GW0742 is an agonist of PPARδ with EC50 of 1.1 nM. It can protect right heart from hypertrophy and enhance lipid metabolism in heart. It also works as an antagonist of vitamin D receptor.
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].
GW0742 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
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