GSK137647A,349085-82-1

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GSK137647A

CAS No. : 349085-82-1

MCE 国际站：GSK137647A

产品活性：GSK137647A (GSK 137647) 是一种有效的选择性游离脂肪酸受体4激动剂 (FFA4)，对于人、小鼠和大鼠的 FFA4，其 pEC₅₀ 值分别为 6.3、6.2 和 6.1，对于FFA1、FFA2 和 FFA3，pEC₅₀ 值分别 < 4.5。GSK137647A 具有抗炎活性。GSK137647A 诱导胰岛素分泌并抑制上皮离子转运。GSK137647A 与调节葡萄糖稳态和抗炎反应有关。

研究领域：GPCR/G Protein

作用靶点：Free Fatty Acid Receptor

In Vitro: GSK137647A (GSK 137647) (50 µM) reduces the production of NO in macrophages without affecting cell viability.
GSK137647A (GSK 137647) (30 µM; 12 hours) alleviates response to inflammatory stimuli in Caco-2 cells and induces secretion of IL-6.
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.

In Vivo: 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.

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