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    Donepezil HCl (E2020)
    Donepezil HCl (E2020)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1159
    CAS #: 120011-70-3Purity ≥98%

    Description: Donepezil Hydrochloride (E2020; Aricept; E-2020), the hydrochloride salt of Donepezil, is a noncompetitive, specific and potent AChE inhibitor for bAChE and hAChE with antiAlzheimer's disease (AD) effects. It inhibits bAChE and hAChE with IC50s of 8.12 nM and 11.6 nM , respectively. Acetylcholinesterase (AChE) is an enzyme possibly involved in cognitive dysfunction of patients suffering Alzheimer's disease (AD). 

    References: Neuropharmacology. 1999 Jan;38(1):181-93; CNS Neurosci Ther. 2012 Feb;18(2):185-7.

    Related CAS #: 120014-06-4 (free base)   120011-70-3 (HCl)  

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    Molecular Weight (MW)416
    FormulaC24H29NO3.HCl
    CAS No.120011-70-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: 5 mg/mL (12.01 mM) 
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
    SynonymsE-2020; E2020; Aricept; E 2020; Donepezil HCl


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    In Vitro

    In vitro activity: 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.


    Kinase Assay:  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).

    In VivoIntraperitoneal 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.
    Animal modelRats
    Formulation & Dosage1 mg/kg
    References

    Neuropharmacology. 1999 Jan;38(1):181-93; CNS Neurosci Ther. 2012 Feb;18(2):185-7.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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