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769169-27-9 | Begacestat

Begacestat NLT 98%

SKU : MC571082

CAS Number : 769169-27-9

Molecular Formula : C9H8ClF6NO3S2 | Molecular Weight : 391.74

Synonyms : GSI-953

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name Begacestat
CAS Number 769169-27-9
MDL Number MFCD18782675
Molecular Formula C9H8ClF6NO3S2
Molecular Weight 391.74
Synonyms GSI-953
Introduction of 769169-27-9 :

Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC5040=15 nM) for the treatment of Alzheimer's disease[1]. IC50 & Target: IC50: 15 nM (Aβ40)[1]. 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].

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