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卡巴拉汀 /Rivastigmine {[allProObj[0].p_purity_real_show]}

货号:A248924 同义名: 利凡斯的明 / S-Rivastigmine;SDZ-ENA 713

Rivastigmine is a acetylcholinesterase inhibitor with IC50 value of 5.5 μM for cholinesterase, used for the treatment of mild to moderate Alzheimer's disease and Parkinson's disease.

Rivastigmine 化学结构 CAS号:123441-03-2
Rivastigmine 化学结构
CAS号:123441-03-2
Rivastigmine 3D分子结构
CAS号:123441-03-2
Rivastigmine 化学结构 CAS号:123441-03-2
Rivastigmine 3D分子结构 CAS号:123441-03-2
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Rivastigmine 纯度/质量文件 产品仅供科研

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Rivastigmine 生物活性

靶点
  • AChR

    AChR, IC50:5.5 μM

描述 Rivastigmine is a pseudo-irreversible, carbamate-type, brain-selective, dual AChE−BuChE inhibitor. In vitro, in male Wistar rats showed greater inhibitory potency (half maximal inhibitory concentration [IC50]) of rivastigmine toward brain BuChE and AChE compared with donepezil under optimal assay conditions (BuChE: 31 vs 7,400 nM; AChE: 4.3 vs 6.7 nM) [3]. Rivastigmine (1 mg/kg) also reduced myeloperoxidase activity and IL-6 by >60%, and the infiltration of CD11b expressing cells by 80%[4]. Rivastigmine can modify the levels of several shedding proteins and directs APP processing toward the non-amyloidogenic pathway[5].

Rivastigmine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02860338 - Completed - -
NCT01401582 Dementia Not Applicable Active, not recruiting March 2018 Germany ... 展开 >> Institute for Community Medicine Greifswald, Mecklenburg- Western Pommerania, Germany, 17489 收起 <<
NCT00291421 - Completed - -

Rivastigmine 参考文献

[1]Abdel-Aal RA, Assi AA, Kostandy BB. Rivastigmine reverses aluminum-induced behavioral changes in rats. Eur J Pharmacol. 2011 Jun 1;659(2-3):169-76.

[2]Jann MW. Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease. Pharmacotherapy. 2000 Jan;20(1):1-12.

[3]Kandiah N, Pai MC, Senanarong V, Looi I, Ampil E, Park KW, Karanam AK, Christopher S. Rivastigmine: the advantages of dual inhibition of acetylcholinesterase and butyrylcholinesterase and its role in subcortical vascular dementia and Parkinson's disease dementia. Clin Interv Aging. 2017 Apr 18;12:697-707. doi: 10.2147/CIA.S129145. PMID: 28458525; PMCID: PMC5402908.

[4]Shifrin H, Nadler-Milbauer M, Shoham S, Weinstock M. Rivastigmine alleviates experimentally induced colitis in mice and rats by acting at central and peripheral sites to modulate immune responses. PLoS One. 2013;8(2):e57668. doi: 10.1371/journal.pone.0057668. Epub 2013 Feb 28. PMID: 23469045; PMCID: PMC3585220.

[5]Ray B, Maloney B, Sambamurti K, Karnati HK, Nelson PT, Greig NH, Lahiri DK. Rivastigmine modifies the α-secretase pathway and potentially early Alzheimer's disease. Transl Psychiatry. 2020 Feb 3;10(1):47. doi: 10.1038/s41398-020-0709-x. Erratum in: Transl Psychiatry. 2020 Mar 2;10(1):81. PMID: 32066688; PMCID: PMC7026402.

Rivastigmine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.99mL

0.80mL

0.40mL

19.97mL

3.99mL

2.00mL

39.95mL

7.99mL

3.99mL

Rivastigmine 技术信息

CAS号123441-03-2
分子式C14H22N2O2
分子量 250.337
别名 利凡斯的明 ;S-Rivastigmine;SDZ-ENA 713;Exelon
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(199.73 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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