产品描述: | GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy. |
靶点: |
GSK-3β:4.9 nM;GSK-3 |
体内研究: |
GSK-3β inhibitor 1(compound 3a) inhibits GSK-3β with IC50 4.19 nM. In a cell-based assay 3a shows no significant leucocyte toxicity at 10 M and is moderately cytotoxic against A549 cells. Compound 3a demonstrated high antidiabetic efficacy in obese streptozotocin-treated rats improving glucose tolerance at a dose of 50 mg/kg body weight thus representing an interesting lead for further optimization. |
参考文献: |
1. Lozinskaya NA, et al. Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3β inhibitors. Bioorg Med Chem. 2019 May 1;27(9):1804-1817. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
4.5 ml |
22.498 ml |
44.996 ml |
5 mM |
0.9 ml |
4.5 ml |
8.999 ml |
10 mM |
0.45 ml |
2.25 ml |
4.5 ml |
50 mM |
0.09 ml |
0.45 ml |
0.9 ml |
|
注意: |
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