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GSK137647A 99%

GSK137647A

源叶(MedMol)
S85041
349085-82-1
C16H19NO3S
305.392
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S85041-2mg 99% ¥100.00元 5 - - -
源叶(MedMol) S85041-5mg 99% ¥200.00元 5 - - -
源叶(MedMol) S85041-10mg 99% ¥350.00元 6 - - -
源叶(MedMol) S85041-25mg 99% ¥500.00元 预计交期:2-3天 - - -
源叶(MedMol) S85041-50mg 99% ¥800.00元 预计交期:2-3天 - - -
源叶(MedMol) S85041-100mg 99% ¥1400.00元 预计交期:2-3天 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

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
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;GPR
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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参考文献

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