您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > GKA50 quarterhydrate
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 quarterhydrate
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 quarterhydrate图片
包装:5mg
市场价:4680元

产品介绍
GKA50quarterhydrate是一种有效的葡萄糖激酶(glucokinase)激活剂(EC50=33nM)。GKA50quarterhydrate刺激小鼠胰岛和MIN6细胞分泌胰岛素。GKA50quarterhydrate对高脂高脂脂肪雌性大鼠有显著的降糖作用。
Canonical SMILESO=C(C1=CC=C(NC(C2=CC(O[C@@H](C)CC3=CC=CC=C3)=CC(O[C@@H](C)COC)=C2)=O)N=C1)O.[1/4].O
分子式C26H28N2O6.¼H2O
分子量469.01
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 quarterhydrate stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats[1][2].

GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50 values 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 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[2]. Cell Proliferation Assay[2] Cell Line: INS-1 cells (starved overnight with 3 μM glucose)

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]

[1]. Coope GJ, et al. Predictive blood glucose lowering efficacy by Glucokinase activators in high fat fed female Zucker rats. Br J Pharmacol. 2006 Oct;149(3):328-35. [2]. McGlasson L, et al. The glucokinase activator GKA50 causes an increase in cell volume and activation of volume-regulated anion channels in rat pancreatic β-cells. Mol Cell Endocrinol. 2011 Aug 6;342(1-2):48-53.