Catalog Number: 2870
Chemical Name: 2-[(1R)-1-[[(4-Chlorophenyl)sulfonyl](2,5-difluorophenyl)amino]ethyl-5-fluorobenzenebutanoic acid
Biological Activity
Orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Exhibits no Notch toxicity. Brain penetrant.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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.
Background References
  1. Dynamics of β-Amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor.
    Barten et al.
    J.Pharmacol.Exp.Ther., 2005;312:635
  2. Reductions in β-amyloid concentrations in vivo by the γ-secretase inhibitors BMS-289948 and BMS-299897.
    Anderson et al.
    Biochem.Pharmacol., 2005;69:689
  3. Ex vivo occupancy of the γ-secretase inhibitors correlates with brain β-amyloid peptide reduction in Tg2576 mice.
    Goldstein et al.
    J.Pharmacol.Exp.Ther., 2007;323:102
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