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别名 多奈哌齐, E2020, Donepezilo, Aricept
Donepezil (Aricept) 是一种AChE 抑制剂,对牛 AChE 和人 AChE 的IC50分别为 8.12 nM 和 11.6 nM。

Donepezil (Aricept) 是一种AChE 抑制剂,对牛 AChE 和人 AChE 的IC50分别为 8.12 nM 和 11.6 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 232 | 现货 | |
| 10 mg | ¥ 372 | 现货 | |
| 25 mg | ¥ 597 | 现货 | |
| 50 mg | ¥ 828 | 现货 | |
| 100 mg | ¥ 1,430 | 现货 | |
| 500 mg | ¥ 3,580 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 322 | 现货 |
Donepezil 相关产品
| 产品描述 | Donepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type. |
| 靶点活性 | AChE (bovine):8.12 nM, AChE (human):11.6 nM |
| 体外活性 | Donepezil对AChE的选择性比对BuChE(butyrylcholinesterase)高出500-1000倍。无论是短期还是长期暴露,Donepezil均会引起SH-SY5Y人类神经母细胞增殖的浓度依赖性抑制,这种抑制与毒蕈碱或烟碱受体阻断或细胞凋亡无关。Donepezil减少了细胞周期中S-G2/M阶段的细胞数量,增加了G0/G1期的细胞比例,并且与p21细胞周期抑制因子表达量的增加平行,降低了G1/S与G2/M转换期中两种cyclins(cyclin E与cyclin B)的表达。此外,Donepezil增加了依赖动作电位的多巴胺释放,并调节了黑质多巴胺能神经元的烟碱受体[1]。 |
| 体内活性 | 在血浆、尿液和胆汁中,多数Donepezil的代谢产物为O-葡萄糖醛酸酯。经口摄入后,3-5小时达到血浆峰值浓度,食物不影响其吸收。Donepezil从胃肠道缓慢吸收,年轻志愿者的终末消除半衰期为50-70小时(老年受试者>100小时)。在肝脏经过广泛代谢后,原化合物有93%与血浆蛋白结合。Donepezil在肝脏通过细胞色素P450系统(CYP1A2-、CYP2D6-、CYP3A4相关酶)代谢。在动物中,Donepezil在大脑中未改变,神经组织中未检测到代谢物。Donepezil在1-10 mg/天的剂量范围内具有线性药动学特性。循环中的Donepezil有96%与蛋白质结合[1]。 |
| 细胞实验 | Cell lines: retinal ganglion cells (RGCs). Concentrations: 0.1-10 μM. Incubation Time: 3 days. RGC survival after exposure to each reagent (glutamate, donepezil, tacrine, galanthamine, and HA14-1) is measured by calcein-AM staining after 3 days in culture, Briefly, cells are incubated in 1 μM calcein-AM in PBS for 15 minutes at 37℃. After the medium is replaced with fresh PBS, cells are examined under a fluorescence microscope using a fluorescein filter. The total number of surviving RGCs defined as cells with a calcein-AM stained cell body and a process extending at least two cell diameters from the cell body is counted in each well. The number of surviving RGCs without any drug served as a control. |
| 动物实验 | Animal Models: male C57BL/6 wild-type and CGRP(?/?) mice (10-12 weeks old, 21–24 g). Formulation: added to the food powder. Dosages: 1.5 mg/kg (i.g.) |
| 别名 | 多奈哌齐, E2020, Donepezilo, Aricept |
| 分子量 | 379.49 |
| 分子式 | C24H29NO3 |
| CAS No. | 120014-06-4 |
| Smiles | O=C1C=2C(=CC(OC)=C(OC)C2)CC1CC3CCN(CC4=CC=CC=C4)CC3 |
| 密度 | 1.141 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 50 mg/mL (131.76 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.27 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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