S80835 |
AZD1080 |
源叶(MedMol) | 99% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)