| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Sultiame targets carbonic anhydrase (CA) enzymes. It is a pan-inhibitor of carbonic anhydrases, with Kis ranging from 6 to 1,540 nM for CAI, -II, and IV-XIV. By inhibiting carbonic anhydrase, sultiame causes a mild intracellular acidosis in central neurons, which lowers the frequency of epileptiform bursts and action potentials. This anticonvulsant effect is the basis for its use in epilepsy.
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| ln Vitro |
As a sulfonamide, sultiame (also known as sulthiame) inhibits carbonic anhydrase and has antiepileptic properties by causing a mild intracellular acidosis in central neurons, which lowers the frequency of epileptiform bursts and action potentials. [1].
Sultiame is a pan-inhibitor of carbonic anhydrases (CA; Kis = 6-1,540 nM for CAI, -II, and IV-XIV). It is selective for these CAs over CAIII (Ki = 630 µM). As a sulfonamide, sultiame inhibits carbonic anhydrase and has antiepileptic properties. |
| ln Vivo |
Sultiame is used in vivo as an anticonvulsant for the treatment of benign and symptomatic focal epilepsy. It is particularly useful in benign childhood focal epilepsies such as benign rolandic epilepsy. It is also registered for behavioural disorders associated with epilepsy, hyperkinetic behaviour, temporal lobe epilepsy, myoclonic seizures, and Jacksonian seizures.
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| Enzyme Assay |
Sultiame is a carbonic anhydrase inhibitor, and its in vitro activity is assessed in enzyme assays. In a typical assay, the enzyme is incubated with varying concentrations of sultiame and a substrate. The inhibition of enzyme activity is measured, and the Ki is determined.
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| Cell Assay |
Sultiame is dissolved in DMSO and applied to cultured cells at concentrations ranging from 1 nM to 10 µM. The effect on intracellular pH and neuronal activity is assessed.
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| ADME/Pharmacokinetics |
Sultiame has a molecular weight of 290.36 g/mol and a molecular formula of C10H14N2O4S2. It is a sulfonamide compound. The compound is typically stored as a powder at room temperature. Sultiame is also known as sulthiame.
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| Toxicity/Toxicokinetics |
Sultiame has a manageable toxicity profile. Common side effects include gastrointestinal disturbances, headache, and paresthesia. No significant hepatotoxicity or nephrotoxicity has been reported.
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| References | |
| Additional Infomation |
Thiamine sulfate is an organic molecular entity.
Sultiame is a sulfonamide and inhibitor of the enzyme carbonic anhydrase. It is used as an anticonvulsant. Sultiame is a pan-inhibitor of carbonic anhydrases (CA; Kis = 6-1,540 nM for CAI, -II, and IV-XIV). It is used in the treatment of benign and symptomatic focal epilepsy. Sultiame is particularly useful in benign childhood focal epilepsies such as benign rolandic epilepsy. |
| Molecular Formula |
C10H14N2O4S2
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|---|---|
| Molecular Weight |
290.352
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| Exact Mass |
290.039
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| CAS # |
61-56-3
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| Related CAS # |
Sulthiame-d4;1795021-05-4
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| PubChem CID |
5356
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| Appearance |
White to off-white solid powder
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| Density |
1.472g/cm3
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| Boiling Point |
520.2ºC at 760 mmHg
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| Flash Point |
268.4ºC
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| Index of Refraction |
1.609
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| LogP |
3.19
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
481
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HMHVCUVYZFYAJI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H14N2O4S2/c11-18(15,16)10-5-3-9(4-6-10)12-7-1-2-8-17(12,13)14/h3-6H,1-2,7-8H2,(H2,11,15,16)
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| Chemical Name |
4-(1,1-dioxothiazinan-2-yl)benzenesulfonamide
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| Synonyms |
R-594; Riker 594; Sultiame
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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 : ~50 mg/mL (~172.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.31 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 12.5 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: ≥ 1.25 mg/mL (4.31 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 12.5 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: ≥ 1.25 mg/mL (4.31 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 | 3.4441 mL | 17.2206 mL | 34.4412 mL | |
| 5 mM | 0.6888 mL | 3.4441 mL | 6.8882 mL | |
| 10 mM | 0.3444 mL | 1.7221 mL | 3.4441 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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