PE859 is a potent Aβ aggregation inhibitor with IC50 values of 1.2μM and 0.66μM for Aβ aggregation and Tau aggregation. PE859 exhibited improved pharmacokinetic profile and brain permeability through oral administration. A four-week oral administration of PE859 at doses of 20 and 40 mg/kg/day significantly reduced the amount of sarkosyl-insoluble tau in the brain of JNPL3 human tau P301L transgenic mice[3]. PE859 inhibited the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner with IC50 values of 0.81 μM and 2.23 μM, respectively, in in vitro assay. Oral administration of PE859 at dose of 40mg/kg/day for 6 months delayed onset and progression of the motor dysfunction and reduced the amount of sarcosyl-insoluble tau in the spinal cord of JNPL3 mice[4].
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