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Begacestat

CAS No. : 769169-27-9

MCE 站：Begacestat

产品活性：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 (IC₅₀Aβ₄₀=15 nM)，有潜力用于阿尔兹海默症的研究。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase

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).
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.
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.

相关产品：DAPT  |  YO-01027  |  LY-411575  |  Compound E  |  E 2012  |  L-685458  |  Semagacestat  |  NGP555  |  BMS 299897  |  Sulindac sulfide  |  Z-Ile-Leu-aldehyde  |  gamma-secretase modulator 3  |  BMS 433796

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