Orally active, potent γ
-secretase inhibitor (IC50
= 12 nM). Inhibits Aβ
40 and Aβ
42 formation in vitro
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.
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.
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.
Reductions in β-amyloid concentrations in vivo by the γ-secretase inhibitors BMS-289948 and BMS-299897.
Anderson et al.
Ex vivo occupancy of the γ-secretase inhibitors correlates with brain β-amyloid peptide reduction in Tg2576 mice.
Goldstein et al.