2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. Rufinamide

Rufinamide  (Synonyms: CGP 33101; E 2080; RUF 331)

Cat. No.: HY-A0042 Purity: 99.88%
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COA
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Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na+ current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome.

For research use only. We do not sell to patients.

Rufinamide Chemical Structure

Rufinamide Chemical Structure

CAS No. : 106308-44-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Rufinamide Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na+ current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome[1][2][3].

In Vitro

Rufinamide (10-300 μM) selectively binds to the slow-inactivated state (Ii) of Na+ channels in CHO-K1 and human embryonic kidney 293 cells transfected with human NaV 1.7 cDNA, causing a hyperpolarizing shift and a kinase-dependent block, and inhibits the resuscitation current in a dose-dependent manner[1][3].
Rufinamide (100 µM) alleviates neuropathic pain in dorsal root ganglion neurons isolated from C57BL/6 mice by affecting the sodium ion stabilization inactivation effect[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rufinamide Related Antibodies
In Vivo

Rufinamide inhibits maximal electroshock-induced seizures in mice by intraperitoneal injection (ED50: 15.5 mg/kg) and oral administration (ED50: 23.9 mg/kg), in addition, intraperitoneal injection can also inhibit the clonus induced by pentylenetetrazol, Bicuculline (HY-N0219) and Picrotoxin (HY-101391) in mice (ED50: 54.0, 50.5 and 76.3 mg/kg, respectively)[2].
Rufinamide is non-neurotoxic and has a high protection index at doses that reduce seizures (i.p. TD50: 500-1,000 mg/kg; p.o. TD50: ≥ 1,000 mg/kg)[2].
Rufinamide (p.o.) can effectively inhibit MES-induced seizures in Sprague-Dawley rats (ED50: 6.1 mg/kg) and is well tolerated with low toxicity[2].
Rufinamide (i.p., 5-50 mg/kg) dose-dependently alleviates neuropathic pain behaviors in the mouse spared nerve injury model without altering basal mechanical sensitivity or thermal paw withdrawal latency[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (male, aged 4-8 weeks, 20-25 g)[3]
Dosage: 5,10,25,50 mg/kg
Administration: i.p. one dose
Result: Showed dose-dependent relief of SNI-induced allodynia, with effects seen 20 minutes after injection, peaking at 60 minutes, and persisting for at least 4 hours, but subsiding by 24 hours after administration,at the highest dose, allodynia-like behaviors were completely reversed.
Did not cause any changes in sedation or basal pain sensitivity.
Clinical Trial
Molecular Weight

238.19

Formula

C10H8F2N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(CC2=C(F)C=CC=C2F)N=N1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (209.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1983 mL 20.9916 mL 41.9833 mL
5 mM 0.8397 mL 4.1983 mL 8.3967 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.88%

SDS (393 KB)

COA (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1983 mL 20.9916 mL 41.9833 mL 104.9582 mL
5 mM 0.8397 mL 4.1983 mL 8.3967 mL 20.9916 mL
10 mM 0.4198 mL 2.0992 mL 4.1983 mL 10.4958 mL
15 mM 0.2799 mL 1.3994 mL 2.7989 mL 6.9972 mL
20 mM 0.2099 mL 1.0496 mL 2.0992 mL 5.2479 mL
25 mM 0.1679 mL 0.8397 mL 1.6793 mL 4.1983 mL
30 mM 0.1399 mL 0.6997 mL 1.3994 mL 3.4986 mL
40 mM 0.1050 mL 0.5248 mL 1.0496 mL 2.6240 mL
50 mM 0.0840 mL 0.4198 mL 0.8397 mL 2.0992 mL
60 mM 0.0700 mL 0.3499 mL 0.6997 mL 1.7493 mL
80 mM 0.0525 mL 0.2624 mL 0.5248 mL 1.3120 mL
100 mM 0.0420 mL 0.2099 mL 0.4198 mL 1.0496 mL
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Rufinamide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rufinamide106308-44-5CGP 33101 E 2080 RUF 331CGP33101CGP-33101E2080E 2080E-2080RUF331RUF 331RUF-331Sodium ChannelNa channelsNa+ channelsLennox-GastautCHO-K1 cellsSpared Nerve Injury neuropathic pain modelCF1 miceInhibitorinhibitorinhibit

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