Itanapraced

Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC₅₀ values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease^[1][2]. IC50 & Target:IC50 value: 3.6 μM (Aβ42), 18.4 μM (Aβ40)^[1] In Vitro: Itanapraced (0.03-100 μM) inhibits Aβ secretion in human neuroglioma cells (H4swe) expressing APPswe with IC₅₀ values of 3.6 and 18.4 μM for Aβ42 and Aβ40, respectively^[1].
Itanapraced (5-200 μM) inhibits Notch processing in HEK293swe cells with concentrations over 15 μM^[1].
Itanapraced (0-1000 μM; 30 min) dose-dependently inhibits the action potential with an IC₅₀ value of 106 μM^[2].
Itanapraced (30-100 μM) dose-dependently inhibits excitatory synaptic transmission^[2].
Itanapraced (1-10 μM) significantly reduces cell apoptosis in hippocampal neurons induced by oxygen and glucose deprivation (OGD)^[2]. In Vivo: Itanapraced (oral administration; 375 ppm in the diet for 17 weeks) decreases Aβ42 and Aβ40 levels, and brain plaque burden in Tg2576 transgenic mice^[1].