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CAS No.: 875787-07-8

LXR-623 Catalog No. CSN16661

Synonyms: WAY 252623

LXR-623 is a novel and brain-penetrant LXR agonist with IC50 values of 179 and 24 nM for LXRα and LXRβ, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究
剂量
Rabbit: 1.5 mg/kg - 15 mg/kg^[4] (p.o.) Cynomolgus monkey: 15 mg/kg, 50 mg/kg^[2] (p.o.) Mice: 50 mg/kg^[2] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Rabbit: 1.5 mg/kg - 15 mg/kg^[4] (p.o.) Cynomolgus monkey: 15 mg/kg, 50 mg/kg^[2] (p.o.) Mice: 50 mg/kg^[2] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00366522	Healthy	Phase 1	Completed	-	United States, Nebraska ... more >> Lincoln, Nebraska, United States, 68502 Collapse <<
NCT00385489	Healthy	Phase 1	Completed	-	Japan ... more >> Toshima-ku, Tokyo, Japan, 171-0014 Collapse <<
NCT00379860	Healthy Subjects	Phase 1	Terminated	-	-

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3653 mL
- 11.8265 mL
- 23.6531 mL
- 5 mM
- 0.4731 mL
- 2.3653 mL
- 4.7306 mL
- 10 mM
- 0.2365 mL
- 1.1827 mL
- 2.3653 mL

技术信息

CAS号

875787-07-8

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H12ClF5N2

运输

蓝冰

分子量

422.78

别名

WAY 252623

溶解度

DMSO	370.0 mg/mL (875.2 mM)
Water	insoluble

动物实验配方

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