BEGACESTAT
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- CAS号:
- 769169-27-9
- 英文名:
- Begacestat
- 英文别名:
- GSI-953;Begacestat;Begacestat(GSI-953);GSI-953
DISCONTINUED;Begacestat (Synonyms: GSI-953);5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxyMethyl)-2-(trifluoroMethyl)propyl]-2-thiophenesulfonaMide;2-Thiophenesulfonamide, 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-;5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2- (trifluoromethyl)propyl] thiophene-2-sulfonamide;(2S)-S-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-N-Methyl-3-(trifluoroMethyl)butane-2-sulfonaMido
- 中文名:
- BEGACESTAT
- 中文别名:
- 贝加塞特;化合物 T14525;化合物 BEGACESTAT;5-氯-N-[(1S)-3,3,3-三氟-1-(羟基甲基)-2-(三氟甲基)丙基]-2-噻吩磺酰胺
- CBNumber:
- CB72535664
- 分子式:
- C9H8ClF6NO3S2
- 分子量:
- 391.74
- MOL File:
- 769169-27-9.mol
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BEGACESTAT化学性质
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熔点:
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153-155°C
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沸点:
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355℃
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密度:
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1.642
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闪点:
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169℃
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储存条件:
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2-8°C
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溶解度:
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DMSO: ≥15mg/mL
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形态:
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powder
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酸度系数(pKa):
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8.16±0.50(Predicted)
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颜色:
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white to tan
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BEGACESTAT性质、用途与生产工艺
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。
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.
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Animal Model:
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Tg2576 mice
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Dosage:
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0, 2.5, 5, or 10 mg/kg
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Administration:
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Oral gavage for two consecutive days
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Result:
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Resulted in a dose-dependent reversal of contextual fear conditioning deficits when compound is orally administered 3 h before training.
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Animal Model:
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Sprague-Dawley rats
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Dosage:
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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
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Administration:
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P.O. for 10 (5 males/group and 5 females at 600 mg/kg/day) or 28 (10/sex/group) consecutive days.
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Result:
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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.
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BEGACESTAT
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/11/08 | HY-14175 | BEGACESTAT
Begacestat | 769169-27-9 | 1mg | 800元 |
| 2024/11/08 | HY-14175 | BEGACESTAT
Begacestat | 769169-27-9 | 10mM * 1mLin DMSO | 1100元 |
769169-27-9, BEGACESTAT 相关搜索:
- Sulfur & Selenium Compounds
- Pharmaceuticals
- Pfizer Compounds
- Intermediates & Fine Chemicals
- Inhibitors
- Heterocycles
- 抑制剂
- C9H8ClF6NO3S2
- 化合物 BEGACESTAT
- 化合物 T14525
- 贝加塞特
- 5-氯-N-[(1S)-3,3,3-三氟-1-(羟基甲基)-2-(三氟甲基)丙基]-2-噻吩磺酰胺
- 769169-27-9
- GSI-953
DISCONTINUED
- Begacestat (Synonyms: GSI-953)
- 2-Thiophenesulfonamide, 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-
- 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2- (trifluoromethyl)propyl] thiophene-2-sulfonamide
- (2S)-S-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-N-Methyl-3-(trifluoroMethyl)butane-2-sulfonaMido
- 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxyMethyl)-2-(trifluoroMethyl)propyl]-2-thiophenesulfonaMide
- GSI-953
- Begacestat(GSI-953)
- Begacestat