assays using stably transfected CHO K-1 cells, with an EC₅₀ of 0.007 μM and an LXRα/LXRβ selectivity ratio of 28.5^[1]. In Vivo:LXRβ agonist-2 ((-)-56) (1-3 mg/kg; p.o.; daily; 10 weeks) increases HDL-C levels and reduces aortic lipid accumulation area in high-fat- and cholesterol-fed LDL receptor knock-out mice without altering LDL-C levels^[1].