1612191-86-2|BAR502|CsnPharm

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CAS No.: 1612191-86-2

BAR502 Catalog No. CSN20202

BAR502 is an agonist of FXR and GPBAR1 that promotes browning of white adipose tissue and reverses liver fibrosis and steatosis.

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纯度 & 质量文件批次:

靶点选择性

生物活性

描述Bile acids (BAs), the end-products of cholesterol catabolism, are signaling molecules activating several cellular networks through the recognition of nuclear and membrane receptors, such as FXR (farnesoid-X-receptor) and GP-BAR1. BAR502 is a dual FXR and GP-BAR1 agonist with EC₅₀ values of 2 and 0.4 μM, respectively. BAR502 (10 μM) was able to induce the expression of pro-glucagon mRNA in GLUTAg cells, an intestinal endocrine cell line, as well as to increase cAMP concentrations in THP-1 cells^[3]. In C57BL6 mice, BAR502 (15 mg/kg/day) reversed the NASH (non-alcoholic steatohepatitis)-like features induced by high fat diet (HFD). In addition, BAR502 reduced liver fibrosis scores by 70% and expression of pro-fibrogenetic genes (αSMA and α1-collagen), as well as the inflammatory score and liver expression of F4/80, IL-1β, IL-6, MCP-1, RANTES and TNFα mRNA^[4].
参考文献

[1] Carino A, Cipriani S, et al. BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis. Sci Rep. 2017 Feb 16;7:42801.
[2] Cipriani S, Renga B, et al. Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling. PLoS One. 2015 Jul 15;10(7):e0129866.
[3] Festa C, Renga B, D'Amore C, Sepe V, Finamore C, De Marino S, Carino A, Cipriani S, Monti MC, Zampella A, Fiorucci S. Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands. J Med Chem. 2014 Oct 23;57(20):8477-95
[4] Carino A, Cipriani S, Marchianò S, Biagioli M, Santorelli C, Donini A, Zampella A, Monti MC, Fiorucci S. BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis. Sci Rep. 2017 Feb 16;7:42801

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
- 2.5470 mL
- 12.7351 mL
- 25.4702 mL
- 5 mM
- 0.5094 mL
- 2.5470 mL
- 5.0940 mL
- 10 mM
- 0.2547 mL
- 1.2735 mL
- 2.5470 mL

技术信息

CAS号

1612191-86-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H44O3

运输

蓝冰

分子量

392.62

别名

溶解度

Ethanol	100.0 mg/mL (254.7 mM) warming
DMF	50.0 mg/mL (127.4 mM) warming

动物实验配方

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动物实验：给药剂量mg/kg 动物体重g 动物数量只每天给药次给药天

需要的总药量：mg

工作液计算器 ✕

动物实验：给药剂量mg/kg 动物体重g 给药体积μL

您需要配制的工作液浓度为：mg/mL

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