产品说明书

BAR502

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Chemical Structure| 1612191-86-2 同义名 : Compound 30
CAS号 : 1612191-86-2
货号 : A482907
分子式 : C25H44O3
纯度 : 98%
分子量 : 392.615
MDL号 : MFCD31381922
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

无水乙醇: 50 mg/mL(127.35 mM)，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

DMF: 50 mg/mL(127.35 mM)，配合低频超声助溶
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.47mL

5.09mL

2.55mL
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