Biological Activity
Potent and selective agonist for the free fatty acid receptor FFA1 (GPR40) (pEC50 values are 7.32, < 4.3 and < 4.3 for FFA1, FFA2 and FFA3 receptors respectively). Inactive against a range of other GPCRs, kinases, proteases, integrins and PPARs. Potentiates glucose-stimulated insulin secretion in MIN6 cells (pEC50 = 6.14).
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries
GW 9508 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 347.41 |
| Formula | C22H21NO3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 885101-89-3 |
| PubChem ID | 11595431 |
| InChI Key | DGENZVKCTGIDRZ-UHFFFAOYSA-N |
| Smiles | OC(=O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1 |
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 | 34.74 | 100 | |
| ethanol | 34.74 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 347.41. 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 | 2.88 mL | 14.39 mL | 28.78 mL |
| 5 mM | 0.58 mL | 2.88 mL | 5.76 mL |
| 10 mM | 0.29 mL | 1.44 mL | 2.88 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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References
References are publications that support the products' biological activity.
Garrido et al (2006) Synthesis and activity of small molecule GPR40 agonists. Bioorg.Med.Chem.Lett. 16 1840 PMID: 16439116
Briscoe et al (2006) Pharmacological regulation of insulin secretion in MIN6 cells through fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br.J.Pharmacol. 148 619 PMID: 16702987
Zhao and Chen (2008) Activation of ATP-sensitive potassium channels in rat pancreatic β-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway. J.Endocrinol. 198 533 PMID: 18550787
Keywords: GW 9508, supplier, Potent, selective, FFA1, GPR40, agonists, Receptors, Free, Fatty, Acid, GW9508, GlaxoSmithKline, GSK, Free, Fatty, Acid, Receptors, Free, Fatty, Acid, Receptors, Tocris Bioscience
