PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.

Product information

CAS Number: 1402727-29-0

Molecular Weight: 448.52

Formula: C28H24N4O2

Chemical Name: 6-[(E)-2-{5-[(E)-2-{2-methoxy-4-[(pyridin-2-yl)methoxy]phenyl}ethenyl]-1H-pyrazol-3-yl}ethenyl]-1H-indole

Smiles: COC1=CC(=CC=C1/C=C/C1=CC(/C=C/C2=CC3NC=CC=3C=C2)=NN1)OCC1C=CC=CN=1

InChiKey: AMBZHNVCLPHAKA-NSJFVGFPSA-N

InChi: InChI=1S/C28H24N4O2/c1-33-28-18-26(34-19-25-4-2-3-14-29-25)12-9-22(28)8-11-24-17-23(31-32-24)10-6-20-5-7-21-13-15-30-27(21)16-20/h2-18,30H,19H2,1H3,(H,31,32)/b10-6+,11-8+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (111.48 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.