Rufinamide
Catalog No.S1256 Synonyms: CGP 33101
Molecular Weight(MW): 238.19
Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
Purity & Quality Control
Choose Selective Sodium Channel Inhibitors
Biological Activity
| Description | Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication. | |
|---|---|---|
| Targets |
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| In vitro |
Rufinamide is extensively metabolised by non-CYP450 systems with a half-life of 8-12 hours. Rufinamide’s mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects. [1] Rufinamide hydrolysis is mediated primarily by human carboxylesterase (hCE) 1 and is nonsaturable up to 500 μM. [2] |
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| In vivo | Rufinamide given orally at 20 mg/kg every 12 h in healthy dogs should result in a plasma concentration and half-life sufficient to achieve the therapeutic level extrapolated from humans without short-term adverse effects in adult dogs. [3] Rufinamide alleviates injury-induced mechanical allodynia for 4 hours. Rufinamide reduces peak current and stabilizes the inactivated state of voltage-gated sodium channel Nav1.7, with similar effects in dorsal root ganglion neurons in the Spared Nerve Injury neuropathic pain model in mice. [4] Rufinamide suppresses pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and is active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg). Rufinamide suppresses pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). Rufinamide is partially effective in the mouse strychnine test. [5] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 18 mg/mL warmed (75.56 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 238.19 |
|---|---|
| Formula | C10H8F2N4O |
| CAS No. | 106308-44-5 |
| Storage | powder |
| Synonyms | CGP 33101 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02095899 | Withdrawn | Peripheral Nerve Injuries|Pain | University of Zurich | March 2014 | Phase 2 |
| NCT02332174 | Completed | Seizures | Wuhan Union Hospital, China | March 2014 | Phase 1 |
| NCT02175173 | Active, not recruiting | Lennox-Gastaut Syndrome | Eisai Co., Ltd.|Eisai Inc. | June 2013 | -- |
| NCT01405053 | Completed | Lennox-Gastaut Syndrome | Eisai Inc. | June 2011 | Phase 3 |
| NCT01146951 | Completed | Lennox-Gastaut Syndrome | Eisai Limited|Eisai Inc. | June 2010 | Phase 3 |
| NCT00448539 | Completed | Refractory Partial Onset Seizures | Eisai Inc. | March 2007 | Phase 3 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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