PE859

SKU: orb1226357

Description

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.

Key Properties

• CAS Number: 1402727-29-0
• MW: 448.5157
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₄N₄O₂
• SMILES: COC1=CC(OCC2=NC=CC=C2)=CC=C1/C=C/C3=CC(/C=C/C4=CC5=C(C=C4)C=CN5)=NN3
• Target: Amyloids
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PE-859 | PE 859

Quick Database Links

Gene Symbol

Amyloids