Z164597606

Names

[ Name ]:
Z164597606

Biological Activity

[Description]:

Z164597606 is a selective BChE inhibitor (IC50: 1.3 and 1.7 μM for eqBChE and hBChE). Z164597606 forms a π-π stacking interaction with the amino acid Trp82 of hBChE. Z164597606 can be used for the research of Alzheimer’s disease (AD)[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> AChE

[Target]

eqBCHE:1.3 μM (IC50)

hBCHE:1.7 μM (IC50)

[In Vitro]

Z164597606 (10 μM) potently inhibits BChE activity, with no more than 30% inhibitory against ACHE[1]. Z164597606 (0.5-20 μM) may bind to catalytic “anionic” site (CAS) when interacting with BChE (determined by Lineweaver-Burk reciprocal plots)[1]. Z164597606 (10 and 50 μM) shows no toxicity on neuronal cell line SH-SY5Y[1].

[References]

[1]. Xin Lu, et al. Expansion of the scaffold diversity for the development of highly selective butyrylcholinesterase (BChE) inhibitors: Discovery of new hits through the pharmacophore model generation, virtual screening and molecular dynamics simulation. Bioorg Chem. 2019 Apr;85:117-127.

[2]. Xin Lu, et al. Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease. Eur J Med Chem. 2022 Sep 2;243:114729.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₉N₃O₄

[ Molecular Weight ]:
365.38

Related Compounds

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