| Identification | Back Directory | [Name]
Begacestat | [CAS]
769169-27-9 | [Synonyms]
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
5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2- (trifluoromethyl)propyl] thiophene-2-sulfonamide
2-Thiophenesulfonamide, 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-
(2S)-S-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-N-Methyl-3-(trifluoroMethyl)butane-2-sulfonaMido | [Molecular Formula]
C9H8ClF6NO3S2 | [MDL Number]
MFCD18782675 | [MOL File]
769169-27-9.mol | [Molecular Weight]
391.74 |
| Chemical Properties | Back Directory | [Melting point ]
153-155°C | [Boiling point ]
355℃ | [density ]
1.642 | [Fp ]
169℃ | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥15mg/mL | [form ]
powder | [pka]
8.16±0.50(Predicted) | [color ]
white to tan |
| Hazard Information | Back Directory | [Uses]
Begacestat (GSI-953) is a selective β-secretase inhibitor that selectively inhibits cleavage of APP over Notch. GSI-953 is used for treating diseases such as cancer in relation to prevention of intestinal secretory metaplasia. | [Biological Activity]
Begacest at (GSI-953) is a selective γ-secretase inhibitor th at selectively inhibits cleavage of APP over Notch. | [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)[1].
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[2].
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[2]. | Animal Model: | Tg2576 mice[2] | | 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[2] | | 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. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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