(S)-Rivastigmine-d4
(S)-Rivastigmine-d4 is deuterium labeled Rivastigmine. Rivastigmine (ENA 713 free base) 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 can pass the blood brain barrier (BBB). Rivastigmine 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.
For research use only. We do not sell to patients.
- Formula: C14H18D4N2O2
- Molecular Weight:254.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 123441-03-2
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Molecular Weight 254.36
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Formula C14H18D4N2O2
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SMILES
CCN(C(OC1=CC([C@@H](N(C([2H])([H])[2H])C([2H])([H])[2H])C)=CC=C1)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : ≥ 50 mg/mL (196.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. 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]
[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]. 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]
[5]. 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
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9314 mL | 19.6572 mL | 39.3144 mL | 98.2859 mL |
| 5 mM | 0.7863 mL | 3.9314 mL | 7.8629 mL | 19.6572 mL | |
| 10 mM | 0.3931 mL | 1.9657 mL | 3.9314 mL | 9.8286 mL | |
| 15 mM | 0.2621 mL | 1.3105 mL | 2.6210 mL | 6.5524 mL | |
| 20 mM | 0.1966 mL | 0.9829 mL | 1.9657 mL | 4.9143 mL | |
| 25 mM | 0.1573 mL | 0.7863 mL | 1.5726 mL | 3.9314 mL | |
| 30 mM | 0.1310 mL | 0.6552 mL | 1.3105 mL | 3.2762 mL | |
| 40 mM | 0.0983 mL | 0.4914 mL | 0.9829 mL | 2.4571 mL | |
| 50 mM | 0.0786 mL | 0.3931 mL | 0.7863 mL | 1.9657 mL | |
| 60 mM | 0.0655 mL | 0.3276 mL | 0.6552 mL | 1.6381 mL | |
| 80 mM | 0.0491 mL | 0.2457 mL | 0.4914 mL | 1.2286 mL | |
| 100 mM | 0.0393 mL | 0.1966 mL | 0.3931 mL | 0.9829 mL |