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AZD1080,612487-72-6

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  • ¥351 - 5663
  • MedChemExpress(MCE)已认证
  • 美国
  • HY-13862
  • 2025年12月05日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

    • 库存

      货期:1-2天

    • 供应商

      MedChemExpress LLC

    • CAS号

      612487-72-6

    • 规格

      10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg/100 mg

    规格:10 mM * 1 mL产品价格:¥660.0
    规格:1 mg产品价格:¥351.0
    规格:5 mg产品价格:¥900.0
    规格:10 mg产品价格:¥1500.0
    规格:50 mg产品价格:¥4500.0
    规格:100 mg产品价格:¥5663.0

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    AZD1080

    CAS No. : 612487-72-6

    MCE 国际站:AZD1080

    产品活性:AZD1080 是一种有效的选择性 GSK3 抑制剂。AZD1080 抑制重组人 GSK3αGSK3βpKi (IC50) 分别为 8.2 (6.9 nM) 和 7.5 (31 nM)。

    研究领域:PI3K/Akt/mTOR  |  Stem Cell/Wnt

    作用靶点:GSK-3

    In Vitro: AZD1080 shows selectivity against cdk2 (pKi=5.9; 1150 nM; 37-fold), cdk5 (pKi=6.4; 429 nM; 14-fold), cdk1 (pKi=5.7; 1980 nM; 64-fold) and Erk2 (pKi< 5; >10 μM; >323-fold). AZD1080 (at 10 μM) is also evaluated for pan-kinase selectivity and showed good overall selectivity versus 23 kinases, as well as against 65 different receptors, enzymes and ion channels in MDS Pharma screen (< 50% effect at 10 μM AZD1080). Concentration-dependent inhibition of tau phosphorylation is observed for AZD1080 (IC50=324 nM) and the non-selective reference GSK3 inhibitor LiCl (IC50=1.5 mM) indicating that AZD1080 is several orders of magnitude more potent than LiCl.

    In Vivo: The pharmacokinetic analysis in blood after oral administration revealed that AZD1080 has a good oral bioavailability in rats (15-24%) with a half-life of 7.1 h, making AZD1080 attractive for further in vivo testing. The subchronic (3 days) oral treatment with AZD1080 at 4 or 15 μmol/kg significantly blocked the MK-801-induced memory deficit (AZD1080 vs. MK-801, p<0.05 at 4 μmol/kg and p<0.01 at 15 μmol/kg) in mice, raising the hypothesis that longer treatment may be required to prime the synapses to function effectively.

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