Name: Riluzole
Brand: Selleck Chemicals
SKU: S1614
Availability: InStock
Rating: 5 (13 reviews)

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Quality Control

Batch: Purity: 99.88%

99.88

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Sodium Channel Inhibitors	Camostat Mesilate A-803467 cariporide Veratramine Tolperisone HCl Bulleyaconi cine A Vinpocetine Tenapanor PF-06869206 Sparteine

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (200.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (17.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.

Chemical Information, Storage & Stability

Molecular Weight	234.2	Formula	C₈H₅F₃N₂OS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1744-22-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RP-54274, PK 26124			Smiles	C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N

Mechanism of Action

Targets/IC₅₀/Ki	Sodium channel NMDA receptor Glutamate release
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 this compound inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). It 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 (K_i = 0.2 μM). This chemical also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. It 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.
In vivo	Riluzole can easily cross the blood-brain barrier. This compound 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 this chemical treatment (8 mg/kg i.p.).
References	[1] https://pubmed.ncbi.nlm.nih.gov/8959995/ [2] http://link.springer.com/article/10.1007%2FPL00005241

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-AKT / AKT p-Smad2 / Smad2 / p-Smad3 / Smad3		23077590

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06270108	Recruiting	Treatment-resistant Schizophrenia\|Treatment-responsive Schizophrenia\|Healthy Controls	King''s College London\|South London and Maudsley NHS Foundation Trust	November 14 2022	Early Phase 1
NCT05292209	Recruiting	Atrial Fibrillation Paroxysmal	University of Utah\|Ohio State University	June 15 2022	Phase 2
NCT04819438	Completed	Bioequivalence	Cross Research S.A.\|Zambon SpA	January 15 2021	Phase 1
NCT02859792	Recruiting	Spinal Cord Injury	Assistance Publique Hopitaux De Marseille	May 27 2019	Phase 2
NCT04630444	Completed	Posttraumatic Stress Disorder	Mclean Hospital\|Brain & Behavior Research Foundation	March 16 2017	Early Phase 1

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Handling Instructions

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Riluzole Sodium Channel inhibitor

Chemical Structure

Molecular Weight: 234.2