PE859

PE859 is a potent inhibitor of both tau and Aβ aggregation with IC₅₀ values of 0.66 and 1.2 μM, respectively. IC50 & Target: IC50: 0.66 μM (tau), 1.2 μM (Aβ)^[1] In Vitro: PE859 inhibits the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner. In each assay, the IC₅₀ values calculated at the last measurement periods are 0.81 μM, and 2.23 μM, respectively. PE859 inhibits tau aggregation through formation of beta-sheet structure^[2]. In Vivo: PE859 could cross the blood-brain barrier and that PE859 could be distributed into the tissues of the central nervous system. The maximum concentration of PE859 is 2.005 μg/mL in the blood at 3 h and 1.428 μg/g in the brain at 6 h. PE859 delays onset and progression of the motor dysfunction in JNPL3 mice. PE859 delays progression of the motor dysfunction through the inhibition of accumulation of sarkosyl-insoluble tau. ^[2]