PE859

Research use only, not for human use.

PE859 is a novel, orally active tau aggregation inhibitor that inhibits the heparin-induced aggregation of both 3RMBD and full length tau with IC50 of 0.81 uM and 2.23 uM, respectively.

PE859 is a novel, orally active tau aggregation inhibitor that inhibits the heparin-induced aggregation of both 3RMBD and full length tau with IC50 of 0.81 uM and 2.23 uM, respectively; also inhibits amyloid β (Aβ) aggregation with IC50 of 1.2 uM; significantly reduces sarkosyl-insoluble aggregated tau along with the prevention of onset and progression of the motor dysfunction in JNPL3 P301L-mutated human tau transgenic mice.

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.

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.

PE-859 | PE 859

Others

Amyloids

Aβ|tau|Microtubule

Neurological Disease

——

1402727-29-0

448.5157

C28H24N4O2

>98% (HPLC)

DMSO: ≥ 30 mg/mL

COC1=CC(OCC2=NC=CC=C2)=CC=C1/C=C/C3=CC(/C=C/C4=CC5=C(C=C4)C=CN5)=NN3

1H-Indole, 6-[(1E)-2-[5-[(1E)-2-[2-methoxy-4-(2-pyridinylmethoxy)phenyl]ethenyl]-1H-pyrazol-3-yl]ethenyl]-

(-20℃)

With Ice Pack

≥ 2 years