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• 产品描述： GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response

• 靶点： Free Fatty Acid Receptor

• 体外研究： GSK137647A (GSK 137647) (50 µM) reduces the production of NO in macrophages without affecting cell viability[1].GSK137647A (GSK 137647) (30 µM; 12 hours) alleviates response to inflammatory stimuli in Caco-2 cells and induces secretion of IL-6[1]. GSK137647A (GSK 137647) (10 µM) reduces the ion flow and affects the colonic epithelial ion transport in healthy. GSK137647A (GSK 137647) (50 µM) increases glucose stimulated insulin secretion. Western Blot Analysis Cell Line: Caco-2 cells Concentration: 30 µM Incubation Time: 12 hours Result: Downregulated FFAR1, FFAR2, and FFAR4 as compared to control. Cell Viability Assay Cell Line: RAW264.7 macrophages Concentration: 10, 20 and 50 µM Incubation Time: 24 hours Result: Without affected cell viability.

• 体内研究： GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) alleviates colitis in TNBS- and DSS-treated mice. GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) restores intestinal permeability in vivo. Animal Model: Male C57BL/6 mice Dosage: 1 mg/kg Administration: Intraperitoneal injection; twice daily, for 7 days Result: Had anti-inflammatory effect and reversed colonic injury induced by DSS. Animal Model: Male C57BL/6 mice Dosage: 1 mg/kg Administration: Intraperitoneal injection; twice daily, for 7 days Result: Decreased the amount of FITC and alleviated intestinal epithelial barrier permeability.

• 参考文献：
  1. Salaga M, et, al. Activation of Free Fatty Acid Receptor 4 Affects Intestinal Inflammation and Improves Colon Permeability in Mice. Nutrients. 2021 Aug 6;13(8):2716. 2. Sparks SM, et, al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.274 ml	16.372 ml	32.745 ml
  5 mM	0.655 ml	3.274 ml	6.549 ml
  10 mM	0.327 ml	1.637 ml	3.274 ml
  50 mM	0.065 ml	0.327 ml	0.655 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *