Riluzole hydrochloride
Based on 16 publication(s) in Google Scholar
Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 850608-87-6
- Formula: C8H6ClF3N2OS
- Molecular Weight:270.66
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Riluzole hydrochloride
More- Cell Res. 2022 Jun;32(6):555-569. [Abstract]
- Nat Biomed Eng. 2026 Apr 24. [Abstract]
- Nat Neurosci. 2025 Nov 24. [Abstract]
- Nat Commun. 2023 Dec 12;14(1):8255. [Abstract]
- Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Oct 10;120(41):e2309773120. [Abstract]
- Free Radic Biol Med. 2024 May 1:217:126-140. [Abstract]
- EMBO Mol Med. 2025 Oct 15. [Abstract]
- J Neurochem. 2025 Oct;169(10):e70246. [Abstract]
- Front Cell Neurosci. 2020 Oct 16;14:575626. [Abstract]
- Front Neural Circuits. 2021 Apr 6:15:657445. [Abstract]
- Pharmacol Biochem Behav. 2018 May:168:43-50. [Abstract]
- Neurosci Lett. 2021 May 14:753:135846. [Abstract]
- bioRxiv. 2026 Apr 30.
- bioRxiv. 2026 Feb 18:2026.02.16.706212. [Abstract]
- Res Sq. 2024 Jul 09.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
Biological Activity
Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM. At 20 μM, Riluzole hydrochloride inhibits peak autaptic IPSCs only slightly but prolongs IPSCs reliably. It is also found that Riluzole hydrochloride causes a strong, concentration-dependent, readily reversible enhancement of responses to 2 μM GABA. At higher concentrations of Riluzole hydrochloride, especially 300 μM, GABA currents exhibit apparent desensitization during prolonged co-exposure to 2 μM GABA and Riluzole hydrochloride. The EC50 of Riluzole hydrochloride potentiation of GABA responses is about 60 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 850608-87-6
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Appearance Solid
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Molecular Weight 270.66
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Formula C8H6ClF3N2OS
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Color White to off-white
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SMILES
NC1=NC2=CC=C(OC(F)(F)F)C=C2S1.Cl
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Synonyms
PK 26124 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (16)
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Journal Impact Factor
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Most Recent
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Cell Res
Gut microbiota drives macrophage-dependent self-renewal of intestinal stem cells via niche enteric serotonergic neurons. [Abstract]2022 Jun;32(6):555-569. PMID: 35379903 -
Nat Biomed Eng
DeepDrugDiscovery identifies blood-brain barrier permeable autophagy enhancers for Alzheimer's disease. [Abstract]2026 Apr 24. PMID: 42032039 -
Nat Neurosci
Large-scale drug screening in iPSC-derived motor neurons from sporadic ALS patients identifies a potential combinatorial therapy. [Abstract]2025 Nov 24. PMID: 41286450
Riluzole hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2025 Nov 24. [Abstract]
Longitudinal quantification of the total neurite length of HB9-tGFP+ motor neurons for a representative SALS donor treated with Riluzole (0-50 μM; 70 days) expressed as a percentage of the pretreatment (day 36) value.
Riluzole hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2025 Nov 24. [Abstract]
Riluzole (0-50 μM; 70 days) resulted in a significant rescue of LD50 survival at 2.5 µM (P = 0.045), 5 µM (P = 0.005) and 10 µM (P = 0.004), with a notable difference in efficacy between SALS donors.
Riluzole hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2025 Nov 24. [Abstract]
Representative live-cell images (day 46) of motor neurons from eight SALS donors (LD50 < 45) treated with 2.5 µM DMSO control (top) or riluzole (bottom).
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Nat Commun
D-serine reconstitutes synaptic and intrinsic inhibitory control of pyramidal neurons in a neurodevelopmental mouse model for schizophrenia. [Abstract]2023 Dec 12;14(1):8255. PMID: 38086803
Riluzole hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Dec 12;14(1):8255. [Abstract]
iluzole (2 μM) decreased spike number of pyramidal neurons in the ACC of MAM group.
Riluzole hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Dec 12;14(1):8255. [Abstract]
Riluzole (8 mg/kg; IP) had no effect on acoustic startle responses, restored the impaired PPI in MAM group, had no effect on locomotor activity in OFTs.
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Adv Sci (Weinh)
Morphine Tolerance Gated through EZH2-Mediated Suppression of Trpc5 in Spinal GABAergic Interneurons in Male Mice. [Abstract]2025 Oct 20:e07908. PMID: 41111460 -
Proc Natl Acad Sci U S A
2023 Oct 10;120(41):e2309773120. PMID: 37782796 -
Free Radic Biol Med
Edaravone counteracts redox and metabolic disruptions in an emerging zebrafish model of sporadic ALS. [Abstract]2024 May 1:217:126-140. PMID: 38531462 -
EMBO Mol Med
Isoginkgetin antagonizes ALS pathologies in its animal and patient iPSC models via PINK1-Parkin-dependent mitophagy. [Abstract]2025 Oct 15. PMID: 41094045 -
J Neurochem
Neuronal Damage Induced by Gradual Oxidative Stress in iPSC-Derived Neurons: Implications for Ferroptosis Involvement and ALS Drug Evaluation. [Abstract]2025 Oct;169(10):e70246. PMID: 41017138 -
Front Cell Neurosci
Three-Week Treadmill Exercise Enhances Persistent Inward Currents, Facilitates Dendritic Plasticity, and Upregulates the Excitability of Dorsal Raphe Serotonin Neurons in ePet-EYFP Mice. [Abstract]2020 Oct 16;14:575626. PMID: 33177992 -
Front Neural Circuits
Serotonergic Modulation of Persistent Inward Currents in Serotonergic Neurons of Medulla in ePet-EYFP Mice. [Abstract]2021 Apr 6:15:657445. PMID: 33889077 -
Pharmacol Biochem Behav
Anticonvulsants lamotrigine and riluzole disrupt maternal behavior in postpartum female rats. [Abstract]2018 May:168:43-50. PMID: 29572014 -
Neurosci Lett
Persistent sodium conductance contributes to orexin-A-mediated modulation of membrane excitability in neonatal rat mesencephalic V neurons. [Abstract]2021 May 14:753:135846. PMID: 33774148 -
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bioRxiv
Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]2026 Feb 18:2026.02.16.706212. PMID: 41757027 -
Solvent & Solubility
DMSO : 100 mg/mL (369.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4.17 mg/mL (15.41 mM; Need ultrasonic)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
Two-electrode voltage clamp of Xenopus oocytes expressing exogenous GABAA receptors is performed with a CA-1B high performance oocyte clamp. The extracellular recording solution is ND-96 medium. Riluzole hydrochloride is applied from a common tip via a gravity-driven multibarrel drug-delivery system. Data acquisition and analysis are performed with pCLAMP 6 software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Adult male Sprague-Dawley rats (180 to 350 g) are housed in a temperature-controlled room and maintained on a 12-h day/night cycle with unrestricted access to food and water. Pain behaviors are measured before and 5 h after induction of a mono-arthritis in the left knee joint. To test the effects of systemic (intraperitoneal, i.p.) application of Riluzole hydrochloride, pain behaviors are measured 1 h postinjection of Riluzole hydrochloride in normal and arthritic animals. To determine effects of Riluzole hydrochloride into the amygdala, pain behaviors are measured 15 min after starting Riluzole hydrochloride application through a stereotaxically implanted microdialysis probe. To investigate site of action in the amygdala of systemically applied Riluzole hydrochloride, potassium channel blockers are administered into the amygdala 45 min after systemic application of Riluzole hydrochloride and pain behaviors are measured 15 min later, i.e., 1 h postinjection of riluzole (i.p.)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. He Y, et al. Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function. Neuropharmacology. 2002 Feb;42(2):199-209. [Content Brief]
[2]. Thompson JM, et al. Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. Mol Pain. 2015 Aug 28;11:51. [Content Brief]
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.6947 mL | 18.4734 mL | 36.9467 mL | 92.3668 mL |
| 5 mM | 0.7389 mL | 3.6947 mL | 7.3893 mL | 18.4734 mL | |
| 10 mM | 0.3695 mL | 1.8473 mL | 3.6947 mL | 9.2367 mL | |
| 15 mM | 0.2463 mL | 1.2316 mL | 2.4631 mL | 6.1578 mL | |
| DMSO | 20 mM | 0.1847 mL | 0.9237 mL | 1.8473 mL | 4.6183 mL |
| 25 mM | 0.1478 mL | 0.7389 mL | 1.4779 mL | 3.6947 mL | |
| 30 mM | 0.1232 mL | 0.6158 mL | 1.2316 mL | 3.0789 mL | |
| 40 mM | 0.0924 mL | 0.4618 mL | 0.9237 mL | 2.3092 mL | |
| 50 mM | 0.0739 mL | 0.3695 mL | 0.7389 mL | 1.8473 mL | |
| 60 mM | 0.0616 mL | 0.3079 mL | 0.6158 mL | 1.5394 mL | |
| 80 mM | 0.0462 mL | 0.2309 mL | 0.4618 mL | 1.1546 mL | |
| 100 mM | 0.0369 mL | 0.1847 mL | 0.3695 mL | 0.9237 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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