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Cat.No. 4283 - Begacestat | C9H8ClF6NO3S2 | CAS No. 769169-27-9
Description: γ-secretase inhibitor; lowers Aβ40 and Aβ42 levels
Alternative Names: GSI-953
Chemical Name: 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-2-thiophenesulfonamide
Purity: ≥98% (HPLC)

Biological Activity

γ-secretase inhibitor; selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). Orally active.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries

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Technical Data

M. Wt 391.74
Formula C9H8ClF6NO3S2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 769169-27-9
PubChem ID 11269353
Smiles ClC1=CC=C(S(N[C@H](CO)C(C(F)(F)F)C(F)(F)F)(=O)=O)S1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 39.17 100
ethanol 39.17 100

Preparing Stock Solutions

The following data is based on the product molecular weight 391.74. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.55 mL 12.76 mL 25.53 mL
5 mM 0.51 mL 2.55 mL 5.11 mL
10 mM 0.26 mL 1.28 mL 2.55 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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Product Datasheets

Safety Datasheet


References are publications that support the products' biological activity.

Mayer et al (2008) Discovery of begacestat, a Notch-1-sparing gamma secretase inhibitor for the treatment of Alzheimer's disease. J.Med.Chem. 51 7348 PMID: 19012391

Martone et al (2009) 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. 331 598 PMID: 19671883

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Keywords: GSI953 Begacestat pfizer gamma gamma-secretase γ g-secretase inhibitors inhibits APP amyloid precursor proteins notch AB40 Abeta40 Aβ40 AB42 Abeta42 Aβ42 amyloidbeta amyloidb amyloidβ GSI-953 Gamma-Secretase

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