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Begacestat

Catalog No. T14525   CAS 769169-27-9
Synonyms: GSI-953

Begacestat is a selective thiophene sulfonamide amyloid precursor protein gamma-secretase inhibitor (Aβ40,IC50=15 nM),and for the treatment of Alzheimer's disease.

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Begacestat Chemical Structure
Begacestat, CAS 769169-27-9
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Biological Description
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Description Begacestat is a selective thiophene sulfonamide amyloid precursor protein gamma-secretase inhibitor (Aβ40,IC50=15 nM),and for the treatment of Alzheimer's disease.
Targets&IC50 Aβ40:15 nM
In vivo 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. 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]. 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]. 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].
Synonyms GSI-953
Molecular Weight 391.74
Formula C9H8ClF6NO3S2
CAS No. 769169-27-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Mayer SC, et al. Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease. J Med Chem. 2008 Dec 11;51(23):7348-51. 2. Martone RL, et al. Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. J Pharmacol Exp Ther. 2009 Nov;331(2):598-608.

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Keywords

Begacestat 769169-27-9 Neuroscience Beta Amyloid GSI953 GSI-953 GSI 953 inhibitor inhibit

 

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