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).
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|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
If you know of a relevant reference for GW 9508, please let us know.
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Keywords: Potent selective FFA1 GPR40 agonists Receptors Free Fatty Acid GW9508 GlaxoSmithKline GSK Free Fatty Acid Receptors
2 Citations for GW 9508
Citations are publications that use Tocris products. Selected citations for GW 9508 include:
Dragano (2017) Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation. J Neuroinflammation 14 91 PMID: 28446241
Oh et al (2010) GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects. Cell 142 687 PMID: 20813258
Do you know of a great paper that uses GW 9508 from Tocris? If so please let us know.