Bioactivity | 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]. |
Invitro | 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]. |
Name | Z164597606 |
CAS | 1050587-57-9 |
Formula | C20H19N3O4 |
Molar Mass | 365.38 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |