Rivastigmine tartrate
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.03%
- CAS. Nr.: 129101-54-8
- Formel: C18H28N2O8
- Molecular Weight:400.42
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Rivastigmine tartrate
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Biologische Aktivität
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AChE |
Rivastigmine tartrate (ENA 713; 1 μM; 24 hours) reduces LPS (2.5 μg/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 μM), respectively and does not cause any significant reduction in pro-inflammatory cytokines [3].
Rivastigmine tartrate (1 μM), carbachol (10 μM), or a combination of both drugs, does not have a cytotoxic effect on activated cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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[3].
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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar albino rats weighing 190–240 g (90 days old)[4]
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Dosage:0.5, 1, 1.5 and 2.5 mg/kg
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Administration:IP; single dose
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Result:Significantly and dose-dependently improved the behavioral impairments caused by Aluminum (100 mg/kg/day; i.p.; for 60 days)
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 129101-54-8
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Appearance Solid
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Molecular Weight 400.42
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Formel C18H28N2O8
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Color White to off-white
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SMILES
O=C(OC1=CC=CC([C@@H](N(C)C)C)=C1)N(CC)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O
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Synonyms
ENA 713; SDZ-ENA 713
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
2021 Dec;8(24):e2100808. PMID: 34719888
Lösungsmittel & Löslichkeit
H2O : 50 mg/mL (124.87 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (249.74 mM); Clear solution; Need ultrasonic
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (564 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.4974 mL | 12.4869 mL | 24.9738 mL | 62.4344 mL |
| 5 mM | 0.4995 mL | 2.4974 mL | 4.9948 mL | 12.4869 mL | |
| 10 mM | 0.2497 mL | 1.2487 mL | 2.4974 mL | 6.2434 mL | |
| 15 mM | 0.1665 mL | 0.8325 mL | 1.6649 mL | 4.1623 mL | |
| 20 mM | 0.1249 mL | 0.6243 mL | 1.2487 mL | 3.1217 mL | |
| 25 mM | 0.0999 mL | 0.4995 mL | 0.9990 mL | 2.4974 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8325 mL | 2.0811 mL | |
| 40 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5609 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL | 1.2487 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0406 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Rivastigmine tartrate Related Classifications
HY-11017 Related Classifications
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