| 产品描述： | AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively. |
| 靶点： |
GSK-3α:8.2 (pKi);GSK-3β:7.5 (pKi);cdk5:6.4 (pKi);cdk2:5.9 (pKi);cdk1:5.7 (pKi);GSK-3 |
| 体内研究： |
The pharmacokinetic analysis in blood after oral administration revealed that AZD1080 has a good oral bioavailability in rats (15-24%) with a half-life of 7.1 h, making AZD1080 attractive for further in vivo testing. The subchronic (3 days) oral treatment with AZD1080 at 4 or 15 μmol/kg significantly blocked the MK-801-induced memory deficit (AZD1080 vs. MK-801, p<0.05 at 4 μmol/kg and p<0.01 at 15 μmol/kg) in mice, raising the hypothesis that longer treatment may be required to prime the synapses to function effectively |
| 参考文献： |
1. Georgievska B, et al. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J Neurochem. 2013 May;125(3):446-56. |
| 溶解性： |
DMSO : 21.35 mg/mL (63.85 mM; Need ultrasonic and warming) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.991 ml |
14.953 ml |
29.907 ml |
| 5 mM |
0.598 ml |
2.991 ml |
5.981 ml |
| 10 mM |
0.299 ml |
1.495 ml |
2.991 ml |
| 50 mM |
0.06 ml |
0.299 ml |
0.598 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京