IMB-808

• CAT Number: I029244
• CAS Number: 870768-70-0
• Molecular Formula: C18H15F3N2O4
• Molecular Weight: 380.32
• Purity: ≥95%
• Synonyms: N-methyl-N-[2-oxo-2-(2,3,4-trifluoroanilino)ethyl]-2,3-dihydro-1,4-benzodioxine-6-carboxamide
• InChI: InChI=1S/C18H15F3N2O4/c1-23(9-15(24)22-12-4-3-11(19)16(20)17(12)21)18(25)10-2-5-13-14(8-10)27-7-6-26-13/h2-5,8H,6-7,9H2,1H3,(H,22,24)
• InChIKey: XITZPIXICJOKTF-UHFFFAOYSA-N
• SMILES: CN(CC(=O)NC1=C(C(=C(C=C1)F)F)F)C(=O)C2=CC3=C(C=C2)OCCO3

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[1].
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].

Reference

[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.
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