| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Topiramate D12 targets the same receptors as its unlabeled parent drug. Topiramate is a broad-spectrum antiepileptic agent. It is an antagonist of the GluR5 receptor, a subtype of the kainate receptor. By blocking this receptor, it modulates excitatory neurotransmission in the brain.
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|---|---|
| ln Vitro |
Topiramate D12 is primarily used as an analytical internal standard rather than for its pharmacological activity. Topiramate is a broad-spectrum antiepileptic drug. The compound is used in LC-MS/MS methods for the quantification of Topiramate in biological matrices. The deuterium labeling provides a mass shift for accurate quantification.
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| ln Vivo |
Topiramate D12 is used in pharmacokinetic studies as an internal standard for the quantification of Topiramate. Topiramate is an antiepileptic agent that is an antagonist of the GluR5 receptor. The deuterium-labeled compound can be co-administered with unlabeled drug to study absorption, distribution, metabolism, and excretion. It is used in bioequivalence studies and method validation.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Topiramate D12 are typically performed as part of analytical method validation. The compound is used as an internal standard in LC-MS/MS assays for the quantification of Topiramate. It is dissolved in an appropriate solvent and spiked into biological matrices at known concentrations. Calibration curves are generated by plotting the peak area ratio of Topiramate to Topiramate D12 against the concentration of Topiramate.
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| Cell Assay |
For in vitro cell-based assays, Topiramate D12 can be used in studies investigating Topiramate's cellular effects, though its primary use is as an analytical internal standard. Cells expressing GluR5 receptors are cultured and treated with the compound. Receptor antagonism is confirmed by measuring downstream signaling. However, due to its role as an internal standard, it is more frequently used in analytical quantification.
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| Animal Protocol |
In vivo animal studies with Topiramate D12 are primarily pharmacokinetic. The compound is administered orally to rodents, and blood samples are collected at predetermined time points. Plasma concentrations of both labeled and unlabeled Topiramate are analyzed by LC-MS/MS using Topiramate D12 as the internal standard. Pharmacodynamic effects can be evaluated in seizure models.
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| ADME/Pharmacokinetics |
Topiramate D12 (CAS: 1279037-95-4) has a molecular weight of 351.44 g/mol and a molecular formula of C₁₂H₉D₁₂NO₈S. Synonyms: Epitoma-d12, Topina-d12, Topomax-d12. Storage: Powder -20°C. The compound is a dodeca-deuterated form of Topiramate.
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| Toxicity/Toxicokinetics |
As a deuterium-labeled analog of an approved antiepileptic drug, Topiramate D12 is expected to have a similar toxicity profile to Topiramate, though toxicity studies are typically not performed on the labeled compound. Topiramate is generally well-tolerated, with common side effects including cognitive impairment and weight loss. The compound is used in very small quantities as an analytical internal standard.
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| References | |
| Additional Infomation |
Topiramate D12 (McN 4853 D12) is the deuterium-labeled form of Topiramate, a broad-spectrum antiepileptic drug and a GluR5 receptor antagonist. It is used as an internal standard for analytical method development and pharmacokinetic studies. It is not intended for therapeutic use and is for research and analytical use only.
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| Molecular Formula |
C12H9D12NO8S
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|---|---|
| Molecular Weight |
351.436
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| Exact Mass |
351.174
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| CAS # |
1279037-95-4
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| PubChem CID |
45040550
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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 |
438.7±55.0 °C at 760 mmHg
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| Flash Point |
219.1±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.497
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| LogP |
2.97
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
556
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O1[C@@]2(COS(=O)(=O)N)OC(C([2H])([2H])[2H])(C([2H])([2H])[2H])O[C@H]2[C@@H]2OC(C([2H])([2H])[2H])(C([2H])([2H])[2H])O[C@@H]2C1
|
| InChi Key |
KJADKKWYZYXHBB-RFYKXYJISA-N
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| InChi Code |
InChI=1S/C12H21NO8S/c1-10(2)18-7-5-16-12(6-17-22(13,14)15)9(8(7)19-10)20-11(3,4)21-12/h7-9H,5-6H2,1-4H3,(H2,13,14,15)/t7-,8-,9+,12+/m1/s1/i1D3,2D3,3D3,4D3
|
| Chemical Name |
[(1R,2S,6S,9R)-4,4,11,11-tetrakis(trideuteriomethyl)-3,5,7,10,12-pentaoxatricyclo[7.3.0.02,6]dodecan-6-yl]methyl sulfamate
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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 | 2.8454 mL | 14.2272 mL | 28.4544 mL | |
| 5 mM | 0.5691 mL | 2.8454 mL | 5.6909 mL | |
| 10 mM | 0.2845 mL | 1.4227 mL | 2.8454 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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