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Rufinamide Sodium Channel inhibitor

Name: Rufinamide
Brand: Selleck Chemicals
SKU: S1256
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1256

Rufinamide (CGP 33101,E 2080,RUF 331,Banzel) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

Chemical Structure

Molecular Weight: 238.19

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	CD markers AChR Calcium Channel Potassium Channel GABA Receptor ATPase TRP Channel GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel MCT Amino acid transporter GLUT CRM1 VDAC BCRP NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
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Chemical Information, Storage & Stability

Molecular Weight	238.19	Formula	C₁₀H₈F₂N₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	106308-44-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGP 33101,E 2080,RUF 331,Banzel			Smiles	C1=CC(=C(C(=C1)F)CN2C=C(N=N2)C(=O)N)F

Solubility

In vitro
Batch:

DMSO : 47 mg/mL ( (197.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	Sodium channel ^[1]
In vitro	Rufinamide is extensively metabolised by non-CYP450 systems with a half-life of 8-12 hours. Its mechanism of action is thought to be inhibition of sodium-dependent action potentials in neurons, with possible membrane-stabilising effects. ^[1] This compound 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] This compound alleviates injury-induced mechanical allodynia for 4 hours. It 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] This chemical 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). It suppresses pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively). This compound is partially effective in the mouse strychnine test. ^[5]
References	https://pubmed.ncbi.nlm.nih.gov/17073844/ https://pubmed.ncbi.nlm.nih.gov/22022867/ https://pubmed.ncbi.nlm.nih.gov/22132708/ https://pubmed.ncbi.nlm.nih.gov/23221868/ https://pubmed.ncbi.nlm.nih.gov/18325020/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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