For research use only.
Molecular Weight(MW): 416
Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
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Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
J Am Heart Assoc 2014 3(3), e000804. Donepezil HCl purchased from Selleck.
Purity & Quality Control
Choose Selective AChR Inhibitors
|Description||Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.|
Donepezil inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity.  A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases. 
|In vivo||Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation and tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/kg following oral administration. . When administered separately in vivo, 5-HT(4) receptor inducer, RS67333 (0.3 and 1 mg/kg) and Donepezil (1 mg/kg) improves recognition performances compared to saline treated mice, while co-administration of subactive doses of RS67333 (0.1mg/kg) and Donepezil (0.3 mg/kg) improves memory. However, this improvement is prevented if a 5-HT(4)R antagonist (GR125487, 10 mg/kg) is also administered. |
|In vitro||Water||5 mg/mL (12.01 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04308304||Not yet recruiting||Drug: MK-1942|Drug: Donepezil|Drug: Placebo||Alzheimer''s Disease||Merck Sharp & Dohme Corp.||October 13 2020||Phase 1|
|NCT03932916||Not yet recruiting||Drug: Donepezil pamoate||AD||Shanghai Synergy Pharmaceutical Sciences Co. Ltd.||May 20 2019||Phase 1|
|NCT03438604||Completed||Drug: Donepezil TDS||Alzheimer''s Disease||Corium International Inc.||February 13 2018||Phase 1|
|NCT03432195||Completed||Drug: Donepezil TDS||Alzheimer''s Disease||Corium International Inc.||January 31 2018||Phase 1|
|NCT03397862||Completed||Drug: Donepezil TDS|Drug: Vehicle TDS||Skin Irritation|Sensitization||Corium International Inc.||November 14 2017||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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