Riluzole (PK 26124)
For research use only.
Catalog No.S1614 Synonyms: RP-54274
7 publications
CAS No. 1744-22-5
Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
2 Customer Reviews
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Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (*p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (*p≤0.036). c Swim Speed. Aged rats swam the most slowly (*p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (*p<0.001).
J Neuroimmune Pharmacol, 2013, 8(5):1098-105.. Riluzole (PK 26124) purchased from Selleck.
The effect of intrathecal administration of riluzole on changes of tail flick latency in EA-treated rats (Mean ± SD, %, n = 6). EA was given once per day for eight consecutive days. Riluzole or vehicle was given once daily 30 min prior to EA. The significance of differences was calculated by a one-way ANOVA. EA + V: EA plus vehicle; EA + R20: EA plus 20 μg riluzole; EA + R10: EA plus 10 μg riluzole; EA + R5: EA plus 5 μg riluzole; R20, 20 μg riluzole. The values with different letters (a–d) at the same day differ (p < 0.05).
Int J Mol Sci, 2016, 17(3):357. Riluzole (PK 26124) purchased from Selleck.
Purity & Quality Control
Choose Selective Sodium Channel Inhibitors
Biological Activity
| Description | Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities. | ||||||
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| In vitro |
Riluzole inhibits the release of glutamic acid from cultured neurons, and from brain slices. These effects may be partly due to inactivation of voltage-dependent sodium channels on glutamatergic nerve terminals, as well as activation of a G-protein-dependent signal transduction process. Electrophysiologic experiments performed on isolated excitatory amino acid receptors expressed in the Xenopus oocyte have revealed that Riluzole inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). Riluzole has been shown to stabilize inactivated sodium channels in frog sciatic nerve, in rat cerebellar granule cells, and on recombinant rat sodium channels expressed in Xenopus oocytes (Ki = 0.2 μM). Riluzole also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. Tiluzole protects cultured neurons from anoxic damage, from the toxic effects of glutamic-acid-uptake inhibitors, and from the toxic factor in the CSF of patients with amyotrophic lateral sclerosis. [1] |
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| Assay |
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| In vivo | Riluzole can easily cross the blood-brain barrier. Riluzole has neuroprotective, anticonvulsant, and sedative properties in vivo. In a rodent model of transient global cerebral ischemia, a complete suppression of the ischemia-evoked surge in glutamic acid release has been observed by Riluzole treatment (8 mg/kg i.p.). [1] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 46 mg/mL (196.41 mM) |
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| Water | Insoluble | |
| Ethanol | '46 mg/mL |
* 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 | 234.2 |
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| Formula | C8H5F3N2OS |
| CAS No. | 1744-22-5 |
| Storage |
powder in solvent |
| Synonyms | RP-54274 |
| Smiles | C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N |
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 | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
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 (mg) = Concentration (mM) × Volume (mL) × 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 SDS / 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 SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
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 | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04819438 | Active not recruiting | Drug: Riluzole 50 mg Oral Film|Drug: Rilutek 50Mg Tablet | Bioequivalence | Cross Research S.A.|Zambon SpA | January 15 2021 | Phase 1 |
| NCT02859792 | Unknown status | Drug: Riluzole|Drug: Placebo|Biological: Blood Samples | Spinal Cord Injury | Assistance Publique Hopitaux De Marseille | May 2019 | Phase 2 |
| NCT04630444 | Completed | Drug: Riluzole | Posttraumatic Stress Disorder | Mclean Hospital|Brain & Behavior Research Foundation | March 16 2017 | Early Phase 1 |
| NCT02238626 | Completed | Drug: Placebo (for MN-166)|Drug: MN-166|Drug: riluzole | Amyotrophic Lateral Sclerosis | MediciNova|Atrium Health | September 2014 | Phase 2 |
| NCT01661855 | Completed | Drug: Riluzole|Drug: Placebo | Autism Spectrum Disorders | Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|The Hospital for Sick Children|University of Western Ontario Canada|Unity Health Toronto|University of Toronto|Anagnostou Evdokia M.D. | September 2013 | Phase 2 |
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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