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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
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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
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0187
Product name
GSI-953
Purity
≥98% (HPLC)
Packaging
5mg
Price
$132
Updated
2024/03/01
Sigma-Aldrich
Product number
PZ0187
Product name
GSI-953
Purity
≥98% (HPLC)
Packaging
25mg
Price
$516
Updated
2024/03/01
Cayman Chemical
Product number
27916
Product name
Begacestat
Packaging
1mg
Price
$56
Updated
2024/03/01
Cayman Chemical
Product number
27916
Product name
Begacestat
Packaging
5mg
Price
$124
Updated
2024/03/01
Tocris
Product number
4283
Product name
Begacestat
Purity
≥98%(HPLC)
Packaging
10
Price
$212
Updated
2021/12/16
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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

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Begacestat Suppliers

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769169-27-9, BegacestatRelated Search:


  • Begacestat
  • Begacestat(GSI-953)
  • GSI-953
  • 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxyMethyl)-2-(trifluoroMethyl)propyl]-2-thiophenesulfonaMide
  • (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] thiophene-2-sulfonamide
  • 2-Thiophenesulfonamide, 5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-
  • Begacestat (Synonyms: GSI-953)
  • GSI-953 DISCONTINUED
  • 769169-27-9
  • C9H8ClF6NO3S2
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pfizer Compounds
  • Pharmaceuticals
  • Sulfur & Selenium Compounds