产品介绍 |
AZD1080是口服活性的可通透脑屏障的GSK3α和GSK3β抑制剂,Ki分别为6.9 nM和31 nM。 |
备注 |
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. |
生化机理 |
Description: IC50 Value: 31 nM [1] AZD1080 is a potent and selective GSK3 inhibitor that demonstrates peripheral target engagement in Phase 1 clinical studies. in vitro: AZD1080 inhibits tau phosphorylation in cells expressing human tau and in intact rat brain. Interestingly, subchronic but not acute administration with AZD1080 reverses MK-801-induced deficits, measured by long-term potentiation in hippocampal slices and in a cognitive test in mice, suggesting that reversal of synaptic plasticity deficits in dysfunctional systems requires longer term modifications of proteins downstream of GSK3β signaling [1]. in vivo: AZD1080 reverses MK-801-induced impairments in mouse model of cognition. AZD1080 treatment significantly prevents MK-801-induced deficits at both time-points (*p < 0.05; **p < 0.01).Data are presented as mean _ SEM (n = 9-12 subjects/group). [1] Clinical trial: Phase 1 |
别名 |
2-羟基-3-[5-[(吗啉-4-基)甲基]吡啶-2-基]-1H-吲哚-5-甲腈;HY-13862; AZD-1080; AZD 1080;2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile |