Biological Activity
Potent and highly selective PPARα agonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively). Modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubules in vitro. Has lipid-lowering effects following oral administration in vivo. Reduces NO production in macrophages; exhibits anti-inflammatory properties.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
GW 7647 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 502.75 |
| Formula | C29H46N2O3S |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 265129-71-3 |
| PubChem ID | 3392731 |
| InChI Key | PKNYXWMTHFMHKD-UHFFFAOYSA-N |
| Smiles | CC(C)(SC1=CC=C(CCN(CCCCC2CCCCC2)C(=O)NC2CCCCC2)C=C1)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.27 | 100 | |
| ethanol | 12.57 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 502.75. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.99 mL | 9.95 mL | 19.89 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.98 mL |
| 10 mM | 0.2 mL | 0.99 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Brown et al (2001) Identification of a subtype selective human PPARα agonist through parallel-array synthesis. Bioorg.Med.Chem.Lett. 11 1225 PMID: 11354382
Cunard et al (2002) Regulation of cytokine expression by ligands of peroxisome proliferator activated receptors. J.Immunol. 168 2795 PMID: 11884448
Muoio et al (2002) Peroxisome proliferator-activated receptor-α regulates fatty acid utilization in primary human skeletal muscle cells. Diabetes 51 901 PMID: 11916905
Paukkeri et al (2007) PPARalpha agonists inhibit nitric oxide production by enhancing iNOS degradation in LPS-treated macrophages. Br.J.Pharmacol. 152 1081 PMID: 17891158
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