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

Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.

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

CAS No. : 120014-06-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Donepezil:

Top Publications Citing Use of Products

    Donepezil purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2025 Feb 14;17(1):43.  [Abstract]

    APP/PS1 mice were administered Donepezil Hydrochloride intraperitoneally at 1 mg/kg daily for three months to perform the Y-maze test.

    Donepezil purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2025 Feb 14;17(1):43.  [Abstract]

    APP/PS1 mice were administered Donepezil Hydrochloride intraperitoneally at 1 mg/kg daily for three months to test plateau quadrant dwell time.

    Donepezil purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2025 Feb 14;17(1):43.  [Abstract]

    APP/PS1 mice were administered Donepezil Hydrochloride intraperitoneally at 1 mg/kg daily for three months to test their plateau quadrant swimming distance.

    Donepezil purchased from MedChemExpress. Usage Cited in: Alzheimers Res Ther. 2025 Feb 14;17(1):43.  [Abstract]

    APP/PS1 mice were intraperitoneally injected daily with Donepezil Hydrochloride at 1 mg/kg for 6E10 staining of the cortex and hippocampus for up to three months.

    Donepezil purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2024 Jun 4:131:155802.  [Abstract]

    Donepezil (Don: 5 mg/kg). The latency of the mice swimming to the platform in MWM test.

    Donepezil purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2024 Jun 4:131:155802.  [Abstract]

    Donepezil (Don: 5 mg/kg). Immunofluorescence staining of Brdu (red) and DCX (green) with DAPI (blue) in hippocampus.

    Donepezil purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2024 Jun 4:131:155802.  [Abstract]

    Donepezil (Don: 5 mg/kg). Representative Western blot images.

    Donepezil purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2024 Feb 5:265:116071.  [Abstract]

    Effects of C7 and Donepezil (DZ, 5 mg/kg) on ​​AChE activity in mouse brain.

    Donepezil purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2024 Feb 5:265:116071.  [Abstract]

    Effects of C7 and Donepezil (DZ, 5 mg/kg) on ​​Aβ1-42-induced learning impairment in mice: spontaneous alternation behavior.

    Donepezil purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2021 Jun;11(6):e428.

    Donepezil Hydrochloride at 1.0 or 2.0 mg/kg/day was injected intraperitoneally at 5 months after MS AAV‐CAG‐hTau‐mCherry‐3flag or AAV‐CAG‐vector‐mCherry‐3flag infusion. Both doses of Donepezil Hydrochloride rescued synaptic transmission in MShTau mice, as evidenced by increased input-output responses.

    Donepezil purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2021 Jun;11(6):e428.

    Five months after infusion of MS AAV-CAG-hTau-mCherry-3flag or AAV-CAG-vector-mCherry-3flag, Donepezil Hydrochloride was administered intraperitoneally at doses of 1.0 or 2.0 mg/kg/day. Both doses of Donepezil Hydrochloride rescued synaptic transmission in MShTau mice, manifested as an increased fEPSP slope induced during LTP induction, and this increase remained significant 60 minutes after high-frequency stimulation (HFS).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].

    IC50 & Target

    AChE

     

    Cellular Effect
    Cell Line Type Value Description References
    BV-2 IC50
    1.54 μM
    Compound: Donepezil
    Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 34923430]
    CHO IC50
    34.3 μM
    Compound: donepezil
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    [PMID: 23812503]
    HEK293 IC50
    0.009 μM
    Compound: 1
    Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
    Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
    [PMID: 26471320]
    HEK293 IC50
    0.01 μM
    Compound: Donepezil
    Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method
    Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured for 5 mins by UV-Vis spectrophotometric method
    [PMID: 28242552]
    HEK293 IC50
    0.016 μM
    Compound: donepezil
    Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins
    Inhibition of recombinant human AChE expressed in HEK293 cells preincubated for 15 mins
    [PMID: 25418133]
    HEK293 IC50
    6.2 nM
    Compound: Donepezil
    Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method
    Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate by Ellman's method
    [PMID: 31304000]
    HEK293 IC50
    7.5 μM
    Compound: 1
    Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
    Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
    [PMID: 26471320]
    HEK293 IC50
    8.2 μM
    Compound: donepezil
    Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins
    Inhibition of recombinant human BuChE expressed in HEK293 cells preincubated for 15 mins
    [PMID: 25418133]
    HEK293 IC50
    > 200 μM
    Compound: Donepezil
    Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32388114]
    HFF IC50
    0.091 μM
    Compound: Donepezil
    Cytotoxicity against HFF cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against HFF cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 32088494]
    HT-22 IC50
    56.42 μM
    Compound: Donepezil
    Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 34923430]
    HepG2 IC50
    262727 nM
    Compound: Donepezil
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    [PMID: 34530383]
    MCF7 IC50
    0.06 μM
    Compound: Donepezil
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 32088494]
    NIH3T3 IC50
    1.26 μM
    Compound: Donepezil
    Cytotoxicity against mouse NIH/3T3 cells incubated for 24 hrs by MTT assay
    Cytotoxicity against mouse NIH/3T3 cells incubated for 24 hrs by MTT assay
    [PMID: 38614062]
    NIH3T3 IC50
    316.42 μM
    Compound: Donepezil
    Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay
    Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay
    [PMID: 27789142]
    SH-SY5Y CC50
    25.06 μM
    Compound: Donepezil
    Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay
    Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay
    [PMID: 30822710]
    SH-SY5Y IC50
    0.3 μM
    Compound: Donepezil
    Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay
    Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay
    [PMID: 32088494]
    SH-SY5Y IC50
    15.54 μM
    Compound: 1
    Cytotoxicity against human SH-SY5Y cells after 72 hrs by SRB assay
    Cytotoxicity against human SH-SY5Y cells after 72 hrs by SRB assay
    [PMID: 27823887]
    SH-SY5Y IC50
    155 μM
    Compound: 2; Don
    Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser396 residue incubated for 24 hrs by ELISA
    Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser396 residue incubated for 24 hrs by ELISA
    [PMID: 36257284]
    SH-SY5Y IC50
    202 μM
    Compound: 2; Don
    Antioxidant activity against okadaic acid-induced ROS generation in human SH-SY5Y cells assessed as reduction in DCF fluorescence intensity pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by DCFH-DA dye based fluorescence analysis
    Antioxidant activity against okadaic acid-induced ROS generation in human SH-SY5Y cells assessed as reduction in DCF fluorescence intensity pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by DCFH-DA dye based fluorescence analysis
    [PMID: 36257284]
    SH-SY5Y IC50
    326 μM
    Compound: 2; Don
    Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of okadaic acid-induced mitochondrial membrane potential by measuring increase in red-to-green fluorescence intensity ratio pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by JC-1 dye based fluorescence analysis
    Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of okadaic acid-induced mitochondrial membrane potential by measuring increase in red-to-green fluorescence intensity ratio pretreated for 24 hrs followed by okadaic acid addition for 24 hrs by JC-1 dye based fluorescence analysis
    [PMID: 36257284]
    SH-SY5Y IC50
    35 μM
    Compound: 2; Don
    Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser199 residue incubated for 24 hrs by ELISA
    Antialzheimer activity in human SH-SY5Y cells assessed as inhibition of GA-induced tau hyperphosphorylation at Ser199 residue incubated for 24 hrs by ELISA
    [PMID: 36257284]
    SH-SY5Y IC50
    84.1 μM
    Compound: Donepezil
    Neurotoxicity against human SH-SY5Y cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay
    Neurotoxicity against human SH-SY5Y cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay
    [PMID: 30795991]
    SH-SY5Y IC50
    95.13 μM
    Compound: 1
    Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
    [PMID: 31280020]
    SH-SY5Y IC50
    > 200 μM
    Compound: Donepezil
    Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32388114]
    SK-N-MC IC50
    > 100 μM
    Compound: Donepezil
    Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
    Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
    [PMID: 28841514]
    Sf21 IC50
    205.7 μM
    Compound: Donepezil
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Sf21 IC50
    519.3 μM
    Compound: Donepezil
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    U-87MG ATCC IC50
    47.24 μM
    Compound: V
    Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth by MTT assay
    Cytotoxicity against human U-87 MG cells assessed as inhibition of cell growth by MTT assay
    [PMID: 36630883]
    In Vitro

    Donepezil (E2020 free base) 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. 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].
    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].

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

    Clinical Trial
    Molecular Weight

    379.49

    Formula

    C24H29NO3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C(C=C(OC)C(OC)=C1)=C1C2)C2CC(CC3)CCN3CC4=CC=CC=C4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture and light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (87.83 mM; Need ultrasonic; 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 2.6351 mL 13.1756 mL 26.3512 mL
    5 mM 0.5270 mL 2.6351 mL 5.2702 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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: ≥ 2.5 mg/mL (6.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.87%

    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 and light). 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 1 mM 2.6351 mL 13.1756 mL 26.3512 mL 65.8779 mL
    5 mM 0.5270 mL 2.6351 mL 5.2702 mL 13.1756 mL
    10 mM 0.2635 mL 1.3176 mL 2.6351 mL 6.5878 mL
    15 mM 0.1757 mL 0.8784 mL 1.7567 mL 4.3919 mL
    20 mM 0.1318 mL 0.6588 mL 1.3176 mL 3.2939 mL
    25 mM 0.1054 mL 0.5270 mL 1.0540 mL 2.6351 mL
    30 mM 0.0878 mL 0.4392 mL 0.8784 mL 2.1959 mL
    40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6469 mL
    50 mM 0.0527 mL 0.2635 mL 0.5270 mL 1.3176 mL
    60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0980 mL
    80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8235 mL
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    • 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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    Product Name:
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    Cat. No.:
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