化合物GW501516 T6151

Product Introduction
Bioactivity


英文名: GW 501516

描述: 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。

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].

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.

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].

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

溶解度: DMSO : 45.4 mg/mL(100 mM)


关键字: GW-501516 | Inhibitor | Peroxisome proliferator-activated receptors | GSK 516 | PPAR | GW 501516 | GW1516 | inhibit | Autophagy | GSK516 | GW-1516

相关产品: Alpinetin | Palmitoylethanolamide | Isosilybin A | EPI-001 | Chiglitazar | GQ-16 | GW590735 | MCC-555 | Fenofibric acid | Ficusin A

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Nuclear Receptor Compound Library | Lipid Metabolism Compound Library | Stem Cell Differentiation Compound Library

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