GLPBio

Donepezil HCl

Catalog No.: GC14490Purity:>99.50%
COASDSData Sheet
Donepezil HCl (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity.

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Donepezil HCl
Cas No.: 120011-70-3
10mM (in 1mL DMSO)In Stock
$38.00
1
1gIn Stock
$56.00
1
5gIn Stock
$167.00
1
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Description

Donepezil Hydrochloride (Donepezil HCL) is a novel, potent and selective inhibitor of acetylcholinesterase (AChE), an enzyme possibly involved in cognitive dysfunction of patients suffering Alzheimer’s disease (AD), with the half maximal inhibition concentration IC50 value of 6.7 nM [1].

Donepezil HCL is a piperidine-class AChE inhibitor containing an N-benzylpiperdine and an indanone moiety, which confers it a longer and more selective action against AchE as compared to BuChE (IC50: 7.4 μM) [1].

Donepezil HCL has been approved by FDA for the treatment of AD, in which it has improved cognitive function of mild to severe moderate AD patients and exhibited excellent tolerability without hepatotoxicity [1].

Reference

References:
[1] Sugimoto H, Ogura H, Arai Y, Limura Y, Yamanishi Y. Research and development of donepezil hydrochloride, a new type of acetylcholinesterase inhibitor. Jpn J Pharmacol. 2002 May;89(1):7-20.

Protocol

Cell experiment [1,2]:

Cell lines

Human SHSY5Y neuroblastoma cells, human umbilical vein endothelial cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 h

Applications

Donepezil dose-dependently inhibited the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells with the IC50 of 4.0 ± 0.2 μM. Donepezil protected human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. Donepezil (100 μM) decreased cell viability. Pretreatment with donepezil at concentrations of 1 and 10 μM significantly inhibited the H2O2–induced reduction in cell viability. Exposure of HUVECs to donepezil (1 μM) for 2 h upregulated HIF-1α expression.
Animal experiment [1,3]:

Animal models

Male Lister Hooded rats, adult male NMRI mice

Dosage form

Intraperitoneal administration, 1 mg/kg

Application

In Male Lister Hooded rats, donepezil dose-dependently increased salivation and tremor with an ED50 of 6 μmol/kg. In adult male NMRI mice, donepezil (1 mg/kg) improved recognition performances.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Snape M F, Misra A, Murray T K, et al. A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066[J]. Neuropharmacology, 1999, 38(1): 181-193.

[2]. Huang Z H, Guo W, Zhang L L, et al. Donepezil protects endothelial cells against hydrogen peroxide‐induced cell injury[J]. CNS neuroscience & therapeutics, 2012, 18(2): 185-187.

[3].Freret T, Bouet V, Quiedeville A, et al. Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT 4 receptor activation (RS67333) on object recognition in mice[J]. Behavioural brain research, 2012, 230(1): 304-308.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
120011-70-3
Chemical Name
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;hydrochloride
SMILES
COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC.Cl
Molecular Formula
C24H30ClNO3
Molecular Weight
415.95
Solubility
≥ 10.4mg/mL in Water
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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