An inhibitor of γ-secretase
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Begacestat

Item No. 27916

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-2-thiophenesulfonamide
CAS Number
769169-27-9
Synonyms
  • GSI-953
Molecular Formula
C9H8ClF6NO3S2
Formula Weight
391.7
Purity
≥98%
Formulation
A solid
λmax
262 nm
SMILES
OC[C@@H](NS(C1=CC=C(Cl)S1)(=O)=O)C(C(F)(F)F)C(F)(F)F
InChi Code
InChI=1S/C9H8ClF6NO3S2/c10-5-1-2-6(21-5)22(19,20)17-4(3-18)7(8(11,12)13)9(14,15)16/h1-2,4,7,17-18H,3H2/t4-/m1/s1
InChi Key
PSXOKXJMVRSARX-SCSAIBSYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $62

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    5 mg

    $137

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    Product Description

    Begacestat is an inhibitor of γ-secretase that inhibits cleavage of amyloid precursor protein (APP) to amyloid-β (1-40) (Aβ40; Item No. 21617) in vitro (IC50 = 15 nM).1 It is 14-fold selective for γ-secretase over Notch-1. Begacestat (5 mg/kg) reduces brain levels of Aβ40 and Aβ42 (Item No. 20574) in the Tg2576 transgenic mouse model of Alzheimer's disease. It also increases contextual fear conditioning freezing time, indicating reversal of contextual memory deficits, in Tg2576 mice in a dose-dependent manner.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mayer, S.C., Kreft, A.F., Harrison, B., et al. Discovery of begacestat, a Notch-1-sparing γ-secretase inhibitor for the treatment of Alzheimer’s disease. J. Med. Chem. 51(23), 7348-7351 (2008).

    2. Martone, R.L., Zhou, H., Atchison, K., et al. Begacestat (GSI-953): A novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein γ-secretase for the treatment of Alzheimer’s disease. J. Pharmacol. Exp. Ther. 331(2), 598-608 (2009).