Donepezil Hydrochloride (E2020) 是一种可逆的选择性AChE抑制剂，对AChE 的IC50为 6.7 nM。对 AChE 的选择性高于 BuChE。Donepezil Hydrochloride对 Aβ42 神经毒性具有神经保护作用。
| 生物活性 | Donepezil Hydrochloride (E2020) is a reversible, selectiveAChEinhibitor with anIC50of 6.7 nM forAChEactivity. Donepezil shows high selectivity forAChEover BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2]. |
体外研究
(In Vitro) | Donepezil’s neuroprotective mechanism is related to the enhanced phosphorylation of Akt and GSK-3β and reduced phosphorylation of tau and glycogen synthase[2].
Cell Viability Assay[2] | Cell Line: | Cortical neuronal cells | | Concentration: | 0.01, 0.1, 1, and 10 μM | | Incubation Time: | 24 hours | | Result: | Exhibited significantly 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 Line: | Cortical neuronal cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours before 20 μM Aβ42 exposure for 6 hours | | Result: | Effects of Donepezil on Akt and the GSK-3 signaling pathway were statistically significant in the presence of Aβ42 toxicity. |
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体内研究
(In Vivo) | Donepezil treatment (3 mg/kg) significantly prevents the progression of scopolamine-induced memory impairment in mice[3].
A pharmacokinetic study of Donepezil shows a mean peak plasma concentration of donepezil after oral treatment (3 and 10 mg/kg) of approximately 1.2±0.4 h and 1.4±0.5 h, respectively; absolute bioavailability is calculated as 3.6%[3].
| Animal Model: | Male imprinting control region (ICR) mice (6 weeks old)[3] | | Dosage: | 3-10 mg/kg | | Administration: | Administered orally | | Result: | Pretreatment with 3–10 mg/kg ameliorated scopolamine-induced memory impairment. |
| Animal Model: | Hairless rats with an average weight of 300 g[3] | | Dosage: | 3 and 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | Administered orally; and blood (250 μL) was collected through the tail vein | | Result: | 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 decreased. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 25 mg/mL(60.10 mM;Need ultrasonic) DMSO : 6.2 mg/mL(14.91 mM;Need warming) 配制储备液 | 1 mM | 2.4041 mL | 12.0207 mL | 24.0414 mL | | 5 mM | 0.4808 mL | 2.4041 mL | 4.8083 mL | | 10 mM | 0.2404 mL | 1.2021 mL | 2.4041 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.25 mg/mL (3.01 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (3.01 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.25 mg/mL (3.01 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (3.01 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.25 mg/mL (3.01 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (3.01 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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