货号:A193069 同义名: L-酒石酸卡巴拉汀 / SDZ-ENA 713;ENA 713
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.
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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 |
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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。 |
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]. |
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 | - | - | |
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 |
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 |