Art. -Nr.: HY-B0211

Riluzole

(Synonyms: PK 26124)

16 Cited Publications

Kundenbewertung

Based on 16 publication(s) in Google Scholar

Riluzole 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.

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Reinheit: 99.75%
CAS. Nr.: 1744-22-5
Formel: C₈H₅F₃N₂OS
Molecular Weight:234.20

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Riluzole Chemical Structure

CAS. Nr.: 1744-22-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Riluzole 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.

IC₅₀ & Target

Sodium channel^[1]
IC50: 43 μM (GABA receptor)^[1]

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	>25 μM Compound: 1b	Mitochondrial toxicity in human 786-O cells measured after 6 hrs by MitoTracker Red chloromethyl-X-rosamine based assay Mitochondrial toxicity in human 786-O cells measured after 6 hrs by MitoTracker Red chloromethyl-X-rosamine based assay	[PMID: 30908048]
A549	GI₅₀	10 μM Compound: 1b	Cytotoxicity against human A549 cells after 48 hrs by Celltiter-glo assay Cytotoxicity against human A549 cells after 48 hrs by Celltiter-glo assay	[PMID: 30908048]
CHO	IC₅₀	2.2 μM Compound: 2 (PK-26124)	Blockade of synaptosomal sodium channels, inhibition of [14C]guanidinium ion flux into CHO cells expressing Type II sodium channel Blockade of synaptosomal sodium channels, inhibition of [14C]guanidinium ion flux into CHO cells expressing Type II sodium channel	10.1016/0960-894X(95)00392-7
CHO-K1	IC₅₀	310 μM Compound: Riluzole	Cytotoxicity against CHOK1 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against CHOK1 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 27287370]
CHO-K1	IC₅₀	480 μM Compound: Riluzole	Cytotoxicity against CHOK1 cells assessed as reduction in cell viability after 24 hrs by LDH assay Cytotoxicity against CHOK1 cells assessed as reduction in cell viability after 24 hrs by LDH assay	[PMID: 27287370]
COS-7	EC₅₀	139.4 μM Compound: 1	Activation of TREK1 (unknown origin) expressed in COS7 cells assessed as increase in whole cell currents at +50 mV relative to control Activation of TREK1 (unknown origin) expressed in COS7 cells assessed as increase in whole cell currents at +50 mV relative to control	[PMID: 26588045]
HEK293	IC₅₀	160 μM Compound: Riluzole	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	180 μM Compound: Riluzole	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEL	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human HEL cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HEL cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
KG-1	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
MCF7	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
MDA-MB-231	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
MOLT-4	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
MRC5	ED₅₀	27.88 μg/mL Compound: 5c	Cytotoxicity against human MRC5 cells after 72 hrs by Alamar blue assay Cytotoxicity against human MRC5 cells after 72 hrs by Alamar blue assay	[PMID: 21126022]
PC-3	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
SK-N-BE(2)	IC₅₀	>10 μM Compound: Riluzole	Antiproliferative activity against human SK-N-BE(2) cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-N-BE(2) cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37875056]
U2OS	GI₅₀	>25 μM Compound: 1b	Cytotoxicity against human U2OS cells assessed as reduction in cell number Cytotoxicity against human U2OS cells assessed as reduction in cell number	[PMID: 30908048]

In Vitro

Riluzole 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 inhibits peak autaptic IPSCs only slightly but prolongs IPSCs reliably. It is also found that Riluzole causes a strong, concentration-dependent, readily reversible enhancement of responses to 2 μM GABA. At higher concentrations of Riluzole, especially 300 μM, GABA currents exhibit apparent desensitization during prolonged co-exposure to 2 μM GABA and Riluzole. The EC₅₀ of Riluzole 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.

In Vivo

In normal na ve rats, systemic injection of Riluzole (8 mg/kg, i.p.; n=6 rats) decreases the duration of ultrasonic but not audible vocalizations evoked by noxious stimulation of the knee joint compare to vehicle tested in the same rats (P<0.05). Systemic application of Riluzole (8 mg/kg, i.p.; n=19 rats) decreases the vocalizations of arthritic rats compare to predrug and vehicle significantly (P<0.05 to 0.001). Riluzole administered into the CeA significantly decreases the duration of audible and ultrasonic vocalizations evoked by noxious stimulation of the knee compare to predrug values (n=8 rats; P<0.05 to 0.01)^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1744-22-5
Appearance Solid
Molecular Weight 234.20
Formel C₈H₅F₃N₂OS
Color White to yellow
SMILES

NC1=NC2=CC=C(OC(F)(F)F)C=C2S1
Synonyms

PK 26124
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (16)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

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 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 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 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).
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 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 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.
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

Dual-pocket inhibition of Nav channels by the antiepileptic drug lamotrigine. [Abstract]

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
bioRxiv

2026 Apr 30.
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
Res Sq

2024 Jul 09.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (426.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (4.27 mM; ultrasonic and adjust pH to 3 with HCl)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.2699 mL

21.3493 mL

42.6985 mL

5 mM

0.8540 mL

4.2699 mL

8.5397 mL

10 mM

0.4270 mL

2.1349 mL

4.2699 mL

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.

* 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (10.67 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (10.67 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (10.67 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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 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.

Animal Administration^[2]

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, pain behaviors are measured 1 h postinjection of Riluzole in normal and arthritic animals. To determine effects of Riluzole into the amygdala, pain behaviors are measured 15 min after starting Riluzole application through a stereotaxically implanted microdialysis probe. To investigate site of action in the amygdala of systemically applied Riluzole, potassium channel blockers are administered into the amygdala 45 min after systemic application of Riluzole 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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
H₂O / DMSO	1 mM	4.2699 mL	21.3493 mL	42.6985 mL	106.7464 mL
DMSO	5 mM	0.8540 mL	4.2699 mL	8.5397 mL	21.3493 mL
	10 mM	0.4270 mL	2.1349 mL	4.2699 mL	10.6746 mL
	15 mM	0.2847 mL	1.4233 mL	2.8466 mL	7.1164 mL
	20 mM	0.2135 mL	1.0675 mL	2.1349 mL	5.3373 mL
	25 mM	0.1708 mL	0.8540 mL	1.7079 mL	4.2699 mL
	30 mM	0.1423 mL	0.7116 mL	1.4233 mL	3.5582 mL
	40 mM	0.1067 mL	0.5337 mL	1.0675 mL	2.6687 mL
	50 mM	0.0854 mL	0.4270 mL	0.8540 mL	2.1349 mL
	60 mM	0.0712 mL	0.3558 mL	0.7116 mL	1.7791 mL
	80 mM	0.0534 mL	0.2669 mL	0.5337 mL	1.3343 mL
	100 mM	0.0427 mL	0.2135 mL	0.4270 mL	1.0675 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.

Keywords

Riluzole

16 Cited Publications

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Riluzole

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Publications Citing Use of MedChemExpress (MCE) Riluzole

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Riluzole Related Classifications

HY-B0211 Related Classifications