ChemicalBook > CAS DataBase List > Begacestat

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