Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAR502 是一种 GPBAR1 和 FXR 双重激动剂,IC50分别为0.4 μM 和 2 μM。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: 48 mg/mL (122.26 mM), sonification is recommended.
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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