Donepezil HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Donepezil Hydrochloride(Donepezil HCL)是一种新型有效的乙酰胆碱酯酶(AChE)的选择性抑制剂,半数最大抑制浓度IC50值为6.7 nM.AChE是一种酶,可能参与阿尔兹海默症(AD)患者的认知功能障碍[1].
Donepezil HCL是一种哌啶类AChE抑制剂,包含一个N-苄基哌啶和一个茚酮基团,使之与BuChE(IC50:7.4 μM)相比对AchE具有更持久和更好的选择活性[1].
Donepezil HCL是FDA批准的治疗AD的药物,可改善轻度至中度严重的AD病人的认知功能,并表现出出色的耐受性,且没有肝毒性[1].
参考文献:
[1] Sugimoto H, Ogura H, Arai Y, Limura Y, Yamanishi Y. Research and development of donepezil hydrochloride, a new type of acetylcholinesterase inhibitor. Jpn J Pharmacol. 2002 May;89(1):7-20.
Storage | Store at -20°C |
M.Wt | 415.95 |
Cas No. | 120011-70-3 |
Formula | C24H30ClNO3 |
Solubility | insoluble in EtOH; insoluble in DMSO; ≥10.4 mg/mL in H2O |
Chemical Name | 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;hydrochloride |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1,2]: | |
细胞系 |
人SHSY5Y神经母细胞瘤细胞,人脐静脉内皮细胞 |
溶解方法 |
溶解度有限。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
1 h |
应用 |
在人SHSY5Y神经母细胞瘤细胞中,Donepezil剂量依赖性地抑制卡巴胆碱刺激的细胞内Ca2+浓度的增加,IC50为4.0 ± 0.2 μM。Donepezil保护人脐静脉内皮细胞(HUVECs)免受H2O2诱导的细胞损伤。Donepezil(100 μM)降低细胞活力。浓度为1和10 μM的Donepezil预处理显著抑制H2O2诱导细胞活力的降低。在HUVECs中,Donepezil(1 μM)处理2h上调HIF-1α表达。 |
动物实验 [1,3]: | |
动物模型 |
雄性Lister连帽大鼠,成年雄性NMRI小鼠 |
给药剂量 |
腹腔注射,1 mg/kg |
应用 |
在雄性Lister大鼠中,donepezil剂量依赖性地增加唾液分泌和震颤,ED50为6 μmol/kg。在成年雄性NMRI小鼠中,donepezil (1 mg/kg)改善了识别性能。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Snape M F, Misra A, Murray T K, et al. A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066[J]. Neuropharmacology, 1999, 38(1): 181-193. [2]. 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. [3].Freret T, Bouet V, Quiedeville A, et al. Synergistic effect of acetylcholinesterase inhibition (donepezil) and 5-HT 4 receptor activation (RS67333) on object recognition in mice[J]. Behavioural brain research, 2012, 230(1): 304-308. |
质量控制和MSDS
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