1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. Donepezil Hydrochloride

Donepezil Hydrochloride  (Synonyms: E2020)

Cat. No.: HY-B0034 Purity: 99.94%
COA Handling Instructions

Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.

For research use only. We do not sell to patients.

Donepezil Hydrochloride Chemical Structure

Donepezil Hydrochloride Chemical Structure

CAS No. : 120011-70-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid
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100 mg USD 106 In-stock
200 mg USD 158 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Donepezil Hydrochloride:

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Description

Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].

IC50 & Target

AChE

 

In Vitro

Donepezil’s neuroprotective mechanism is related to the enhanced phosphorylation of Akt and GSK-3β and reduced phosphorylation of tau and glycogen synthase[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Cortical neuronal cells
Concentration: 0.01, 0.1, 1, and 10 μM
Incubation Time: 24 hours
Result: Exhibited significantly increased cell viability (maximized 89.2±2.1% in MTT, 96.3±5.5% in TBS, and 95.1±3.2% in CCK-8).

Western Blot Analysis[2]

Cell Line: Cortical neuronal cells
Concentration: 10 μM
Incubation Time: 24 hours before 20 μM Aβ42 exposure for 6 hours
Result: Effects of Donepezil on Akt and the GSK-3 signaling pathway were statistically significant in the presence of Aβ42 toxicity.
In Vivo

Donepezil treatment (3 mg/kg) significantly prevents the progression of scopolamine-induced memory impairment in mice[3].
A pharmacokinetic study of Donepezil shows a mean peak plasma concentration of donepezil after oral treatment (3 and 10 mg/kg) of approximately 1.2 h and 1.4 h, respectively; absolute bioavailability is calculated as 3.6%[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male imprinting control region (ICR) mice (6 weeks old)[3]
Dosage: 3-10 mg/kg
Administration: Administered orally
Result: Pretreatment with 3–10 mg/kg ameliorated scopolamine-induced memory impairment.
Animal Model: Hairless rats with an average weight of 300 g[3]
Dosage: 3 and 10 mg/kg (Pharmacokinetic Analysis)
Administration: Administered orally; and blood (250 μL) was collected through the tail vein
Result: After oral treatment (3 and 10 mg/kg), a maximum concentration (Cmax) was reached after approximately 1.2 ± 0.4 h and 1.4 ± 0.5 h, respectively, and gradually decreased.
Clinical Trial
Molecular Weight

415.95

Formula

C24H30ClNO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(CC2CCN(CC3=CC=CC=C3)CC2)CC4=C1C=C(OC)C(OC)=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (60.10 mM; Need ultrasonic)

DMSO : 6.2 mg/mL (14.91 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4041 mL 12.0207 mL 24.0414 mL
5 mM 0.4808 mL 2.4041 mL 4.8083 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (3.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.94%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.4041 mL 12.0207 mL 24.0414 mL 60.1034 mL
5 mM 0.4808 mL 2.4041 mL 4.8083 mL 12.0207 mL
10 mM 0.2404 mL 1.2021 mL 2.4041 mL 6.0103 mL
H2O 15 mM 0.1603 mL 0.8014 mL 1.6028 mL 4.0069 mL
20 mM 0.1202 mL 0.6010 mL 1.2021 mL 3.0052 mL
25 mM 0.0962 mL 0.4808 mL 0.9617 mL 2.4041 mL
30 mM 0.0801 mL 0.4007 mL 0.8014 mL 2.0034 mL
40 mM 0.0601 mL 0.3005 mL 0.6010 mL 1.5026 mL
50 mM 0.0481 mL 0.2404 mL 0.4808 mL 1.2021 mL
60 mM 0.0401 mL 0.2003 mL 0.4007 mL 1.0017 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Donepezil Hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Donepezil Hydrochloride
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