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酒石酸卡巴拉汀 /Rivastigmine tartrate {[allProObj[0].p_purity_real_show]}

货号:A193069 同义名: L-酒石酸卡巴拉汀 / SDZ-ENA 713;ENA 713 Ambeed 开学季,买赠积分,赢豪礼

Rivastigmine tartrate is an AchR inhibitor use for treatment of mild to moderate Alzheimer's disease and Parkinson's disease with elimination half-life of ‎1.5 hours.

Rivastigmine tartrate 化学结构 CAS号:129101-54-8
Rivastigmine tartrate 化学结构
CAS号:129101-54-8
Rivastigmine tartrate 3D分子结构
CAS号:129101-54-8
Rivastigmine tartrate 化学结构 CAS号:129101-54-8
Rivastigmine tartrate 3D分子结构 CAS号:129101-54-8
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Rivastigmine tartrate 纯度/质量文件 产品仅供科研

货号:A193069 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AChE AChR mAChR nAChR 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 nM

{[allProObj[0].p_purity_real_show]}
Loganin ++

AChE, IC50: 3.95 μM

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topride HCl ++

AChE, IC50: 2.04 μM

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Dehydroevodiamine HCl {[allProObj[0].p_purity_real_show]}
Jatrorrhizine ++

AChE, IC50: 872 nM

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Palmatine ++

AChE, IC50: 0.51 μM

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(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

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Galanthamine HBr ++

AChE, IC50: 0.35 μM

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Trospium chloride {[allProObj[0].p_purity_real_show]}
Tiotropium Bromide Monohydrate {[allProObj[0].p_purity_real_show]}
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

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Hexamethonium Bromide {[allProObj[0].p_purity_real_show]}
Pancuronium dibromide {[allProObj[0].p_purity_real_show]}
Neostigmine bromide {[allProObj[0].p_purity_real_show]}
Orphenadrine citrate {[allProObj[0].p_purity_real_show]}
Oxybutynin {[allProObj[0].p_purity_real_show]}
Irsogladine PDE {[allProObj[0].p_purity_real_show]}
Pyridostigmine bromide {[allProObj[0].p_purity_real_show]}
Rivastigmine +

AChR, IC50: 5.5 μM

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Paroxetine hydrochloride {[allProObj[0].p_purity_real_show]}
Rocuronium Bromide {[allProObj[0].p_purity_real_show]}
Tropicamide +++

M4 mAChR, IC50: 8 nM

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Diphenmanil methylsulfate {[allProObj[0].p_purity_real_show]}
Umeclidinium bromide {[allProObj[0].p_purity_real_show]}
Otilonium bromide {[allProObj[0].p_purity_real_show]}
Flavoxate HCl +

mAChR, IC50: 12.2 μM

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Ipratropium bromide {[allProObj[0].p_purity_real_show]}
Diphenidol HCl {[allProObj[0].p_purity_real_show]}
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

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Aclidinium Bromide ++++

M2 mAChR, Ki: 0.1 nM

M4 mAChR, Ki: 0.21 nM

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Oxybutynin chloride {[allProObj[0].p_purity_real_show]}
Pentoxyverine citrate {[allProObj[0].p_purity_real_show]}
Solifenacin {[allProObj[0].p_purity_real_show]}
Catharanthine {[allProObj[0].p_purity_real_show]}
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

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Vinblastine sulfate +

nAChR, IC50: 8.9 μM

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PNU-120596 ++

α7 nAChR, EC50: 216 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Rivastigmine tartrate 生物活性

描述 Rivastigmine tartrate, a cholinesterase inhibitor (IC50= 5.5 μM), inhibits both butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE). Rivastigmine (0.6 mg/kg intraperitoneally [i.p.]) inhibited AChE and BuChE by 40% and 25%, respectively[3]. Both preclinical studies and studies in human volunteers have shown that rivastigmine induces substantially greater inhibition of AChE in the central nervous system compartment than in the periphery[4]. Moreover, Rivastigmine can modify the levels of several shedding proteins and directs APP processing toward the non-amyloidogenic pathway for Alzheimer's disease[5].

Rivastigmine tartrate 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
NCT00291421 - 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 <<
NCT01401582 - Active, not recruiting - -

Rivastigmine tartrate 参考文献

[1]Nieto RA, Deardorff WJ, Grossberg GT. Efficacy of rivastigmine tartrate, transdermal system, in Alzheimer's disease. Expert Opin Pharmacother. 2016;17(6):861-70.

[2]Han HJ, Lee JJ, et al. Efficacy and safety of switching from oral cholinesterase inhibitors to the rivastigmine transdermal patch in patients with probable Alzheimer's disease. J Clin Neurol. 2011 Sep;7(3):137-42.

[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]Polinsky RJ. Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Clin Ther. 1998 Jul-Aug;20(4):634-47. doi: 10.1016/s0149-2918(98)80127-6. PMID: 9737824.

[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 tartrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.49mL

2.50mL

1.25mL

24.97mL

4.99mL

2.50mL

Rivastigmine tartrate 技术信息

CAS号129101-54-8
分子式C18H28N2O8
分子量 400.423
别名 L-酒石酸卡巴拉汀 ;SDZ-ENA 713;ENA 713;Exelon;Rivastigmine (tartrate)
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

H2O: 50 mg/mL(124.87 mM),配合低频超声助溶

动物实验配方
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