GW0742
产品说明书
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同义名 : | GW610742 |
| CAS号 : | 317318-84-6 | |
| 货号 : | A469160 | |
| 分子式 : | C21H17F4NO3S2 | |
| 纯度 : | 95% | |
| 分子量 : | 471.49 | |
| MDL号 : | MFCD07369423 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
2% DMSO+40% PEG 300+2% Tween 80+water 3 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 描述 | GW0742 is a potent and highly selective PPARδ agonist with EC50 values of 0.001, 1.1 and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively[4]. GW0742 (1 μM) results in an increase in the number of cells in the G1 phase and a decrease in the number of cells in the S phase, preventing cell cycle progression from G1 to S phase[5]. GW0742 leads to inhibition of cell growth likely through the induction of terminal differentiation, but not lead to an anti-apoptotic effect in either human or mouse keratinocytes. GW0742 results in a significant decrease in the level of ERK phosphorylation[5]. PPARβ is implicated in the regulation of genes with potential roles in neurotoxicity[6]. PPARβ activation by GW0742 after 24 hr of exposure, was not inherently toxic to rat cerebellar granule neurons measured with a lactate dehydrogenase release (LDH) assay. However, toxicity was observed after 48 hr, with cell death mediated via an apoptotic mechanism[6]. Treatment with a 7-day GW0742 markedly increased expressions of PPARδ[7]. Increased expressions of FA oxidation and TCA cycle related genes were also observed in the heart of Wistar rats and in the primary cultured cardiomyocytes from neonatal rat[7]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| C2C12 cells | Function assay | 4 days | Agonist activity at PPARdelta in mouse C2C12 cells assessed as upregulation of TFAM gene expression after 4 days by real time PCR analysis | 23273519 | |
| CV-1 cells | Function assay | 24 h | Agonist activity at mouse PPAR-alpha expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay | 21074432 | |
| HEK293 cells | Function assay | Transactivation of PPARdelta (unknown origin) expressed in HEK293 cells co-transfected with PDK4-PPRE by luciferase reporter gene assay | 23273519 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.60mL 2.12mL 1.06mL |
21.21mL 4.24mL 2.12mL |
| 参考文献 |
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