In Vitro: IMB-808 (0.001 μM-30 μM) significantly dose-dependently induces LXRβ activation under the concentrations ranged from 0.001 μM to 30 μM, with an EC50 of 0.53 μM. In a luciferase reporter assay IMB-808 using GAL4-pGL4-luc reporter plasmid, IMB-808 also could dose-dependently active LXRα with a lower EC50 of 0.15 μM.IMB-808 (0 μM-10 μM; 18 hours) significantly increases protein and mRNA levels of ABCG1 as well as ABCA1 in RAW264.7 macrophages.IMB-808 (0.1 μM, 0.3 μM, 1 μM, 3 μM, or 10 μM; 24 hours) promotes cholesterol efflux towards ApoA-I and HDL dose-dependently and reduces the cellular cholesterol concentration in these two cell lines.