| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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Description: Rivastigmine, also known as ENA-713 and SDZ-ENA 713, is a reversible cholinesterase inhibitor with IC50 of 5.5 μM, it 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 |
Rivastigmine (S-rivastigmine; 1 µM; 24 hours) coupled with carbachol (10 µM) reduced LPS (2.5 µg/ml)-induced TNF-α and IL-6 by 50% and 46%, respectively. % without making any substantial impact. Pro-inflammatory cytokines are lowered [3]. Rivastigmine (1 µM), carbachol (10 µM), or a combination of both medications show no cytotoxic effects on activated cells [3].
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| ln Vivo |
An intraperitoneal injection of rivastigmine (S-rivastigmine; 0.5-2.5 mg/kg; administered 60 minutes prior to testing) markedly and dose-dependently alleviated behavioral abnormalities caused by aluminum [4]. In BALB/c OlaHsd male 8–9 week old mice weighing 200–250 grams with acute colitis, rivastigmine (0.5, 1 mg/kg/day; SC; for 8 days) decreases IL-6 concentrations by roughly 50% and 60%, respectively, but not TNF-α and IL-1β concentrations [3]. At 1 mg/kg, rivastigmine totally stopped bleeding and inhibited colonic contractions, but not at 0.5 mg/kg. While rivastigmine (1 mg/kg) reduced submucosal edema and cellular infiltration, treatment with rivastigmine (0.5 mg/kg) showed minimal change in these pathological findings. Additionally, partial recovery of the crypt architecture was observed. At the conclusion of the trial, a 4.7% weight reduction was achieved with 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
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|---|---|
| Molecular Weight |
250.34
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| CAS # |
123441-03-2
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| Related CAS # |
Rivastigmine tartrate;129101-54-8;(rac)-Rivastigmine-d6;194930-04-6
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| SMILES |
O=C(N(C)CC)OC1=CC=CC([C@H](C)N(C)C)=C1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ≥ 50 mg/mL (~199.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9946 mL | 19.9728 mL | 39.9457 mL | |
| 5 mM | 0.7989 mL | 3.9946 mL | 7.9891 mL | |
| 10 mM | 0.3995 mL | 1.9973 mL | 3.9946 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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