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Submit ReviewGW 9508 is a 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
GW 9508 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 347.41 |
公式 | C22H21NO3 |
储存 | Store at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 34.74 | 100 | |
ethanol | 34.74 | 100 |
以下数据基于产品分子量 347.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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 Ins 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.
关键词: GW 9508, GW 9508 supplier, Potent, selective, FFA1, GPR40, agonists, Receptors, Free, Fatty, Acid, GW9508, GlaxoSmithKline, GSK, 2649, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GW 9508 的部分引用包括:
Oh et al (2010) GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and Ins-sensitizing effects. Cell 142 687 PMID: 20813258
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
Watson et al (2012) Differential signaling by splice variants of the human free fatty acid receptor GPR120. Mol Pharmacol 81 631 PMID: 22282525
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