|2-(4-(((2-(3-氟-4-(三氟甲基)苯基)-4-甲基-噻唑-5-基)甲基)硫基)-2-甲基苯氧基)乙酸|CsnPharm

CAS No.: 317318-84-6

GW0742 Catalog No. CSN13142

Synonyms: GW610742

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.

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靶点选择性

生物活性

实验方案

技术信息

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1209 mL
- 10.6047 mL
- 21.2094 mL
- 5 mM
- 0.4242 mL
- 2.1209 mL
- 4.2419 mL
- 10 mM
- 0.2121 mL
- 1.0605 mL
- 2.1209 mL

技术信息

CAS号

317318-84-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H17F4NO3S2

运输

蓝冰

分子量

471.49

别名

GW610742

溶解度

DMSO	215.0 mg/mL (456.0 mM)
Water	insoluble

动物实验配方

2% DMSO+40% PEG 300+2% Tween 80+water

3 mg/mL

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GW0742 Catalog No. CSN13142

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