Donepezil (E2020) |
| رقم الكتالوجGC30810 |
Donepezil (E2020) (قاعدة خالية من E2020) هو مثبط محدد وقوي لـ AChE مع IC50s من 8.12 نانومتر و 11.6 نانومتر لـ AChE البقري و AChE البشري ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120014-06-4
Sample solution is provided at 25 µL, 10mM.
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Donepezil (E2020) is an acetylcholinesterase (AChE) inhibitor with an IC50 of 6.7nM[1]. Donepezil (E2020) can block MAPK and NF-κB signaling, directly inhibit AβO-induced microglial activation, and help improve neurodegenerative memory impairment [2].
In vitro, Donepezil (E2020) (10 μM) treated rat primary cortical cells for 24 hours, which induced an increase in SNX33 mRNA expression in the cells, and the Aβ40 level in the culture medium was significantly reduced in a concentration- and timedependent manner[3]. Donepezil (E2020) (0.1-10μM) dose-dependently reduces glutamate toxicity-induced retinal ganglion cell death[4]. Donepezil (E2020) (1-10μM) can protect HUVECs from hydrogen peroxide-induced cell damage, significantly upregulating the expression of HIF-1α and MnSOD in the cells, and may also have a similar protective effect on ischemic tissue[5].
In vivo, Donepezil (E2020) (1.5mg/kg) was administered orally twice a day for 21 days, significantly increasing ACh levels in the cortex of aged rats, with ACh release increasing by 210% [6]. Donepezil (E2020), injected intraperitoneally in rats, dose-dependently caused an increase in salivation and tremor, which are obvious signs of cholinergic behavior, with an ED50 of 6 μmol/kg[7].
References:
[1] Ramón Cacabelos. Donepezil in Alzheimer's disease: From conventional trials to pharmacogenetics[J]. Neuropsychiatric Disease & Treatment, 2007, 3(3): 303-333.
[2] Kim H G , Moon M , Choi J G ,et al.Donepezil inhibits the amyloid-beta oligomer-induced microglial activation in vitro and in vivo.[J].Neurotoxicology, 2014, 40:23-32.
[3] Takada-Takatori Y , Nakagawa S , Kimata R ,et al. Donepezil modulates amyloid precursor protein endocytosis and reduction by up-regulation of SNX33 expression in primary cortical neurons[J]. Scientific Reports, 2019.
[4] Miki A, Otori Y, et al. Protective effect of donepezil on retinal ganglion cells in vitro and in vivo[J]. Curr Eye Res. 2006, 31(1):69-77.
[5] Huang Z H , Guo W , Zhang L L ,et al.Donepezil Protects Endothelial Cells against Hydrogen Peroxide‐Induced Cell Injury[J]. Cns Neuroscience & Therapeutics, 2012, 18(2):185-187.
[6] Scali C , Casamenti F , Bellucci A ,et al. Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats[J]. Journal of Neural Transmission, 2002, 109(7-8):1067-1080.
[7]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):181-93.
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Cell experiment [1]: |
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Cell lines |
rat primary cortical cells |
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Preparation method |
Cells were treated with 10 μM Donepezil (E2020) for 24 h. The relative mRNA level of SNX33/β-actin was determined by RT-qPCR. |
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Reaction Conditions |
10μM; 24h |
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Applications |
Donepezil(E2020) treated cells show a concentration-dependent increase in SNX33 mRNA levels compared with untreated control cells. |
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Animal experiment [2]: |
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Animal models |
male Fisher 344 rats |
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Preparation method |
Donepezil (E2020) (1.5mg/kg) or vehicle (5% Na-citrate buffer adjusted to pH 5.5–6) were administered per os for 21 days, twice daily (8:00 am and 4:00 pm). |
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Dosage form |
1.5mg/kg; p.o. |
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Applications |
rats treated with Donepezil(E2020) a statistically significant 210% increase in cortical acetylcholine release was detected. |
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References: [1] Takada-Takatori Y , Nakagawa S , Kimata R ,et al. Donepezil modulates amyloid precursor protein endocytosis and reduction by up-regulation of SNX33 expression in primary cortical neurons[J]. Scientific Reports, 2019. [2] Scali C , Casamenti F , Bellucci A ,et al. Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats[J]. Journal of Neural Transmission, 2002, 109(7-8):1067-1080. |
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| Cas No. | 120014-06-4 | SDF | |
| Canonical SMILES | O=C(C(C=C(OC)C(OC)=C1)=C1C2)C2CC(CC3)CCN3CC4=CC=CC=C4 | ||
| Formula | C24H29NO3 | M.Wt | 379.49 |
| الذوبان | DMSO : 33.33 mg/mL (87.83 mM) | Storage | Store at RT, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6351 mL | 13.1756 mL | 26.3512 mL |
| 5 mM | 0.527 mL | 2.6351 mL | 5.2702 mL |
| 10 mM | 0.2635 mL | 1.3176 mL | 2.6351 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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