| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Targets |
Dimethadione is a metabolite of the anticonvulsant drug trimethadione. Trimethadione is a prodrug that is metabolized to dimethadione, which is the active anticonvulsant metabolite. Dimethadione acts as an anticonvulsant by reducing T-type calcium channel currents in thalamic neurons, thereby suppressing the abnormal oscillatory activity that underlies absence seizures. As a metabolite, its targets are similar to those of trimethadione, primarily involving voltage-gated calcium channels in the central nervous system.
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| ln Vitro |
In vitro, dimethadione is the active metabolite of trimethadione and exhibits anticonvulsant activity. It reduces T-type calcium channel currents in thalamic neurons, suppressing abnormal neuronal firing. However, specific in vitro activity data for dimethadione alone are limited, as most studies have focused on trimethadione. The compound may also affect other ion channels and neurotransmitter systems at higher concentrations.
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| ln Vivo |
In vivo, dimethadione is the active metabolite of trimethadione that mediates its anticonvulsant effects. Trimethadione is metabolized to dimethadione in the liver, and the metabolite accumulates in the body due to its long half-life. The anticonvulsant activity of trimethadione in animal models of absence seizures is attributed to dimethadione. However, specific in vivo efficacy data for dimethadione as a single compound are limited.
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| Enzyme Assay |
There are no specific in vitro enzyme or receptor binding assays for dimethadione as a drug target. As an anticonvulsant metabolite, it may be studied in ion channel assays using patch-clamp electrophysiology on thalamic neurons expressing T-type calcium channels. The compound is incubated with cells at various concentrations (typically 1-1000 μM), and calcium currents are recorded before and after compound application to assess inhibition. However, detailed assay protocols for this specific compound are not extensively reported.
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| Cell Assay |
There are no specific in vitro cellular assays for dimethadione as a pharmacologically active compound. As an anticonvulsant, it can be tested in neuronal cell cultures or primary thalamic neurons. Cells are cultured in appropriate media and treated with various concentrations of the compound (typically 1-1000 μM) for 1-24 hours. T-type calcium channel activity is assessed by patch-clamp electrophysiology or calcium imaging. Cell viability is assessed using MTT assays. However, detailed protocols for this specific compound are not extensively reported.
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| Animal Protocol |
There are no specific in vivo animal studies for dimethadione as a single compound. As the active metabolite of trimethadione, its effects are studied indirectly through trimethadione administration. Typical animal models of absence seizures (e.g., genetic absence epilepsy rats from Strasbourg, GAERS) are used. Trimethadione is administered orally or intraperitoneally at doses of 50-300 mg/kg, and seizure activity is monitored by EEG. The anticonvulsant effects are attributed to its metabolite dimethadione.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Dimethyldione is a known human metabolite of trimethyldione. Pharmacokinetic properties of dimethadione: Dimethadione is the active metabolite of trimethadione. It has a long elimination half-life (several days) due to its low protein binding and extensive distribution. It is primarily excreted unchanged in urine. The compound accumulates in the body with repeated dosing of trimethadione. Specific PK parameters such as Cmax, AUC, and bioavailability for dimethadione as a single compound are not extensively reported. |
| Toxicity/Toxicokinetics |
The toxicity profile of dimethadione is related to its use as a metabolite of trimethadione. Trimethadione has been associated with adverse effects including sedation, dizziness, and hematological abnormalities. Dimethadione accumulates in the body and contributes to the drug's toxicity profile. The compound is for research use only and not for human therapeutic use. Standard toxicity studies would include assessment of neurotoxicity, hepatotoxicity, and hematological effects. No specific genotoxicity data are reported.
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| References | |
| Additional Infomation |
5,5-Dimethyloxazolidine-2,4-dione is an oxazolidine ketone compound. It is the active metabolite of trimethyldione and is an anticonvulsant.
Dimethadione (CAS 695-53-4) is the demethylated metabolite of trimethadione, an anticonvulsant drug formerly used to treat absence seizures. It has a molecular formula of C5H7NO3 and a molecular weight of 129.12. The compound is a white to almost white powder with a melting point of 75-77°C. It is primarily used as a pharmaceutical impurity standard and research chemical. Dimethadione is not approved for clinical use and is available for research purposes only. |
| Molecular Formula |
C5H7NO3
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|---|---|
| Molecular Weight |
129.1140
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| Exact Mass |
129.042
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| CAS # |
695-53-4
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| PubChem CID |
3081
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
137 °C / 6mmHg
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| Melting Point |
77-80 °C(lit.)
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| Flash Point |
44.2ºC
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| Index of Refraction |
1.442
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| LogP |
0.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
9
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| Complexity |
173
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(N([H])C(C1(C([H])([H])[H])C([H])([H])[H])=O)=O
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| InChi Key |
JYJFNDQBESEHJQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H7NO3/c1-5(2)3(7)6-4(8)9-5/h1-2H3,(H,6,7,8)
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| Chemical Name |
5,5-dimethyl-1,3-oxazolidine-2,4-dione
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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) |
DMSO : ~100 mg/mL (~774.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (19.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (19.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (19.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.7453 mL | 38.7267 mL | 77.4533 mL | |
| 5 mM | 1.5491 mL | 7.7453 mL | 15.4907 mL | |
| 10 mM | 0.7745 mL | 3.8727 mL | 7.7453 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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