您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > GKA50
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
GKA50
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GKA50图片
CAS NO:851884-87-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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.
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.
分子量

464.51

性状

Solid

Formula

C26H28N2O6

CAS 号

851884-87-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 46 mg/mL(99.03 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1528 mL10.7640 mL21.5281 mL
5 mM0.4306 mL2.1528 mL4.3056 mL
10 mM0.2153 mL1.0764 mL2.1528 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。