Rufinamide

Catalog No.S1256 Synonyms: CGP 33101

For research use only.

Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

Rufinamide Chemical Structure

CAS No. 106308-44-5

Purity & Quality Control

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Biological Activity

Description Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
Targets
Sodium channel [1]
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]

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 (from reference)

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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C(=C1)F)CN2C=C(N=N2)C(=O)N)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01151540 Completed Drug: Rufinamide Lennox-Gastaut Syndrome Eisai Co. Ltd.|Eisai Inc. November 2010 Phase 3
NCT01991041 Completed -- Lennox-Gastaut Syndrome Eisai Limited|Eisai Inc. June 2008 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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