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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Riluzole (formerly PK26124, RP54274, RP-54274, PK-26124; Rilutek), an anticonvulsant of the Na+ channel blocker class, is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic activities. Riluzole has been approved as a medication to treat amyotrophic lateral sclerosis. Riluzole acts by complex mechanism involving inhibition of voltage-dependent Na channels, high-voltage activated Ca and K channels, and inhibition of protein kinase C. It was suggested that this mechanism was involved in antioxidative processes.
| ln Vitro |
Riluzole is an anticonvulsant that is a member of the use-dependent Na+ channel blocker family. It has an IC50 of 43 μM and inhibits GABA uptake as well. Riluzole consistently prolongs IPSCs at 20 μM, but it only slightly inhibits peak self-exposure to IPSCs. Furthermore, a significant, concentration-dependent, and easily reversible enhancement of the response to 2 μM GABA was observed with riluzole. After a prolonged co-exposure to 2 μM GABA and Riluzole at higher concentrations, particularly 300 μM, GABA currents demonstrated a notable desensitization. Riluzole has an EC50 of about 60 μM for increasing GABA response[1].
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| ln Vivo |
In comparison to the vehicle tested in the same rats, systemic injection of Riluzole (8 mg/kg, i.p.; n = 6 rats) decreased the duration of ultrasound caused by painful stimulation of the knee joint. but did not lessen vocalizations that could be heard (P < 0.05). When compared to predose and vehicle, systemic administration of Riluzole (8 mg/kg, ip; n=19 rats) dramatically decreased vocalizations in arthritic rats (P<0.05 to 0.001). When compared to predose values, the length of audible and ultrasonic vocalizations elicited by painful stimulation of the knee was considerably reduced by administering Riluzole into the CeA (n = 8 rats; P < 0.05 to 0.01) [2].
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| References |
[1]. He Y, et al. Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function. Neuropharmacology. 2002 Feb;42(2):199-209.
[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 |
| Molecular Formula |
C8H5F3N2OS
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| Molecular Weight |
234.2
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| CAS # |
1744-22-5
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| Related CAS # |
Riluzole hydrochloride;850608-87-6;Riluzole-13C,15N2;1215552-03-6
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| SMILES |
S1C(N([H])[H])=NC2C([H])=C([H])C(=C([H])C1=2)OC(F)(F)F
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| InChi Key |
FTALBRSUTCGOEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)
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| Chemical Name |
6-(trifluoromethoxy)-1,3-benzothiazol-2-amine
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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