| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Donepezil-d4 hydrochloride targets acetylcholinesterase (AChE), acting as a reversible and selective inhibitor. It has an IC50 of 6.7 nM for AChE and is selective for AChE over butyrylcholinesterase (BChE), for which it has an IC50 of 988 nM. The deuterated compound is used as an analytical internal standard.
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|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
Donepezil-d4 hydrochloride is not pharmacologically active in its own right; it serves as an analytical internal standard. It exhibits the same physicochemical properties as native donepezil hydrochloride, including similar chromatographic behavior and ionization efficiency. The compound is used to correct for matrix effects, extraction efficiency, and instrument variability in quantitative analyses. Donepezil-d4 hydrochloride is used in cell culture experiments as an internal standard for measuring donepezil concentrations. Cells are treated with the deuterated compound at known concentrations, and samples are analyzed by LC-MS. The internal standard corrects for variations in sample preparation and instrument response. |
| ln Vivo |
In vivo, Donepezil-d4 hydrochloride is used as an internal standard for quantifying donepezil concentrations in plasma and other biological fluids. It is added to samples prior to analysis. The compound enables accurate measurement of donepezil levels in pharmacokinetic and therapeutic drug monitoring studies.
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| Enzyme Assay |
Cell-free receptor binding assays are not applicable for Donepezil-d4 hydrochloride as it is not a pharmacologically active compound. However, the deuterated standard is used in analytical method development for donepezil quantification. Validation experiments demonstrate that it exhibits identical chromatographic retention time and ionization efficiency as native donepezil.
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| Cell Assay |
Cellular assays using Donepezil-d4 hydrochloride are limited to its use as an analytical internal standard. Cells are cultured and treated with the compound at known concentrations, followed by sample preparation and LC-MS analysis. The compound is used to validate analytical methods for donepezil quantification in cellular models.
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| ADME/Pharmacokinetics |
As an internal standard, Donepezil-d4 hydrochloride exhibits identical pharmacokinetic behavior to native donepezil. It is used in GC- or LC-MS methods to measure donepezil concentrations in plasma and other biological fluids. The deuterated compound enables accurate and reliable quantification of donepezil in pharmacokinetic and therapeutic drug monitoring studies.
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| Toxicity/Toxicokinetics |
Donepezil-d4 hydrochloride is not a therapeutic agent and toxicity studies are not applicable. It is used in trace amounts as an analytical internal standard. Standard laboratory safety practices for handling chemical reference standards should be followed.
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| References |
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| Additional Infomation |
Donepezil-d4 hydrochloride is a high-purity deuterated compound used as an internal standard for the quantification of donepezil in biological samples. It is essential for analytical method development, method validation, and quality control applications. The incorporation of deuterium enhances the molecule's stability and facilitates detailed pharmacokinetic and metabolic studies. The compound is not intended for therapeutic use.
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| Molecular Formula |
C24H26D4CLNO3
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|---|---|
| Molecular Weight |
419.98
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| Exact Mass |
415.191
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| CAS # |
1219798-88-5
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| Related CAS # |
Donepezil Hydrochloride;120011-70-3
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| PubChem CID |
131869293
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])(C1CCN(CC1)C([2H])([2H])C2=CC=CC=C2)C3CC4=CC(=C(C=C4C3=O)OC)OC.Cl
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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 |
| 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 | 2.3811 mL | 11.9053 mL | 23.8107 mL | |
| 5 mM | 0.4762 mL | 2.3811 mL | 4.7621 mL | |
| 10 mM | 0.2381 mL | 1.1905 mL | 2.3811 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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