Donepezil (Synonyms: E2020 free base)

Name: Donepezil
Brand: MedChemExpress
SKU: HY-14566
Rating: 5.0 (9 reviews)

Cat. No.: HY-14566 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Donepezil Chemical Structure

CAS No. : 120014-06-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 114	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 222	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Donepezil:

9 Publications Citing Use of MCE Donepezil

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AChE BChE

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	> 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]
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]
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]
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]
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	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	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]
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	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	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 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	[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]
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]

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.

120014-06-4

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
10 mM	0.2635 mL	1.3176 mL	2.6351 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.91%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Ogura, H., et al., Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol, 2000. 22(8): p. 609-13. [Content Brief]

[2]. Snape, M.F., et al., A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066. Neuropharmacology, 1999. 38(1): p. 181-93. [Content Brief]

[3]. Huang, Z.H., et al., Donepezil protects endothelial cells against hydrogen peroxide-induced cell injury. CNS Neurosci Ther, 2012. 18(2): p. 185-7. [Content Brief]

Complete Stock Solution Preparation Table

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

Donepezil 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.

Keywords:

Donepezil120014-06-4E2020E 2020E-2020Cholinesterase (ChE)AChEbAChEhAChEInhibitorinhibitorinhibit

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Donepezil (Synonyms: E2020 free base)

Customer Review

Other Forms of Donepezil:

Donepezil Related Antibodies

9 Publications Citing Use of MCE Donepezil

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All Cholinesterase (ChE) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Donepezil Related Antibodies

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Complete Stock Solution Preparation Table

Donepezil Related Classifications

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