PE859 是 tau 和 Aβ 聚集的有效抑制剂，IC50值分别为 0.66 和 1.2 μM。

PE859 is a potent inhibitor of both tau and Aβ aggregation.

In an Alzheimer's patient's brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid β (Aβ) peptide and Tau Protein, are observed as the two major hallmarks of this disease. 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 the formation of a beta-sheet structure[2].

PE859 is able to cross the blood-brain barrier and thus 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]

PEL cells are incubated in triplicate in a 96-well microculture plate in the presence of different concentrations of methyl-β-cyclodextrin (0-10 mM) in a final volume of 0.1 mL for 24 h at 37°C. Subsequently, MTT (0.5 mg/mL final concentration) is added to each well. After 3 h of additional incubation, 100 μL of a 0.04 N HCl is added to dissolve the crystals. Absorption values at 570 nm are determined.

1402727-29-0

C28H24N4O2

448.526

DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years