Begacestat
- Product Name
- Begacestat
- CAS No.
- 769169-27-9
- Chemical Name
- Begacestat
- 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;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
- CBNumber
- CB72535664
- Molecular Formula
- C9H8ClF6NO3S2
- Formula Weight
- 391.74
- MOL File
- 769169-27-9.mol
Begacestat Property
- Melting point:
- 153-155°C
- Boiling point:
- 355℃
- Density
- 1.642
- Flash point:
- 169℃
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥15mg/mL
- form
- powder
- pka
- 8.16±0.50(Predicted)
- color
- white to tan
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- PZ0187
- Product name
- GSI-953
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $132
- Updated
- 2024/03/01
- Product number
- PZ0187
- Product name
- GSI-953
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $516
- Updated
- 2024/03/01
- Product number
- 27916
- Product name
- Begacestat
- Packaging
- 1mg
- Price
- $56
- Updated
- 2024/03/01
- Product number
- 27916
- Product name
- Begacestat
- Packaging
- 5mg
- Price
- $124
- Updated
- 2024/03/01
- Product number
- 4283
- Product name
- Begacestat
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $212
- Updated
- 2021/12/16
Begacestat Chemical Properties,Usage,Production
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. |
Begacestat Preparation Products And Raw materials
Raw materials
Preparation Products
Begacestat Suppliers
- Tel
- --
- Fax
- --
- info@trc-canada.com
- Country
- Canada
- ProdList
- 6038
- Advantage
- 71