GKA50 quarterhydrate
目录号 : KM7131

GKA50 quarterhydrate 是一种有效的葡萄糖激酶 (glucokinase) 激活剂 (EC50=33 nM)。GKA50 quarterhydrate 刺激小鼠胰岛分泌胰岛素。GKA50 quarterhydrate 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 quarterhydrate 对高脂喂养的雌性大鼠血糖有显著的降低作用。

规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg 询价 In-stock
50mg 询价 In-stock
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生物活性

GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.

体外研究

GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50 values ranging from 1 to 2 μM.
GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells.
GKA50 activates human glucokinase enzymatic activity with an EC50 of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC50 of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD.

Cell Proliferation Assay

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 EC50 values ranging from 1 to 2 μM.
体内研究

GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test.

Animal Model: High-fat-fed obese female Zucker (fa/fa) rats
Dosage: 1, 3, 10, 30 mg/kg
Administration: Oral administration
Result: Significant percentage glucose lowering.
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
溶解性数据
In Vitro: 

DMSO : 46 mg/mL (98.08 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1322 mL 10.6608 mL 21.3215 mL
5 mM 0.4264 mL 2.1322 mL 4.2643 mL
10 mM 0.2132 mL 1.0661 mL 2.1322 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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