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> Riluzole [1744-22-5]

Riluzole [1744-22-5]

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Referencia HY-B0211-1g

embalaje : 1g

Marca : MedChemExpress

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Descripciòn

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.

Riluzole Related Antibodies
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.
Ensayo clínico
Peso molecular

234.20

Fòrmula

C8H5F3N2OS
No. CAS
Appearance

Solid

Color

White to yellow

SMILES

NC1=NC2=CC=C(OC(F)(F)F)C=C2S1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
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
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.
Pureza y Documentación
Referencias

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Referencia
Descripción
Cond.
Precio Sin IVA
HY-B0211-500mg
Riluzole [1744-22-5]
 500mg