769169-27-9
基本信息
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
物理化学性质
| 沸点 | 355℃ |
| 密度 | 1.642 |
| 闪点 | 169℃ |
| 储存条件 | 2-8°C |
| 溶解度 | 在DMSO中的溶解度≥15mg/mL |
| 酸度系数(pKa) | 8.16±0.50(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至棕褐色 |
安全数据
| WGK Germany | 3 |
常见问题列表
IC50: 15 nM (Aβ 40 ).
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. |