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- 详细信息
- 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.
- 英文名：
GSI-953
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
769169-27-9
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1100.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥800.0 |
| 规格： | 5 mg | 产品价格： | ￥1280.0 |
| 规格： | 10 mg | 产品价格： | ￥2050.0 |
| 规格： | 25 mg | 产品价格： | ￥4100.0 |
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Begacestat
CAS No. : 769169-27-9
MCE 国际站：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.
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