AZD1080 612487-72-6
AZD-1080
分子式:C19H18N4O2 分子量:334.37
产品描述
AZD1080是口服生物有效的,选择性,可透过大脑的GSK3抑制剂,抑制人类GSK3α 和GSK3β,Ki分别为6.9 nM 和31 nM, 比作用于CDK2, CDK5, CDK1 和Erk2选择性高14倍以上。
靶点
IC50
体外研究
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
体内研究
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
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO