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  • AZD1080

    • AZD 1080,AZD-1080
    货号: abs810379
    CAS号: 612487-72-6
    分子式: C19H18N4O2
    分子量: 334.37
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810379-5mg 1-2周 ¥2463.00
    - +
    abs810379-10mg 1-2周 ¥3513.00
    - +
    abs810379-50mg 1-2周 ¥8127.00
    - +
    abs810379-100mg 1-2周 ¥11610.00
    - +
    大包装询价
    产品描述
    描述
    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.
    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    AZD 1080,AZD-1080
    外观
    Powder
    可溶性/溶解性
    DMSO 52 mg/mL (155.51 mM)






    生物活性
    靶点
    GSK-3α ,GSK-3β
    In vitro(体外研究)
    AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with a Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against cdk2, cdk5, cdk1 and Erk2. AZD1080 inhibits tau phosphorylation in cells expressing human tau, with IC50 of 324 nM.
    In vivo(体内研究)
    AZD1080 inhibits tau phosphorylation in rat brain after oral dministration, with brain/plasma exposure ratio of 0.5 – 0.8 at peak concentrations. AZD1080 reverses cognitive deficits and rescues dysfunctional synapses in mice. Acute oral treatment with AZD1080 inhibits peripheral GSK3 activity, produces a dose-dependent reduction of the phosphorylated to total glycogen synthase (GS) ratio, with a mean maximal inhibitory effect of 49% at the highest dose (10 μmol/kg) at 2 h after dosing.
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