| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
(R)-Rivastigmine D6 tartrate targets cholinesterase enzymes, specifically acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). As a deuterium-labeled analog of (R)-Rivastigmine, this compound acts as a cholinesterase inhibitor. The parent compound, Rivastigmine, is a carbamate-type inhibitor that forms a covalent bond with the esteratic site of the enzyme, leading to reversible inactivation of cholinesterases. By inhibiting these enzymes, Rivastigmine increases the concentration of acetylcholine in the synaptic cleft, enhancing cholinergic neurotransmission.
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| ln Vitro |
(R)-Rivastigmine D6 tartrate is a deuterium-labeled compound and its in vitro activity is comparable to that of the non-labeled (R)-Rivastigmine. The parent compound Rivastigmine is a potent inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The deuterium labeling does not significantly alter the compound's pharmacological activity but provides a mass shift that is useful for analytical detection and quantification. The compound is used as an internal standard in analytical methods for measuring Rivastigmine concentrations in biological samples.
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| ln Vivo |
(R)-Rivastigmine D6 tartrate is not typically used for in vivo pharmacological studies as it is primarily an analytical standard. The parent compound, Rivastigmine, is clinically used for the treatment of mild to moderate Alzheimer's disease and Parkinson's disease dementia. As a cholinesterase inhibitor, Rivastigmine increases acetylcholine levels in the brain, improving cognitive function in patients with dementia. The deuterium-labeled compound serves as an internal standard for quantifying Rivastigmine in pharmacokinetic and bioanalytical studies.
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| Enzyme Assay |
(R)-Rivastigmine D6 tartrate is used as an analytical standard and does not have a typical receptor binding assay protocol. The compound is used in LC-MS or GC-MS methods as an internal standard for the quantification of Rivastigmine. In these assays, a known amount of the deuterium-labeled compound is added to biological samples (e.g., plasma, urine, or tissue homogenates). Samples are extracted and analyzed by LC-MS or GC-MS, and the ratio of the analyte (Rivastigmine) to the internal standard ((R)-Rivastigmine D6) is used to calculate the concentration of Rivastigmine.
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| Cell Assay |
(R)-Rivastigmine D6 tartrate is used in analytical chemistry applications rather than traditional cell-based assays. The compound is added as an internal standard to biological samples prior to extraction and LC-MS or GC-MS analysis. In research settings, the compound may be used in cell culture experiments to study the metabolism or uptake of Rivastigmine, where the deuterium-labeled compound serves as a tracer or internal standard for quantifying the parent compound and its metabolites.
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| Animal Protocol |
(R)-Rivastigmine D6 tartrate is not used directly in animal studies as a therapeutic agent. The compound is used as an internal standard in pharmacokinetic studies of Rivastigmine in animal models. In these studies, animals are administered Rivastigmine, and plasma or tissue samples are collected at various time points. (R)-Rivastigmine D6 tartrate is added to the samples as an internal standard, and the samples are analyzed by LC-MS or GC-MS to quantify Rivastigmine concentrations. This allows for the determination of pharmacokinetic parameters such as half-life, clearance, and bioavailability.
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| ADME/Pharmacokinetics |
(R)-Rivastigmine D6 tartrate has a molecular weight of 406.46 and a molecular formula of C18H22D6N2O8. The compound is used as an internal standard for the quantification of Rivastigmine by GC or LC-MS. The deuterium labeling provides a mass shift of 6 Da relative to the non-labeled compound, allowing for clear differentiation in mass spectrometric detection. The compound is typically used in bioanalytical method development and validation for pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
(R)-Rivastigmine D6 tartrate is a research compound and comprehensive toxicology data are not applicable as it is used as an analytical standard rather than a therapeutic agent. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional chemical hygiene guidelines.
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| Additional Infomation |
(R)-Rivastigmine D6 tartrate is the deuterium-labeled form of (R)-Rivastigmine, a cholinesterase inhibitor. It is intended for use as an internal standard for the quantification of Rivastigmine by GC- or LC-MS. Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits both butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). The parent compound is clinically used for the treatment of Alzheimer's disease and Parkinson's disease dementia. (R)-Rivastigmine D6 tartrate is for research purposes only and is not approved for therapeutic use.
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| Molecular Formula |
C18H22D6N2O8
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|---|---|
| Molecular Weight |
406.461
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| Exact Mass |
406.222
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| CAS # |
194930-00-2
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| Related CAS # |
Rivastigmine tartrate;129101-54-8
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| PubChem CID |
76973134
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| Appearance |
White to off-white solid powder
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| LogP |
0.637
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
402
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O=C(OC1=CC=CC([C@@H](C)N(C([2H])([2H])[2H])C([2H])([2H])[2H])=C1)N(CC)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O
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| InChi Key |
GWHQHAUAXRMMOT-XVXYZIQCSA-N
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| InChi Code |
InChI=1S/C14H22N2O2.C4H6O6/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4;5-1(3(7)8)2(6)4(9)10/h7-11H,6H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t11-;1-,2-/m01/s1/i3D3,4D3;
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| Chemical Name |
[3-[(1S)-1-[bis(trideuteriomethyl)amino]ethyl]phenyl] N-ethyl-N-methylcarbamate;(2R,3R)-2,3-dihydroxybutanedioic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4603 mL | 12.3013 mL | 24.6027 mL | |
| 5 mM | 0.4921 mL | 2.4603 mL | 4.9205 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4603 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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