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别名 盐酸多奈哌齐, E2020, Donepezil HCl, BNAG, Aricept
Donepezil HCl(Aricept) 是可逆的选择性AChE 抑制剂,IC50=6.7 nM,对 AChE 的选择性高于 BuChE。Donepezil Hydrochloride (Aricept) 对 Aβ42 神经毒性具有神经保护作用。

Donepezil HCl(Aricept) 是可逆的选择性AChE 抑制剂,IC50=6.7 nM,对 AChE 的选择性高于 BuChE。Donepezil Hydrochloride (Aricept) 对 Aβ42 神经毒性具有神经保护作用。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 156 | 现货 | |
| 10 mg | ¥ 213 | 现货 | |
| 25 mg | ¥ 328 | 现货 | |
| 50 mg | ¥ 469 | 现货 | |
| 100 mg | ¥ 693 | 现货 | |
| 500 mg | ¥ 1,860 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 372 | 现货 |
Donepezil Hydrochloride 相关产品
| 产品描述 | Donepezil HCl(Aricept) is a selective and effective AChE inhibitor for bAChE and hAChE (IC50: 8.12/11.6 nM). |
| 靶点活性 | AChE (bovine):8.12 nM, AChE (human):11.6 nM |
| 体外活性 | Donepezil以浓度依赖的方式抑制人类SHSY5Y神经母细胞系中carbachol诱导的细胞内Ca2+浓度增加,表明Donepezil具有抗胆碱能活性。[2] 最近的研究表明,Donepezil能够保护人类脐静脉内皮细胞(HUVECs)免受Water2引起的细胞损伤。这对于心血管和脑血管疾病中的氧化应激潜在治疗具有重要意义。[3] |
| 体内活性 | 大鼠腹腔内注射Donepezil导致剂量依赖性的增加唾液分泌和震颤,这些是明显的 Choline 能行为表现,其ED50为6μmol/kg。口服给药后,Donepezil的效力略低,ED50为50μmol/kg。[2]。在体内单独给药时,5-HT(4)受体诱导剂RS67333(0.3及1 mg/kg)和Donepezil(1 mg/kg)比生理盐水处理的小鼠改善了识别性能,而RS67333(0.1 mg/kg)和Donepezil(0.3 mg/kg)的低活性剂量联合给药可以改善记忆。然而,如果同时给予5-HT(4)R拮抗剂(GR125487,10 mg/kg),这种改善会被阻止。[4] |
| 激酶实验 | [3H]-Pyrilamine binding to histamine (H1) receptors in guinea pig cerebellum membranes.: Antagonists are incubated with guinea pig cerebellum membranes (0.6 mg/ml) and [3H]-pyrilamine (1.2 nM) in 0.5 ml 50 mM PBS, pH 7.5, for 30 min at 25 ℃. The incubation is ended by the addition of 5 ml of ice-cold PBS containing 2 μM pyrilamine and the collection of membranes on Whatman GF/B filters. Then the filters are washed with 3 × 5 ml of ice-cold PBS plus 2 μM pyrilamine and transferred to counting vials. The radioactivity retained by each filter is measured by liquid scintillation counting in 3 ml of HiSafe 3. Specific binding is determined from the difference between the [3H]-pyrilamine bound in the absence and in the presence of a large molar excess (10 μM) of unlabeled promethazine. |
| 别名 | 盐酸多奈哌齐, E2020, Donepezil HCl, BNAG, Aricept |
| 分子量 | 415.96 |
| 分子式 | C24H29NO3·HCl |
| CAS No. | 120011-70-3 |
| Smiles | Cl.COc1c(OC)cc2C(=O)C(CC3CCN(Cc4ccccc4)CC3)Cc2c1 |
| 密度 | no data available |
| 存储 | 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: 4.2 mg/mL (10.1 mM), Sonication is recommended. H2O: 31.2 mg/mL (75.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | Saline: 5.82 mg/mL (13.99 mM), Solution. 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/H2O
H2O
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