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Purity: ≥98%
Rivastigmine Tartrate (formerly ENA-713, SDZ-ENA 713; Exelon, Exelon Patch), the tartrate salt of rivastigmine, is a potent and reversible cholinesterase inhibitor used to treat mild to moderate dementia caused by Alzheimer's or Parkinson's disease. It inhibits cholinesterase with an IC50 of 5.5 μM, and is used as a parasympathomimetic or cholinergic agent for the management of mild to moderate Alzheimer disease, Dementia, and Parkinson's Disease. Rivastigmine is a carbamate-derived reversible cholinesterase inhibitor that is selective for the central nervous system. It acts by covalently modifying a serine residue in the active site by carbamoylation, as it stabilizes or reduces the rate of decline in certain cognitive functions.
| ln Vitro |
When coupled with carbachol (10 µM), rivastigmine tartrate (ENA 713; 1 µM; 24 hours) decreased TNF-α and IL-6 produced by LPS (2.5 µg/ml) by 50% and 46%, respectively. and has little to no noticeable effect. Decreases in pro-inflammatory cytokines occur [3]. On activated cells, rivastigmine tartrate (1 µM), carbachol (10 µM), or a mix of the two medications show no harmful effects [3].
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| ln Vivo |
Rivastigmine tartrate (ENA 713; 0.5-2.5 mg/kg; IP; 60 minutes before testing) aluminum-induced behavioral abnormalities were considerably and dose-dependently alleviated [4]. When administered intraperitoneally (SC) to BALB/c OlaHsd male mice 8–9 weeks old weighing 200–250 grams and suffering from acute colitis, rivastigmine (0.5, 1 mg/kg/day; SC; for 8 days) decreases IL-6 concentrations by around 50% and 60%, respectively, but does not affect TNF-α. In contrast to 0.5 mg/kg, rivastigmine (1 mg/kg) totally stopped bleeding and very slightly inhibited colonic contractions. Little changed in these pathological findings after treatment with rivastigmine (0.5 mg/kg); however, rivastigmine (1 mg/kg) reduced submucosal edema and cellular infiltration and partially restored the crypt architecture. At the conclusion of the experiment, 4.7% of the participants lost weight when using rivastigmine (1 mg/kg) [3].
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| Animal Protocol |
Animal/Disease Models: Male Wistar albino rat, body weight 190–240 g (90 days old) [4]
Doses: 0.5, 1, 1.5 and 2.5 mg/kg Route of Administration: intraperitoneal (ip) injection; single dose Experimental Results: significant and dose Dependently improves aluminum-induced behavioral disturbances (100 mg/kg/day; i.p.; for 60 days) |
| References |
[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. |
| Molecular Formula |
C14H22N2O2.C4H6O6
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| Molecular Weight |
400.42
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| CAS # |
129101-54-8
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| Related CAS # |
(S)-Rivastigmine-d6 tartrate;194930-00-2;Rivastigmine;123441-03-2
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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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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4974 mL | 12.4869 mL | 24.9738 mL | |
| 5 mM | 0.4995 mL | 2.4974 mL | 4.9948 mL | |
| 10 mM | 0.2497 mL | 1.2487 mL | 2.4974 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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