GKA50 quarterhydrate|西域试剂

GKA50 quarterhydrate

产品编号：Bellancom-15671A| 分子式：C₂₆H₂₈N₂O₆.1/4H₂O| 分子量：469.01

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-15671A		￥1850.00	杭州北京（现货）
Bellancom-15671A		￥5500.00	杭州北京（现货）

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GKA50 quarterhydrate

产品介绍

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。

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 Ca²⁺-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats^[4].

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式