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Donepezil

Catalog No. T7041 CAS 120014-06-4

Synonyms: E2020, Donepezilo, Aricept

Donepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type.

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Donepezil, CAS 120014-06-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 31.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 70.00
50 mg	In stock	$ 85.00
100 mg	In stock	$ 153.00
500 mg	In stock	$ 377.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.8%

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Description	Donepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type.
Targets&IC50	AChE (human):11.6 nM, AChE (bovine):8.12 nM
In vitro	Donepezil 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. In addition, donepezil increases action potential-dependent dopamine release and modulates nicotinic receptors of substantia nigra dopaminergic neurons[1].
In vivo	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 absorption is not affected by food. Donepezil is slowly absorbed from the gastrointestinal tract and has a terminal elimination half-life of 50-70 hours in young volunteers (>100 hours in elderly subjects). After extensive metabolization in the liver, the parent compound is 93% bound to plasma proteins. Donepezil is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, donepezil is found unchanged in the brain, and no metabolites are detected in the nervous tissue. Donepezil has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound [1].
Cell Research	Cell lines: retinal ganglion cells (RGCs). Concentrations: 0.1-10 μM. Incubation Time: 3 days. 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.
Animal Research	Animal Models: male C57BL/6 wild-type and CGRP(?/?) mice (10-12 weeks old, 21–24 g). Formulation: added to the food powder. Dosages: 1.5 mg/kg (i.g.)

Synonyms	E2020, Donepezilo, Aricept
Molecular Weight	379.49
Formula	C24H29NO3
CAS No.	120014-06-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (131.75 mM)

References and Literature

1. Cacabelos R. Donepezil in Alzheimer’s disease: From conventional trials to pharmacogenetics[J]. Neuropsychiatric Disease & Treatment, 2007, 3(3):303-333. 2. Miki A, et al. Protective effect of donepezil on retinal ganglion cells in vitro and in vivo[J]. Current Eye Research, 2006, 31(1):69-77. 3. Jiang Q, Lu C, Sun T, et al. Alterations of the Brain Proteome and Gut Microbiota in d-Galactose-Induced Brain-Aging Mice with Krill Oil Supplementation[J]. Journal of agricultural and food chemistry. 2019, 67(35): 9820-9830.

Citations

1. Jiang Q, Lu C, Sun T, et al. Alterations of the Brain Proteome and Gut Microbiota in d-Galactose-Induced Brain-Aging Mice with Krill Oil Supplementation. Journal of agricultural and food chemistry. 2019, 67(35): 9820-9830.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Human Metabolite Library FDA-Approved & Pharmacopeia Drug Library FDA-Approved Drug Library Anti-Aging Compound Library Drug-induced Liver Injury (DILI) Compound Library Neuronal Signaling Compound Library Clinical Compound Library

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Keywords

Donepezil 120014-06-4 Neuroscience AChE E2020 Cholinesterase (ChE) Donepezilo Inhibitor inhibit Aricept hAChE E 2020 E-2020 bAChE inhibitor

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