Riluzole

Catalog No.S1614 Batch:S161408

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Technical Data

Formula

C8H5F3N2OS
Molecular Weight 234.2 CAS No. 1744-22-5
Solubility (25°C)* In vitro DMSO 47 mg/mL (200.68 mM)
Ethanol 47 mg/mL (200.68 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
4.0mg/ml 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. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Targets
Sodium channel [1] NMDA receptor [1] Glutamate release [2]
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]
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 (from reference)

Customer Product Validation

Data from [Data independently produced by , , J Neuroimmune Pharmacol, 2013, 8(5):1098-105.]

Data from [Data independently produced by , , Int J Mol Sci, 2016, 17(3):357]

Selleck's Riluzole has been cited by 12 publications

BDNF Augmentation Using Riluzole Reverses Doxorubicin-Induced Decline in Cognitive Function and Neurogenesis [ Neurotherapeutics, 2023, none] PubMed: 36720792
Riluzole Suppresses Growth and Enhances Response to Endocrine Therapy in ER+ Breast Cancer [ J Endocr Soc, 2023, 7(10):bvad117] PubMed: 37766843
Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain [ Front Bioeng Biotechnol, 2022, 10:855755] PubMed: 35372313
Small-Molecule-Driven Direct Reprogramming of Fibroblasts into Functional Sertoli-Like Cells as a Model for Male Reproductive Toxicology [ Adv Biol (Weinh), 2022, e2101184] PubMed: 35212192
Reduction of glutamate neurotoxicity: A novel therapeutic approach for Niemann-Pick disease, type C1 [ Mol Genet Metab, 2021, S1096-7192(21)00826-X] PubMed: 34802899
Concurrent Targeting of Glutaminolysis and Metabotropic Glutamate Receptor 1 (GRM1) Reduces Glutamate Bioavailability in GRM1+ Melanoma [ Cancer Res, 2019, 79(8):1799-1809] PubMed: 30987979
Treatment with the glutamate modulator riluzole prevents early life stress-induced cognitive deficits and impairments in synaptic plasticity in APPswe/PS1dE9 mice [ Neuropharmacology, 2019, 150:175-183] PubMed: 30794835
The new role of riluzole in the treatment of pancreatic cancer through the apoptosis and autophagy pathways [ J Cell Biochem, 2019, 10.1002/jcb.29533] PubMed: 31709624
Targetable Clinical Nanoparticles for Precision Cancer Therapy Based on Disease-Specific Molecular Inflection Points. [ Nano Lett, 2017, 17(11):7160-7168] PubMed: 29035540
Exploiting ROS and metabolic differences to kill cisplatin resistant lung cancer [ Oncotarget, 2017, 8(30):49275-49292] PubMed: 28525376

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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