Home Neuronal Signaling AChR inhibitor Donepezil HCl For research use only.

Donepezil HCl

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

Donepezil HCl Chemical Structure

Donepezil HCl Chemical Structure

CAS: 120011-70-3

Selleck's Donepezil HCl has been cited by 10 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Biological Activity

Description Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
Targets
bAChE [1] hAChE [1]
8.12 nM 11.6 nM
In vitro
In vitro 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. [2] 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. [3]
In Vivo
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. [2]. 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. [4]
Animal Research Animal Models Male Lister Hooded rats
Dosages 18 μM/kg
Administration Administered via i.p. or p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT03905096 Completed Healthy Boehringer Ingelheim April 12 2019 Phase 1
NCT03438604 Completed Alzheimer''s Disease Corium Inc. February 13 2018 Phase 1

Chemical lnformation & Solubility

Molecular Weight 416 Formula

C24H29NO3.HCl
CAS No. 120011-70-3 SDF Download Donepezil HCl SDF
Smiles COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 5 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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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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Tech Support

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.

Handling Instructions

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