GKA50 是一种有效的葡萄糖激酶 (glucokinase) 激活剂 (EC50=33 nM)。GKA50 刺激小鼠胰岛分泌胰岛素。GKA50 是啮齿动物和人类胰岛中 β 细胞代谢的葡萄糖样激活剂，以及 Ca2+依赖性胰岛素分泌调节剂。GKA50对高脂喂养的雌性大鼠血糖有显著的降低作用。
| 生物活性 | GKA50 is a potentglucokinaseactivator (EC50=33 nM at 5 mM glucose). GKA50 stimulatesinsulinrelease from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca2+-dependent modulator ofinsulinsecretion. GKA50 shows significant glucose lowering in high fat fed female rats[1][2][3][4]. |
体外研究
(In Vitro) | GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50values ranging from 1 to 2 μM[2].
GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells[2].
GKA50 activates human glucokinase enzymatic activity with an EC50of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC50of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD[2].
Cell Proliferation Assay[2] | Cell Line: | INS-1 cells (starved overnight with 3 μM glucose) | | Concentration: | 0.01-100 μM | | Incubation Time: | 24 hours | | Result: | Stimulated cell proliferation in a dose-dependent manner, with EC50values ranging from 1 to 2 μM. |
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体内研究
(In Vivo) | GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test[1].
| Animal Model: | High-fat-fed obese female Zucker (fa/fa) rats[1] | | Dosage: | 1, 3, 10, 30 mg/kg | | Administration: | Oral administration | | Result: | Significant percentage glucose lowering. |
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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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 46 mg/mL(99.03 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 2.1528 mL | 10.7640 mL | 21.5281 mL | | 5 mM | 0.4306 mL | 2.1528 mL | 4.3056 mL | | 10 mM | 0.2153 mL | 1.0764 mL | 2.1528 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。 |
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