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GSK-3β inhibitor 2,1702428-31-

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  • 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

      1702428-31-6

    • 规格

      10 mM * 1 mL/5 mg/10 mg/25 mg

    规格:10 mM * 1 mL产品价格:¥3850.0
    规格:5 mg产品价格:¥1750.0
    规格:10 mg产品价格:¥2800.0
    规格:25 mg产品价格:¥5600.0

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    GSK-3β inhibitor 2

    CAS No. : 1702428-31-6

    MCE 国际站:GSK-3β inhibitor 2

    产品活性:GSK-3β inhibitor 2 (Compound 3) 是一种有效,选择性和口服活性的 GSK-3β 抑制剂,IC50 为 1.1 nM。GSK-3β inhibitor 2 可以穿越血脑屏障。GSK-3β inhibitor 2 有用于阿尔茨海默氏病的潜力。

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

    作用靶点:GSK-3

    In Vitro: The pyridine carboxamide of GSK-3β inhibitor 2 (Compound 3) makes hydrogen bonds with the hinge V135 backbone amide, and the carbonyl oxygen of the thiazolyl primary amide formed a critical hydrogen bond with K85. The quality of the electron density for the methyl group of the methoxy moiety in GSK-3β inhibitor 2 does not allow its unambiguous placement in the model, but a small molecule crystal structure of GSK-3β inhibitor 2 determined by single crystal X-ray diffraction method confirmed the intramolecular hydrogen bonding between the methoxy -O- and the amide N-H in GSK-3β inhibitor 2.

    In Vivo: The elevation of hyperphosphorylated Tau (pTau) is mimicked in LaFerla 3xTg-C57BL6 mice, and accordingly, these mice are used as an in vivo model of Alzheimer’s disease. GSK-3β inhibitor 2 (Compound 3) shows a significant reduction in pTau396 when administered orally at 30 mg/kg as a nanosuspension to LaFerla 3xTg-C57BL6 male mice. GSK-3β inhibitor 2 shows only modest brain exposure (B/P = 0.26) as determined as a single time point.

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