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| Targets |
Voltage-gated sodium channels. Carbamazepine-D10 is a stable isotope-labeled version of carbamazepine. The deuterium atoms are expected to have a minimal kinetic isotope effect on the drug's pharmacodynamics, meaning it retains the same primary mechanism of action as the parent drug. Carbamazepine blocks voltage-gated sodium channels in neurons, particularly in the inactivated state, preventing high-frequency repetitive firing of action potentials. This action stabilizes neuronal membranes and is the basis for its anticonvulsant, antiepileptic, and analgesic (trigeminal neuralgia) properties.
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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].
Because Carbamazepine-D10 is a stable isotope-labeled internal standard, it is not typically used for in vitro activity assessment. Instead, its utility lies in its identical chemical behavior to the unlabeled drug during sample preparation (extraction, derivatization) and chromatographic separation, while being distinguishable by mass spectrometry. The substitution of hydrogen atoms (¹H) with the heavier isotope deuterium (2H) results in a predictable mass shift (m/z 246.33 for the D10 vs. m/z 236.27 for the parent), which allows for its use as an internal standard. The isotope purity is typically >98% D. |
| ln Vivo |
In biological sample analysis, Carbamazepine-D10 is used to correct for matrix effects, extraction recovery, and instrument variability. A known concentration of the labeled internal standard is added to each sample (plasma, urine, tissue homogenate) before processing. Because it co-elutes with the analyte (carbamazepine) but is resolved by mass, the detector can separately measure the signals of the drug and the standard. Any loss of the internal standard during sample preparation is assumed to be identical to that of the drug, allowing for precise quantification. It is not used in cell-based assays for pharmacological effect.
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| Enzyme Assay |
The use of Carbamazepine-D10 is confined to analytical method validation and routine sample analysis. A typical protocol for an LC-MS/MS assay involves spiking a volume of plasma (e.g., 50-100 uL) with a known amount of Carbamazepine-D10 (e.g., 10-100 ng/mL). The samples are then processed, typically by protein precipitation with acetonitrile or by solid-phase extraction (SPE). The resulting extract is injected onto a reverse-phase C18 HPLC column. The column eluent is directed into a mass spectrometer operated in positive ion electrospray (ESI+) multiple reaction monitoring (MRM) mode. The transition for the drug (e.g., m/z 237.0 → 194.1) and the internal standard (e.g., m/z 246.3 → 203.2) are monitored. The concentration of the drug is calculated using a calibration curve of drug-to-internal standard peak area ratios.
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| Cell Assay |
As a stable isotope internal standard, Carbamazepine-D10 is not used in cell culture. Its application is entirely in the field of bioanalysis. Quality control (QC) samples, prepared by spiking blank plasma with known, low, middle, and high concentrations of carbamazepine and a fixed concentration of internal standard, are used to validate the assay's accuracy and precision. The internal standard compensates for any variability in the instrument response, injection volume, and ion suppression. Cell-based studies are not applicable, as the compound is a non-biological standard.
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| Animal Protocol |
In animal studies, Carbamazepine-D10 is administered as an internal standard (IS) for the quantification of carbamazepine in pharmacokinetic (PK) or tissue distribution studies. For example, an animal is dosed with non-labeled carbamazepine, and blood samples are collected over time. A fixed amount of Carbamazepine-D10 is spiked into each plasma sample after collection. The concentration of carbamazepine in the plasma is then determined by LC-MS/MS, and the D10-labeled compound serves as the IS. This method allows for accurate and precise determination of PK parameters (Cmax, Tmax, AUC, t1/2). The internal standard itself is not used to assess pharmacodynamics.
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| ADME/Pharmacokinetics |
Carbamazepine-D10 (as an internal standard) has the same physicochemical properties as the unlabeled drug. Carbamazepine is known to have a slow and variable absorption rate after oral administration, with a Tmax of 4-12 hours. It is highly protein-bound (70-80%). It is a potent inducer of hepatic cytochrome P450 enzymes (especially CYP3A4) and of its own metabolism (auto-induction), leading to a variable half-life (20-65 hours) after chronic dosing. The compound is extensively metabolized to its active 10,11-epoxide metabolite. These ADME properties are the same for the deuterated form, which is crucial for its use as an internal standard.
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| Toxicity/Toxicokinetics |
The toxicity of Carbamazepine-D10 is presumed to be the same as that of the parent drug, though as an internal standard, it is used in trace amounts (sub-milligram quantities) and is not intended for human administration. The parent drug's toxicity includes dose-related adverse effects such as drowsiness, dizziness, ataxia, and hyponatremia. Rare but serious side effects include Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and aplastic anemia. The compound is a known teratogen and should be handled with caution. For laboratory use, standard safety protocols for handling cytotoxic and hazardous drugs should be followed.
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| References |
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| Additional Infomation |
Carbamazepine-D10 is a research-grade compound used exclusively as an internal standard for the quantification of carbamazepine in biological matrices. The deuteration replaces ten hydrogen atoms, providing a mass increase of 10 Da. This compound is essential for regulatory bioanalysis (GLP-compliant studies) to accurately measure drug concentrations in clinical and preclinical studies. It is supplied as a stable, neat solid or in solution. The molecular formula is C15H2D10N2O, with a molecular weight of 246.33. It is not approved for therapeutic use and is intended for laboratory research only. The parent drug, carbamazepine, was first approved by the FDA in 1974 for the treatment of epilepsy and trigeminal neuralgia.
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| Molecular Formula |
C15H12N2O
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| Molecular Weight |
246.330200195313
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| Exact Mass |
246.157
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| CAS # |
132183-78-9
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| Related CAS # |
Carbamazepine;298-46-4;Carbamazepine-(Ph)d8
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| PubChem CID |
12412209
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
411.0±48.0 °C at 760 mmHg
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| Flash Point |
202.4±29.6 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
2.67
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
326
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1=C(C(=C2C(=C1[2H])C(=C(C3=C(C(=C(C(=C3N2C(=O)N)[2H])[2H])[2H])[2H])[2H])[2H])[2H])[2H]
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| InChi Key |
FFGPTBGBLSHEPO-LHNTUAQVSA-N
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| InChi Code |
InChI=1S/C15H12N2O/c16-15(18)17-13-7-3-1-5-11(13)9-10-12-6-2-4-8-14(12)17/h1-10H,(H2,16,18)/i1D,2D,3D,4D,5D,6D,7D,8D,9D,10D
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| Chemical Name |
1,2,3,4,5,6,7,8,9,10-decadeuteriobenzo[b][1]benzazepine-11-carboxamide
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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 | 4.0596 mL | 20.2980 mL | 40.5959 mL | |
| 5 mM | 0.8119 mL | 4.0596 mL | 8.1192 mL | |
| 10 mM | 0.4060 mL | 2.0298 mL | 4.0596 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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