Bioactivity | 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]. |
Invitro | 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]. |
Name | IMB-808 |
CAS | 870768-70-0 |
Formula | C18H15F3N2O4 |
Molar Mass | 380.32 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. |