| 溶解性 | DMSO 52 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 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 |
2-羟基-3-[5-[(吗啉-4-基)甲基]吡啶-2-基]-1H-吲哚-5-甲腈(AZD1080)
AZD1080 （订货以英文为准）
编号：A126905
CAS号：612487-72-6
分子式：C19H18N4O2
分子量：334.37
| 产品名称 | AZD1080 |
| 中文名称 | 2-羟基-3-[5-[(吗啉-4-基)甲基]吡啶-2-基]-1H-吲哚-5-甲腈(AZD1080) |
| CAS号 | 612487-72-6 |
| 分子式（M.F.） | C19H18N4O2 |
| 分子量（M.W.） | 334.37 |
| 储存条件 | -20°C储存 |
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