LXR-623 | WAY 252623 | LXRα/β Agonist | AmBeed-信号通路专用抑制剂

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LXR-623 {[allProObj[0].p_purity_real_show]}

货号：A566900 同义名： 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.

LXR-623 化学结构
CAS号：875787-07-8

LXR-623 3D分子结构
CAS号：875787-07-8

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LXR-623 纯度/质量文件产品仅供科研

货号：A566900 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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LXR-623 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].

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	19962892

LXR-623 动物研究

Dose	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.)
Administration	p.o.

LXR-623 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.

LXR-623 实验方案

计算器

存储液制备

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

LXR-623 技术信息

CAS号	875787-07-8
分子式	C₂₁H₁₂ClF₅N₂
分子量	422.778

别名	WAY 252623
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

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

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

LXR-623 {[allProObj[0].p_purity_real_show]}

LXR-623 纯度/质量文件产品仅供科研

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LXR-623 质控信息

LXR-623 生物活性

LXR-623 细胞研究

LXR-623 动物研究

LXR-623 参考文献

LXR-623 实验方案

LXR-623 技术信息

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LXR-623 {[allProObj[0].p_purity_real_show]}

LXR-623 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

LXR-623 质控信息

LXR-623 生物活性

LXR-623 细胞研究

LXR-623 动物研究

LXR-623 参考文献

LXR-623 实验方案

LXR-623 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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LXR-623 纯度/质量文件产品仅供科研