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。
| 生物活性 | GSK137647A (GSK 137647) is a potent, selectivefree fatty acid receptor4(FFA4) agonist withpEC50values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, andpEC50values< 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A inducesinsulinsecretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response[1][2]. |
体外研究
(In Vitro) | 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[1].
GSK137647A (GSK 137647) (50 μM) increases glucose stimulated insulin secretion[2].
Western Blot Analysis[1] | 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[1] | Cell Line: | RAW264.7 macrophages | | Concentration: | 10, 20 and 50 μM | | Incubation Time: | 24 hours | | Result: | Without affected cell viability. |
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体内研究
(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[1].
GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) restores intestinal permeability in vivo[1].
| Animal Model: | Male C57BL/6 mice[1] | | 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[1] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; twice daily, for 7 days | | Result: | Decreased the amount of FITC and alleviated intestinal epithelial barrier permeability. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(327.45 mM) H2O : mg/mL (ultrasonic;warming)(Need ultrasonic and warming) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.2745 mL | 16.3725 mL | 32.7450 mL | | 5 mM | 0.6549 mL | 3.2745 mL | 6.5490 mL | | 10 mM | 0.3275 mL | 1.6373 mL | 3.2745 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
