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BAR502

BAR502

产品编号 TQ0252   CAS 1612191-86-2

BAR502 是一种 GPBAR1 和 FXR 双重激动剂,IC50分别为0.4 μM 和 2 μM。

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BAR502 Chemical Structure
BAR502, CAS 1612191-86-2
规格 价格/CNY 货期 数量
1 mg ¥ 638 现货
5 mg ¥ 1,550 现货
10 mg ¥ 2,470 现货
25 mg ¥ 4,930 现货
50 mg ¥ 7,750 现货
100 mg ¥ 9,870 现货
产品目录号及名称: BAR502 (TQ0252)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).
靶点活性 FXR:2 μM, GPBAR1:0.4 μM
体外活性 At the concentration of 10 μM, BAR502 fails to transactivate GR, PPARγ, and LXR, respectively, but it transactivates the nuclear receptor PXR. BAR502 is able to induce the expression of proglucagon mRNA in GLUTAg cells, an intestinal endocrine cell line, as well as to increase cAMP concentrations in THP-1 cells. BAR502 induces the expression of OSTα, BSEP, and SHP in HepG2 cells. BAR502 shows very potent activity in the recruitment of SRC-1 coactivator and high affinity to FXR [1].
体内活性 In models of non-obstructive cholestasis, BAR502 attenuates liver injury without causing itching. Co-treatment with BAR502 increases survival attenuates serum alkaline phosphatase levels and robustly modulates the liver expression of canonical FXR target genes including OSTα, BSEP, SHP, and MDR1, without inducing pruritus [2]. Treatment with BAR502 causes a 10% reduction of b.w., increases insulin sensitivity and circulating levels of HDL, while reduces steatosis, inflammatory and fibrosis scores and liver expression of SREPB1c, FAS, PPARγ, CD36, and CYP7A1 mRNA. BAR502 increases the expression of SHP and ABCG5 in the liver and SHP, FGF15 and GLP1 in the intestine. BAR502 promotes the browning of epWAT and reduces liver fibrosis induced by CCl4 [3].
动物实验 C57BL6 mice 24 weeks old are fed a high-fat diet containing 60% kj fat and fructose in drinking water (42?g/L) or normal diet (6 mice) for 18 weeks. After 10 weeks of HFD, mice are randomized to receive HFD alone (9 mice) or HFD plus BAR502 (15?mg/kg/day) body weight by gavage (9 mice) for 8 weeks. Mice are housed under controlled temperatures (22?°C) and photoperiods (12:12-hour light/dark cycle), allowed unrestricted access to standard mouse chow and tap water and allowed to acclimate to these conditions for at least 5 days before inclusion in an experiment [3].
分子量 392.62
分子式 C25H44O3
CAS No. 1612191-86-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMF: 48 mg/mL (122.26 mM), sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMF 1 mM 2.547 mL 12.735 mL 25.4699 mL 63.6748 mL
5 mM 0.5094 mL 2.547 mL 5.094 mL 12.735 mL
10 mM 0.2547 mL 1.2735 mL 2.547 mL 6.3675 mL
20 mM 0.1273 mL 0.6367 mL 1.2735 mL 3.1837 mL
50 mM 0.0509 mL 0.2547 mL 0.5094 mL 1.2735 mL
100 mM 0.0255 mL 0.1273 mL 0.2547 mL 0.6367 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Festa C, et al. 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. 2. Cipriani S, 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. Carino A, 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.
Valinomycin KJ Pyr 9 Bortezomib Oxaliplatin PF-04691502 Sulfabenzamide SB 239063 Norepinephrine

相关化合物库

该产品包含在如下化合物库中:
抗代谢疾病化合物库 核受体化合物库 GPCR靶点分子库 已知活性化合物库 脂代谢化合物库 抗癌化合物库 经典已知活性库 NO PAINS 化合物库 自噬库 代谢化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BAR502 1612191-86-2 Autophagy GPCR/G Protein Metabolism FXR GPCR19 G protein-coupled Bile Acid Receptor 1 GPBAR1 BAR-502 NR1H4 Inhibitor G-protein coupled receptor 19 inhibit BAR 502 TGR5 inhibitor

 

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