Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GW 501516 (Endurobol) 是一种有效且高度特异性的 PPARβ/δ 激动剂,EC50值为 1 nM,选择性是 hPPARα/γ 的 1000 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 183 | 现货 | ||
5 mg | ¥ 372 | 现货 | ||
10 mg | ¥ 592 | 现货 | ||
25 mg | ¥ 970 | 现货 | ||
50 mg | ¥ 1,450 | 现货 | ||
100 mg | ¥ 1,980 | 现货 | ||
200 mg | ¥ 2,930 | 现货 | ||
500 mg | ¥ 4,780 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 397 | 现货 |
产品描述 | GW 501516 (Endurobol) is a effective and highly specifc PPARβ/δ agonist (EC50: 1 nM), with 1000-fold selectivity over hPPARα/γ. |
靶点活性 | PPARδ:1 nM(Ki) |
体外活性 | GW 501516 is shown to be the most potent and selective PPARδ agonist as known with an EC50 of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ[1]. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner[3]. |
体内活性 | GW 501516 causes impaired bone formation that leads to decreased BMD and deterioration of bone properties in OVX rats[2]. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model[3]. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice[4]. |
激酶实验 | Tyrosine Kinase Assays: Enzyme assays for determination of IC50 are performed in 96-well filter plates in a total volume of 0.1 mL, containing 20 mM Hepes, pH 7.4, 50 mM sodium vanadate, 40 mM magnesium chloride, 10 μM adenosine triphosphate (ATP) containing 0.5 mCi of [32P]ATP, 20 mg of polyglutamic acid/tyrosine, 10 ng of EGFR tyrosine kinase, and appropriate dilutions of CI-1033. All components except the ATP are added to the well and the plate is incubated with shaking for 10 min at 25 °C. The reaction is started by adding [32P]ATP, and the plate is incubated at 25 °C for another 10 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid (TCA). The plate is kept at 4 °C for at least 15 min to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% TCA and 32P incorporation determined with a Wallac β plate counter. |
细胞实验 | GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 μM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 μM palmitate bound to 8.0% BSA for 12 h[3]. |
别名 | Cardarine, GW501516, GW 1516, GSK-516, Endurobol |
分子量 | 453.5 |
分子式 | C21H18F3NO3S2 |
CAS No. | 317318-70-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.4 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2051 mL | 11.0254 mL | 22.0507 mL | 55.1268 mL |
5 mM | 0.441 mL | 2.2051 mL | 4.4101 mL | 11.0254 mL | |
10 mM | 0.2205 mL | 1.1025 mL | 2.2051 mL | 5.5127 mL | |
20 mM | 0.1103 mL | 0.5513 mL | 1.1025 mL | 2.7563 mL | |
50 mM | 0.0441 mL | 0.2205 mL | 0.441 mL | 1.1025 mL | |
100 mM | 0.0221 mL | 0.1103 mL | 0.2205 mL | 0.5513 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。
GW 501516 317318-70-0 Autophagy DNA Damage/DNA Repair Metabolism PPAR GW-501516 Inhibitor Peroxisome proliferator-activated receptors GSK 516 Cardarine GW1516 GW501516 inhibit GW 1516 GSK-516 Endurobol GSK516 GW-1516 inhibitor