BEGACESTAT
- CAS号:769169-27-9
- 英文名:Begacestat
- 中文名:BEGACESTAT
- CBNumber:CB72535664
- 分子式:C9H8ClF6NO3S2
- 分子量:391.74
- MOL File:769169-27-9.mol
- 熔点 :153-155°C
- 沸点 :355℃
- 密度 :1.642
- 闪点 :169℃
- 储存条件 :2-8°C
- 溶解度 :DMSO: ≥15mg/mL
- 形态 :powder
- 酸度系数(pKa) :8.16±0.50(Predicted)
- 颜色 :white to tan
- WGK Germany :3
BEGACESTAT性质、用途与生产工艺
- 生物活性 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。
-
靶点
IC50: 15 nM (Aβ 40 ).
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体内研究
Begacestat (5 mg/kg, p.o. in mice) treatment for 4 h significantly reduces the Aβ 40 and Aβ 42 in brain (37% lowering of brain Aβ 40 and 25% lowering of Aβ 40 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.Animal Model: Tg2576 mice 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 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.
- 更新日期：2024/11/08
- 产品编号：HY-14175
- 产品名称：BEGACESTAT Begacestat
- CAS编号：769169-27-9
- 包装：1mg
- 价格：800元
- 更新日期：2024/11/08
- 产品编号：HY-14175
- 产品名称：BEGACESTAT Begacestat
- CAS编号：769169-27-9
- 包装：10mM * 1mLin DMSO
- 价格：1100元
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
