AZD1080  612487-72-6

AZD-1080
分子式：C19H18N4O2  分子量：334.37
 
產(chǎn)品描述
AZD1080是口服生物有效的，選擇性，可透過(guò)大腦的GSK3抑制劑,抑制人類GSK3α 和GSK3β，Ki分別為6.9 nM 和31 nM, 比作用于CDK2, CDK5, CDK1 和Erk2選擇性高14倍以上。
靶點(diǎn)
           
IC50
           
體外研究
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
體內(nèi)研究
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).
溶解性
DMSO 52 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO