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Donepezil

Cat. No. M8888

All AbMole products are for research use only, cannot be used for human consumption.

Donepezil Structure
Synonym:

E2020

Size Price Availability Quantity
5mg USD 30 In stock
10mg USD 45 In stock
25mg USD 70 In stock
50mg USD 100 In stock
100mg USD 180 In stock
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Quality Control & Documentation
Biological Activity

Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.

Donepezil has reversible and noncompetitive inhibition effects on AChE. It has 500-1000-fold more selective for AChE over butyrylcholinesterase (BuChE). Short- and long-exposure of SH-SY5Y human neuroblastoma cells to donepezil induces a concentration-dependent inhibition of cell proliferation unrelated to muscarinic or nicotinic receptor blockade or apoptosis. Donepezil reduces the number of cells in the S-G2/M phases of the cell cycle, increases the G0/G1 population, and reduces the expression of two cyclins of the G1/S and G2/M transitions, cyclin E and cyclin B, in parallel with an increase in the expression of the cell cycle inhibitor p21.

Donepezil is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, donepezil is found unchanged in brain, and no metabolites are detected in the nervous tissue. In plasma, urine, and bile, most donepezil metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are achieved in 3-5 hours and its absortion is not affected by food. Donepezil has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines retinal ganglion cells (RGCs)
Preparation method RGC survival after exposure to each reagent (glutamate, donepezil, tacrine, galanthamine, and HA14-1) is measured by calcein-AM staining after 3 days in culture, Briefly, cells are incubated in 1 μM calcein-AM in PBS for 15 minutes at 37℃. After the medium is replaced with fresh PBS, cells are examined under a fluorescence microscope using a fluorescein filter. The total number of surviving RGCs defined as cells with a calcein-AM stained cell body and a process extending at least two cell diameters from the cell body is counted in each well. The number of surviving RGCs without any drug served as a control.
Concentrations 100 nM-10 μM
Incubation time 3 days
Animal Experiment
Animal models Age-matched (10-12 weeks old, 21–24 g) male C57BL/6 wild-type and CGRP(−/−) mice
Formulation added to the food powder
Dosages 1.5 mg/kg
Administration oral
Chemical Information
Molecular Weight 379.49
Formula C24H29NO3
CAS Number 120014-06-4
Solubility (25°C) DMSO: 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Cacabelos R. Neuropsychiatr Dis Treat. Donepezil in Alzheimer's disease: From conventional trials to pharmacogenetics.

[2] Miki A, et al. Curr Eye Res. Protective effect of donepezil on retinal ganglion cells in vitro and in vivo.

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Keywords: Donepezil, E2020 supplier, AChR/AChE, inhibitors, activators

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