IMB-808

IMB-808 is a potent LXRα/β dual agonist with EC50 values of 0.53 μM and 0.15 μM (0.15 μM, using GAL4-pGL4-luc reporter plasmid) for LXRβ and LXRα, respectively. IMB-808 promotes expression of genes related to reverse cholesterol transport (ABCA1 and ABCG1). IMB-808 can be used as a promising agent for the prospective treatment of atherosclerosis research.

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^[1].
IMB-808 (0 μM-10 μM; 18 hours) significantly increases protein and mRNA levels of ABCG1 as well as ABCA1 in RAW264.7 macrophages^[1].
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^[1].

References:
[1]. Duo Lu, et al. Identification of a Novel Liver X Receptor Agonist that Regulates the Expression of Key Cholesterol Homeostasis Genes with Distinct Pharmacological Characteristics. Mol Pharmacol. 2017 Apr;91(4):264-276.