Begacestat

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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)
Datasheet
Citations
Reviews
Literature (3)

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
InChI Key PSXOKXJMVRSARX-SCSAIBSYSA-N
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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References

References are publications that support the biological activity of the product.

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: Begacestat, Begacestat supplier, 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, Amyloid, Beta, Peptides, 4283, Tocris Bioscience

Citations for Begacestat

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