| Size | Price | Stock | Qty |
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| 250mg |
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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).
| 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 |
[1]. H Ogura, et al. Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol. 2000 Oct;22(8):609-13.
[2]. Min-Young Noh,et al. Neuroprotective effects of donepezil through inhibition of GSK-3 activity in amyloid-beta-induced neuronal cell death. J Neurochem. 2009 Mar;108(5):1116-25. [3]. Chang Yell Shin, et al. The Effects of Donepezil, an Acetylcholinesterase Inhibitor, on Impaired Learning and Memory in Rodents. Biomol Ther (Seoul). 2018 May 1;26(3):274-281. |
| Molecular Formula |
C24H29NO3.HCL
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| Molecular Weight |
416
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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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| 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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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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| 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.
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