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LXR-623

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Chemical Structure| 875787-07-8 同义名 : WAY 252623
CAS号 : 875787-07-8
货号 : A566900
分子式 : C21H12ClF5N2
纯度 : 99%+
分子量 : 422.778
MDL号 : MFCD16495812
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(106.44 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 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].
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 19962892
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.83mL

2.37mL

1.18mL

23.65mL

4.73mL

2.37mL
参考文献

[1]Ponnal N, Michael D B, et al. LXR-623, a novel Liver X Receptor modulator, displays neutral lipid effects in Cholesteryl Ester Transfer Protein-expressing species and inhibits atherosclerotic lesion progression in Low Density Lipoprotein receptor knockout mice. Abstract 1453.

[2]DiBlasio-Smith EA, Arai M, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J Transl Med. 2008 Oct 16;6:59.

[3]Villa GR, Hulce JJ, et al. An LXR-Cholesterol Axis Creates a Metabolic Co-Dependency for Brain Cancers. Cancer Cell. 2016 Nov 14;30(5):683-693.