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产品描述： Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease |
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靶点：
IC50: 0.037 μM (BChE) and 4.15 μM (AChE);AChR;AChE |
体内研究：
Rivastigmine tartrate (ENA 713; 0.5-2.5 mg/kg; IP; 60 min before the tests) significantly and dose-dependently improved the behavioral impairments caused by Aluminum (HY-B1521). Rivastigmine (0.5, 1 mg/kg/day; s.c; for 8 days) reduces by about 50% and 60% respectively, the concentration of IL-6 but not those of TNF-α and IL-1β in BALB/c OlaHsd male mice aged 8-9 weeks weighing 200–250 g with acute colitis. Rivastigmine (1 mg/kg), but not (0.5 mg/kg), partially antagonized colon shrinkage and completely prevented bleeding. Treatment with rivastigmine (0.5 mg/kg) causes little change in these pathological manifestations, but rivastigmine (1 mg/kg) causes a partial restoration of the structure of the crypts and a reduction in sub-mucosal edema and cell infiltration. Rivastigmine (1 mg/kg) causes a 4.7% reduction in body weight at the end of the experiment |
参考文献：
1. Qian-Sheng Yu, et al. Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. J Med Chem. 2002 Aug 15;45(17):3684-91. 2. Han HJ, Lee JJ, Park SA 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. Helena Shifrin, et al. 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. 4. Raafat A Abdel-Aal, et al. Rivastigmine reverses aluminum-induced behavioral changes in rats. Eur J Pharmacol. 2011 Jun 1;659(2-3):169-76. |
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溶解性：
H2O : 50 mg/mL (124.87 mM; Need ultrasonic) |
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保存条件：
RT |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.497 ml |
12.487 ml |
24.973 ml |
| 5 mM |
0.499 ml |
2.497 ml |
4.995 ml |
| 10 mM |
0.25 ml |
1.249 ml |
2.497 ml |
| 50 mM |
0.05 ml |
0.25 ml |
0.499 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京