Riluzole [1744-22-5]
Référence HY-B0211-500mg
Conditionnement : 500mg
Marque : MedChemExpress
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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Riluzole Chemical Structure
CAS No. : 1744-22-5
This product is a controlled substance and not for sale in your territory.
Based on 9 publication(s) in Google Scholar
Other Forms of Riluzole:
- Riluzole hydrochloride In-stock
- Riluzole-13C,15N2 Obtenir un devis
Voir tous les produits spécifiques à Isoform Sodium Channel:
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] |
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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. |
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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. |
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Essai clinique |
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Masse moléculaire |
234.20 |
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Formule |
C8H5F3N2OS |
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CAS No. |
1744-22-5 |
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Appearance |
Solid |
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Color |
White to yellow |
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SMILES |
NC1=NC2=CC=C(OC(F)(F)F)C=C2S1 |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
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Solvant et solubilité |
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
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. * 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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Pureté et documentation | |||||||||||||
Références |
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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.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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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.
Riluzole Related Classifications
- Membrane Transporter/Ion Channel Neuronal Signaling
- Sodium Channel GABA Receptor