Reagents and instruments for immunology, cell biology and molecular biology.

Riluzole [1744-22-5]

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Cat# HY-B0211-1g

Size : 1g

Brand : MedChemExpress

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Description

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]

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-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]
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]
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]

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

Molecular Weight

234.20

Formula

C₈H₅F₃N₂OS

CAS No.

1744-22-5

Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 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.

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.

Purity & Documentation

Purity: 99.80%

Data Sheet (277 KB) SDS (479 KB)

COA (245 KB) HNMR (127 KB) LCMS (136 KB)

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]

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