LXRs (Liver X receptors) are ligand-activated transcription factors of the nuclear receptor superfamily, consist of two LXR isoforms termed alpha and beta. It is characterized as key transcriptional regulators of lipid and carbohydrate metabolism. LXR-623 is a brain permeable synthetic ligand for LXRs with IC50 values of 179 and 24 nM for LXRα and LXRβ, respectively. LXR-623 could upregulate the expression of LXR target gene ABCA1 and stimulate cholesterol efflux with EC50 values of 0.3–1.2 uM in acLDL- loaded foam cell macrophages. Dose of LXR-623 at 15 mg/kg for 8 weeks resulted in a significant reduction of atherosclerotic lesion by 37% in high fat diet mice[1]. Treatment with 2μM LXR-623 for 16h significantly increase the expression of LXR target gene ABCA1, ABCG1 and PLTP in human PBMCs[2]. The highly brain permeability of LXR-623 facilitated its therapeutic in brain cancers. Treatment with LXR-623 at concentration of 2.5μM and 5μM for 3 or 5 days selectively killed GBM cells in an LXRβ- and cholesterol-dependent fashion. Daily oral administration of LXR-623 at 400 mg/kg for 5 weeks inhibited tumor growth, promoted tumor cell death, and prolonged the survival of mice bearing intracranial patient-derived GBMs[3].
LXR-623 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
HepG2 cells
Function assay
Effect on triglyceride accumulation in human HepG2 cells, EC50=1 μM
19962892
HuH7 cells
Function assay
Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay, EC50=3.67 μM
19962892
THP1 cells
Function assay
Effect on ABCA1 gene expression in human differentiated THP1 cells, EC50=0.54 μM
Effect on triglyceride accumulation in human HepG2 cells, EC50=1 μM
19962892
HuH7 cells
Function assay
Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay, EC50=3.67 μM
19962892
THP1 cells
Function assay
Effect on ABCA1 gene expression in human differentiated THP1 cells, EC50=0.54 μM
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