| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 5g |
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Purity: ≥98%
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).
| Targets |
Acetylcholinesterase (AChE)
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| ln Vitro |
The phosphorylation of tau and glycogen synthase is reduced and that of Akt and GSK-3β is enhanced in the neuroprotective mechanism of donepezil hydrochloride [2].
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| ln Vivo |
In mice, scopolamine-induced memory impairment was significantly halted from progressing by donepezil treatment (3 mg/kg) [3]. According to pharmacokinetic studies, the mean peak plasma concentrations of donepezil hydrochloride were measured to be 3.6% absolute bioavailability, and they occurred roughly 1.2 and 1.4 hours after oral administration (3 and 10 mg/kg), respectively [3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Cortical neuronal cells Tested Concentrations: 0.01, 0.1, 1, and 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated Dramatically 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 Types: Cortical neuronal cells Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) before 20 μM Aβ42 exposure for 6 hrs (hours) Experimental Results: Effects of Donepezil on Akt and the GSK-3 signaling pathway were statistically significant in the presence of Aβ42 toxicity. |
| Animal Protocol |
Animal/Disease Models: Male imprinting control region (ICR) mice (6 weeks old)[3]
Doses: 3-10 mg/kg Route of Administration: Administered orally Experimental Results: Pretreatment with 3–10 mg/kg ameliorated scopolamine-induced memory impairment. Animal/Disease Models: Hairless rats with an average weight of 300 g[3] Doses: 3 and 10 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Administered po (oral gavage) and blood (250 μL) was collected through the tail vein Experimental Results: 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 diminished. |
| References |
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| Additional Infomation |
Donepezil Hydrochloride is the hydrochloride salt of a piperidine derivative with neurocognitive-enhancing activity. Donepezil reversibly inhibits acetylcholinesterase, thereby blocking the hydrolysis of the neurotransmitter acetylcholine and, consequently, increasing its activity. This agent may improve neurocognitive function in Alzheimer's disease, reduce sedation associated with opioid treatment of cancer pain, and improve neurocognitive function in patients who have received radiation therapy for primary brain tumors or brain metastases.
An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE. See also: Donepezil (has active moiety); Donepezil hydrochloride; memantine hydrochloride (component of). |
| Molecular Formula |
C24H29NO3.HCL
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|---|---|---|
| Molecular Weight |
416
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| Exact Mass |
415.191
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| Elemental Analysis |
C, 69.30; H, 7.27; Cl, 8.52; N, 3.37; O, 11.54
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| CAS # |
120011-70-3
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| Related CAS # |
Donepezil;120014-06-4;Donepezil-d4 hydrochloride;1219798-88-5;Donepezil-d5 hydrochloride;1883548-90-0
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| PubChem CID |
5741
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| Appearance |
White to off-white solid powder
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| Boiling Point |
527.9ºC at 760 mmHg
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| Melting Point |
220-222ºC
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| Flash Point |
273.1ºC
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| Vapour Pressure |
3.11E-11mmHg at 25°C
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| LogP |
5.101
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O=C1C2=C([H])C(=C(C([H])=C2C([H])([H])C1([H])C([H])([H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C([H])([H])C1([H])[H])OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
XWAIAVWHZJNZQQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H29NO3.ClH/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18;/h3-7,14-15,17,20H,8-13,16H2,1-2H3;1H
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| Chemical Name |
2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one hydrochloride
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| Synonyms |
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| HS Tariff Code |
2933.39.9100
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4038 mL | 12.0192 mL | 24.0385 mL | |
| 5 mM | 0.4808 mL | 2.4038 mL | 4.8077 mL | |
| 10 mM | 0.2404 mL | 1.2019 mL | 2.4038 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02097056 | Completed Has Results | Drug: Donepezil HCL | Alzheimer's Disease | Eisai Korea Inc. | February 2014 | Phase 4 |
| NCT04661280 | Recruiting | Drug: Donepezil | Alzheimer Disease, Early Onset | Assistance Publique - Hôpitaux de Paris | February 10, 2022 | Phase 3 |
| NCT01063556 | Completed | Drug: donepezil HCl | End-Stage Renal Disease | Eisai Co., Ltd. | February 2010 | Phase 4 |
| NCT02787746 | Completed | Drug: Donepezil | Alzheimer's Disease | Beijing Friendship Hospital | April 2016 | Phase 4 |
| NCT00047697 | Completed Has Results | Drug: Donepezil HCl Drug: Placebo |
Autistic Disorder | University of Pittsburgh | October 2002 | Phase 2 |
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