First high potency synthetic agonist at GPR40.
GPR40 was formerly an orphan GPCR whose endogenous ligands have been shown to be free fatty acids and has therefore been designated the free fatty acid receptor 1 (FFAR1). It is abundantly expressed on insulin-expressing beta cells and has been shown to mediate the majority of the effects of free fatty acids on insulin secretion. GW9508 enhanced insulin secretion in INS-1E cells and activates ATP-sensitive potassium channels in rat pancreatic beta cells (40μM). It is a useful tool for exploring the biology of GPR40 mediated signaling and physiology.
Product Details
| Alternative Name: | 4-[[(3-Phenoxyphenyl)methyl]amino]benzene propanoic acid |
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| Formula: | C22H21NO3 |
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| MW: | 347.4 |
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| CAS: | 885101-89-3 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | Off-white solid. |
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| Solubility: | Soluble in DMSO (15mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | Ambient |
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| Use/Stability: | Stable for 1 year as supplied. Solutions can be stored at -20°C for up to 3 months. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells: M. Yang, et al.; Mol. Cell. Endocrinol.
315, 308 (2010),
Abstract;
Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signaling pathway: Y.F. Zhao, et al.; J. Endocrinol.
198, 533 (2008),
Abstract;
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40 : identification of agonist and antagonist small molecules: C.P. Briscoe, et al.; Br. J. Pharmacol.
148, 619 (2006),
Abstract;
Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40: Y. Itoh, et al.; Nature
422, 173 (2003),
Abstract;
