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).
Sold with the permission of GlaxoSmithKline
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|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|
References are publications that support the biological activity of the product.
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: GW 9508, GW 9508 supplier, Potent, selective, FFA1, GPR40, agonists, Receptors, Free, Fatty, Acid, GW9508, GlaxoSmithKline, GSK, 2649, Tocris Bioscience
3 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
Watson et al (2012) Differential signaling by splice variants of the human free fatty acid receptor GPR120. Mol Pharmacol 81 631 PMID: 22282525
Do you know of a great paper that uses GW 9508 from Tocris? Please let us know.
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Literature in this Area
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