Name: ZINC12613047
Price: 339.00 USD

- Overview
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    Background
    
    IC50: 21 nM for human BChE
    ZINC12613047 is a BChE inhibitor.
    Butyrylcholinesterase (BChE) is considered as a promising drug target as its levels and activity increase significantly in the late stages of Alzheimer’s disease.
    In vitro: In previous study, the complex structure between ZINC12613047 and BChE revealed the molecular basis of the high affinity binding. In contrast, the pocket was comparatively smaller in AChE likely explaining why ZINC12613047 displayed low affinity. In addition, ZINC12613047 was tested at 10 μM, where it showed significant Aβ1-42-antiaggregation effects with 61.7% inhibition. The cytotoxicity profile was assessed using the human neuroblastoma SH-SY5Y cell line and the MTS assay. ZINC12613047 at 10 μM was completely noncytotoxic. Moreover, to compare neuronal death induced by Aβ1-42 with or without various concentrations of ZINC12613047, the MTS assay was performed. Results showed that incubation of SH-SY5Y cells with 5 μM Aβ1-42 led to significant toxicity; the cell-death was about 35% higher than in the control. A clear dose-response neuroprotective effect was observed when the cells were incubated with Aβ1-42 in the presence of ZINC12613047. ZINC12613047 at 10 μM could completely protect the human neuronal SH-SY5Y cells from Aβ1-42 peptide toxicity [1].
    In vivo: There is no animal in vivo data reported.
    Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Alternative Name
    
    N-[[1-(2,3-dihydro-1H-inden-2-yl)-3-piperidinyl]methyl]-N-(2-methoxyethyl)-2-naphthalenecarboxamide
    
    CAS Number
    
    1069521-64-7
    
    Molecular Formula
    
    C29H34N2O2
    
    Molecular Weight
    
    442.6
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥95.00%
    
    Solubility
    
    ≤5mg/ml in ethanol;10mg/ml in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

ZINC12613047

ZINC12613047

Background

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