Biological Activity
Potent and highly selective PPARδ agonist. EC50 values are 0.001, 1.1 and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively. Neuroprotective in rat cerebellar granule neuronal cultures after brief (12-hour) exposure but exhibits inherent toxicity after prolonged (48-hour) incubation. Increases rate of fatty acid oxidation and protects against ischemia/reperfusion injury in neonatal and adult cardiomyocytes.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
GW 0742 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 471.49 |
| Formula | C21H17F4NO3S2 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 317318-84-6 |
| PubChem ID | 9934458 |
| InChI Key | HWVNEWGKWRGSRK-UHFFFAOYSA-N |
| Smiles | CC1=C(CSC2=CC(C)=C(OCC(O)=O)C=C2)SC(=N1)C1=CC(F)=C(C=C1)C(F)(F)F |
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 | 48.5 | 100 | |
| ethanol | 24.23 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 471.49. 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 | 2.12 mL | 10.6 mL | 21.21 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.24 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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References
References are publications that support the products' biological activity.
Sznaidman et al (2003) Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - Synthesis and biological activity. Bioorg.Med.Chem.Lett. 13 1517 PMID: 12699745
Smith et al (2004) Effect of the peroxisome proliferator-activated receptor β activator GW0742 in rat cultured cerebellar granule neurons. J.Neurosci.Res. 77 240 PMID: 15211590
Yue et al (2008) In vivo activation of peroxisome proliferator-activayed receptor-δ protects the heart from ischemia/reperfusion injury in Zucker fatty rats. J.Pharm.Exp.Ther. 325 466 PMID:
Keywords: GW 0742, supplier, selective, potent, PPARδ, PPARdelta, agonists, Peroxisome, Proliferator-activating, Receptors, GW0742, GlaxoSmithKline, GSK, PPARdelta, Receptors, PPARdelta, Receptors, Tocris Bioscience
