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| Product Name: | GW7647 | | Synonyms: | GW647;GW7647;2-(4-(2-(1-CYCLOHEXANEBUTYL)-3-CYCLOHEXYLUREIDO)ETHYL)PHENYLTHIO)-2-METHYLPROPIONIC ACID;2-[[4-[2-[[(CYCLOHEXYLAMINO)CARBONYL](4-CYCLOHEXYLBUTYL)AMINO]ETHYL]PHENYL]THIO]-2-METHYLPROPANOIC ACID;2-((4-(2-(((Cyclohexylamino)carbonyl)-(4-cyclohexylbutyl)amino)ethyl)phenyl)thio)-2-methylpropanoicacid;GW 7647X;GWalpha 7647;Propanoic acid, 2-[[4-[2-[[(cyclohexylaMino)carbonyl](4-cyclohexylbutyl)aMino]ethyl]phenyl]thio]-2-Methyl- | | CAS: | 265129-71-3 | | MF: | C29H46N2O3S | | MW: | 502.75 | | EINECS: | | Product Categories: | Intracellular receptor | | Mol File: | 265129-71-3.mol |
| GW7647 Chemical Properties |
| Melting point | 156 - 157°C | | Boiling point | 693.9±55.0 °C(Predicted) | | density | 1.12 | | storage temp. | Store at RT | | solubility | DMSO: 16 mg/mL, soluble | | form | White solid | | pka | 3.79±0.10(Predicted) | | color | white | | InChIKey | PKNYXWMTHFMHKD-UHFFFAOYSA-N |
| GW7647 Usage And Synthesis |
| Description | 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. | | Uses | 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
| | Uses | GW 7647 is a potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ. It can also be used for regenerative cardiac cell therapies. | | Definition | 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. | | General Description | 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. | | Biological Activity | 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 . | | Biochem/physiol Actions | GW7647 reduces serum triglyceride levels and enhances hepatic expression of genes associated with β-oxidation. Usage of GW7647 along with metformin in conditions of liver steatosis or injury improves the enzymatic levels of aspartate transaminase (AST) and alanine transaminase (ALT) in serum. |
| GW7647 Preparation Products And Raw materials |
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