Donepezil Hydrochloride (Synonyms:盐酸多奈哌齐; E2020)
目录号 : KM20214 CAS No. : 120011-70-3 纯度 : 98%

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。

规格 价格 是否有货 数量
50mg
In-stock
100mg
In-stock
200mg
In-stock
500mg 询价 In-stock
1g 询价 In-stock

Other Forms of Rapamycin:

KKL Med 的所有产品和服务仅用于科学研究,不能被用于人体,兽医,我们也不向个人提供产品和服务。
生物活性

Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.

体外研究

Donepezil’s neuroprotective mechanism is related to the enhanced phosphorylation of Akt and GSK-3β and reduced phosphorylation of tau and glycogen synthase.

Cell Viability Assay

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

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.
体内研究

Donepezil treatment (3 mg/kg) significantly prevents the progression of scopolamine-induced memory impairment in mice.
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%.

Animal Model: Male imprinting control region (ICR) mice (6 weeks old)
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
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.
分子式
C24H30ClNO3
分子量
415.95
CAS号
120011-70-3
中文名称
盐酸多奈哌齐
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 : 33.33 mg/mL (80.13 mM; Need ultrasonic)

DMSO : 6.2 mg/mL (14.91 mM; Need warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 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-CD in 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 μL 20% 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。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
在线客服
咨询热线
400-881-9290
关注微信公众号