GW7647

GW7647 価格

GW7647 化学特性,用途語,生産方法

• 説明

  Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis. Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. GW 7647 is a potent, selective agonist of human and murine PPARα It activates human PPARα, PPARγ, and PPARδ with EC₅₀ values of 0.006, 1.1 and 6.2 μM, respectively, in a GAL4-PPAR binding assay. Similar EC₅₀ values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.

• 使用

  GW7647 has been used as a peroxisome proliferator-activated receptor α (PPAR α) ligand:
  
  • in defatting medium to treat primary human hepatocytes
  • to test its effect on the glycolytic function in cardiomyocytes
  • to test its effect on infant mouse heart
  • in breast cancer MDA-MB-231 cells to activate PPARs
  
  

• 定義

  ChEBI: A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.

• 一般的な説明

  A cell-permeable urea-substituted thioisobutyric acid (ureido-TiBA) compound that acts as a potent and selective PPARα agonist (PPARα, γ and δ - EC₅₀ = 6 nM, 1.1 μM and 6.2 μM for human; 1 nM, 1.3 μM and 2.9 μM for murine, respectively). Also displays in vivo lipid-lowering activity in rats.

• 生物活性

  Potent and highly selective PPAR α agonist (EC 50 values are 6, 1100 and 6200 nM for human PPAR α , PPAR γ and PPAR δ receptors respectively). Modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubules in vitro . Has lipid-lowering effects following oral administration in vivo .

GW7647 生産企業

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265129-71-3, GW7647 キーワード