1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase

Begacestat (Synonyms: GSI-953)

Cat. No.: HY-14175 Purity: >99.0%
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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.

For research use only. We do not sell to patients.

Begacestat Chemical Structure

Begacestat Chemical Structure

CAS No. : 769169-27-9

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Estimated Time of Arrival: December 31
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Description

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].

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.
References
Molecular Weight

391.74

Formula

C₉H₈ClF₆NO₃S₂

CAS No.

769169-27-9

SMILES

FC(F)(F)C([[email protected]](NS(=O)(C1=CC=C(Cl)S1)=O)CO)C(F)(F)F

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >99.0%

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Begacestat
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HY-14175
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Begacestat

Cat. No.: HY-14175