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    1. Neuronal Signaling
      Stem Cell/Wnt
    2. γ-secretase

    Begacestat (Synonyms: GSI-953)

    目录号: HY-14175 纯度: >99.0%
    产品使用指南

    Begacestat (GSI-953) 是淀粉样前体蛋白 γ 分泌酶 (gamma-secretase) 的选择性噻吩磺酰胺抑制剂 (IC5040=15 nM),用于阿尔兹海默症的治疗。

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    Begacestat Chemical Structure

    Begacestat Chemical Structure

    CAS No. : 769169-27-9

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    1 mg ¥800 In-stock
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    Description

    Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC5040=15 nM) for the treatment of Alzheimer's disease[1].

    IC50 & Target

    IC50: 15 nM (Aβ40)[1].

    In Vivo

    Begacestat (5 mg/kg, p.o. in mice) treatment for 4 h significantly reduces the Aβ40 and Aβ42 in brain (37% lowering of brain Aβ40 and 25% lowering of Aβ40 observed)[1].
    Begacestat (GSI-953: 0, 2.5, 5, or 10 mg/kg, oral gavage, 3 h) results in a dose-dependent reversal of contextual fear conditioning deficits when compound is orally administered 3 h before training. Significant deficits are observed after treatment with 2.5 mg/kg Begacestat, and there is some reversal of this at 5 mg/kg and full reversal at 10 mg/kg compared with vehicle-dosed Tg2576 mice[2].
    A dosage-related trend of slightly lower percentages of SP CD4+ cells in males at all dosages (SP CD4+ cells=~11% in controls compared with ~7% to ~9% in Begacestat-dosed animals) and females at 2000 mg/kg/day (SP CD4+ cells=~10% in controls compared with ~8% in Begacestat-dosed animals) is observed[2].

    Animal Model: Tg2576 mice[2]
    Dosage: 0, 2.5, 5, or 10 mg/kg
    Administration: Oral gavage for two consecutive days
    Result: Resulted in a dose-dependent reversal of contextual fear conditioning deficits when compound is orally administered 3 h before training.
    Animal Model: Sprague-Dawley rats[2]
    Dosage: 0, 200, 600, or 2000 mg/kg/day for 10 (5 males/group and 5 females at 600 mg/kg/day) or 28 (10/sex/group) consecutive days
    Administration: P.O. for 10 (5 males/group and 5 females at 600 mg/kg/day) or 28 (10/sex/group) consecutive days.
    Result: A dosage-related trend of slightly lower percentages of SP CD4+ cells in males at all dosages and females at 2000 mg/kg/day was observed.
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5527 mL 12.7636 mL 25.5271 mL
    5 mM 0.5105 mL 2.5527 mL 5.1054 mL
    10 mM 0.2553 mL 1.2764 mL 2.5527 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    391.74

    Formula

    C?H?ClF?NO?S?

    CAS No.

    769169-27-9

    SMILES

    FC(F)(F)C([C@H](NS(=O)(C1=CC=C(Cl)S1)=O)CO)C(F)(F)F

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: >99.0%

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

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    产品名称:
    Begacestat
    目录号:
    HY-14175
    需求量:

    Begacestat

    Cat. No.: HY-14175

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