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GW 501516

GW 501516

产品编号 T6151   CAS 317318-70-0
别名: Cardarine, GW501516, GW 1516, GSK-516, Endurobol

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。

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GW 501516 Chemical Structure
GW 501516, CAS 317318-70-0
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
产品目录号及名称: GW 501516 (T6151)
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纯度: 99.94%
纯度: 98.91%
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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 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

存储

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

溶解度

DMSO: 45.4 mg/mL(100 mM)

溶液配制表

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

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. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8. 2. Chen, W., Gao, R., Xie, X., Zheng, Z., Li, H., & Li, S. et al. (2015). A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice. Scientific Reports, 5(1). doi: 10.1038/srep09884

文献引用

1. Han W, Wang N, Kong R, et al. Ligand-activated PPARδ expression promotes hepatocellular carcinoma progression by regulating the PI3K-AKT signaling pathway. Journal of Translational Medicine. 2022, 20(1): 1-14. 2. Ren Q, Xie X, Zhao C, et al. 2, 2′, 4, 4′-Tetrabromodiphenyl Ether (PBDE 47) Selectively Stimulates Proatherogenic PPARγ Signatures in Human THP-1 Macrophages to Contribute to Foam Cell Formation. Chemical Research in Toxicology. 2022
Daltroban Icariin Inolitazone Alliin Kihadanin B Isosilybin A Repaglinide GSK0660

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗衰老化合物库 抗乳腺癌化合物库 人代谢物化合物库 神经退行性疾病化合物库 抗心血管疾病化合物库 抗癌化合物库 DNA 损伤和修复分子库 表型筛选靶点鉴定库

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。
% DMSO
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% ddH2O
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

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

 

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