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IMB-808

Names

[ CAS No. ]:
870768-70-0

[ Name ]:
IMB-808

[Synonym ]:
N-Methyl-N-(2-oxo-2-((2,3,4-trifluorophenyl)amino)ethyl)-3,4-dihydro-2H-benzo[b][1,4] dioxin-7-carboxamide
IMB-808
N-Methyl-N-{2-oxo-2-[(2,3,4-trifluorophenyl)amino]ethyl}-2,3-dihydro-1,4-benzodioxine-6-carboxamide
1,4-Benzodioxin-6-carboxamide, 2,3-dihydro-N-methyl-N-[2-oxo-2-[(2,3,4-trifluorophenyl)amino]ethyl]-
2,3-Dihydro-N-methyl-N-[2-oxo-2-[(2,3,4-trifluorophenyl)amino]ethyl]-1,4-benzodioxin-6-carboxamide

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> LXR
Research Areas >> Inflammation/Immunology

[In Vitro]

IMB-808 (0.001 μM-30 μM) 在 0.001 μM 到 30 μM 的浓度范围内显着剂量依赖性地诱导 LXRβ 激活，EC50 为 0.53 μM。在使用 GAL4-pGL4-luc 报告质粒的荧光素酶报告基因测定中，IMB-808 还可以剂量依赖性地激活 LXRα，EC50 为 0.15 μM[1]. IMB-808（0 μM-10 μM；18 小时）显着增加 RAW264.7 巨噬细胞中 ABCG1 和 ABCA1 的蛋白质和 mRNA 水平[1]。 IMB-808（0.1 μM、0.3 μM、1 μM、3 μM 或 10 μM；24 小时）剂量依赖性地促进胆固醇流向，并降低细胞系中的细胞胆固醇浓度[ 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.  

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
572.8±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H15F3N2O4

[ Molecular Weight ]:
380.32

[ Flash Point ]:
300.2±30.1 °C

[ Exact Mass ]:
380.098389

[ LogP ]:
2.96

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.592

Related Compounds