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851884-87-2

中文名称 GKA-50; GKA 50
英文名称 GKA-50
CAS 851884-87-2
分子式 C26H28N2O6
分子量 464.51
MOL 文件 851884-87-2.mol
851884-87-2 结构式 851884-87-2 结构式

基本信息

中文别名
化合物 T11401
英文别名
GKA50
GKA-50
GKA 50
GKA-50
GKA 50
OCBMECSFDVUYQN-ROUUACIJSA-N
6-[[3-[(1S)-2-Methoxy-1-Methylethoxy]-5-[(1S)-1-Methyl-2-phenylethoxy]benzoyl]aMino]-3-pyridinecarboxylic Acid

物理化学性质

储存条件-20°C
溶解度DMSO:可溶15mg/mL,澄清
形态粉末
颜色白色至米色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H413
危险品标志Xn
危险类别码22
WGK Germany3
GKA-50; GKA 50价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-15671GKA-50; GKA 50
GKA50
851884-87-21mg650元
2024/04/30HY-15671GKA-50; GKA 50
GKA50
851884-87-25mg1600元
2024/04/30HY-15671GKA-50; GKA 50
GKA50
851884-87-210mM * 1mLin DMSO1635元

常见问题列表

生物活性
GKA50 是一种有效的葡萄糖激酶 (glucokinase) 激活剂 (EC50=33 nM)。GKA50 刺激小鼠胰岛和 MIN6 细胞分泌胰岛素。GKA50 对高脂高脂脂肪雌性大鼠有显著的降糖作用。
体外研究

GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC 50 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 EC 50 of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC 50 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 EC 50 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.
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