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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 GSK3α 和 GSK3β，pK_i (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 (pK_i=5.9; 1150 nM; 37-fold), cdk5 (pK_i=6.4; 429 nM; 14-fold), cdk1 (pK_i=5.7; 1980 nM; 64-fold) and Erk2 (pK_i< 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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