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PE859

Chemical Structure : PE859

CAS No.: 1402727-29-0

PE859 (PE-859;PE 859)

Catalog No.: PC-43143Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 448.5157
Formula C28H24N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

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

References

1. Okuda M, et al. PLoS One. 2015 Feb 6;10(2):e0117511.

2. Okuda M, et al. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5024-5028.

3. Okuda M, et al. J Alzheimers Dis. 2017;59(1):313-328.

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