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Donepezil AChR inhibitor

Name: Donepezil
Brand: Selleck Chemicals
SKU: S5073
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S5073

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

Chemical Structure

Molecular Weight: 379.49

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Quality Control

Batch: S507301 DMSO]75 mg/mL]false]]]false]]]false Purity: 99.96%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.96

Related Targets	Adrenergic Receptor 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other AChR Inhibitors	PNU-120596 Benzethonium Chloride Arecoline HBr Otilonium Bromide Lycorine Hyoscyamine (-)-Huperzine A (HupA) Nitenpyram Cytisine Chelidonine

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (197.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight	379.49	Formula	C₂₄H₂₉NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	120014-06-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Aricept, Donepezilo			Smiles	COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC

Mechanism of Action

Targets/IC₅₀/Ki	AChE 6.7 nM
In vitro	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 this compound induces a concentration-dependent inhibition of cell proliferation unrelated to muscarinic or nicotinic receptor blockade or apoptosis. This chemical 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, it increases action potential-dependent dopamine release and modulates nicotinic receptors of substantia nigra dopaminergic neurons.
In vivo	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. This compound is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, it is found unchanged in brain, and no metabolites are detected in the nervous tissue. In plasma, urine, and bile, most of its metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are achieved in 3-5 hours and its absortion is not affected by food. This chemical has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2654795/ [2] https://pubmed.ncbi.nlm.nih.gov/16421021/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06373094	Not yet recruiting	Alzheimer Disease	Shanghai Synergy Pharmaceutical Sciences Co. Ltd.\|Zhejiang Huahai Pharmaceutical Co. Ltd.	June 1 2024	Phase 1
NCT05345509	Recruiting	Alzheimer Disease	Inventage Lab. Inc.	April 1 2023	Phase 1\|Phase 2
NCT04308304	Completed	Alzheimer''s Disease	Merck Sharp & Dohme LLC	February 16 2021	Phase 1
NCT04617782	Completed	Healthy Subjects	Corium Inc.	December 8 2020	Phase 1

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