Riluzole
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.75%
- No. CAS: 1744-22-5
- Fòrmula: C8H5F3N2OS
- Peso molecular:234.20
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Riluzole
More- Cell Res. 2022 Jun;32(6):555-569. [Abstract]
- Nat Biomed Eng. 2026 Apr 24. [Abstract]
- Nat Neurosci. 2025 Nov 24. [Abstract]
- Nat Commun. 2023 Dec 12;14(1):8255. [Abstract]
- Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Oct 10;120(41):e2309773120. [Abstract]
- Free Radic Biol Med. 2024 May 1:217:126-140. [Abstract]
- EMBO Mol Med. 2025 Oct 15. [Abstract]
- J Neurochem. 2025 Oct;169(10):e70246. [Abstract]
- Front Cell Neurosci. 2020 Oct 16:14:575626. [Abstract]
- Front Neural Circuits. 2021 Apr 6:15:657445. [Abstract]
- Pharmacol Biochem Behav. 2018 May:168:43-50. [Abstract]
- Neurosci Lett. 2021 May 14:753:135846. [Abstract]
- bioRxiv. 2026 Apr 30.
- bioRxiv. 2026 Feb 18:2026.02.16.706212. [Abstract]
- Res Sq. 2024 Jul 09.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | IC50 |
>25 μM
Compound: 1b
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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
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[PMID: 30908048] |
| A549 | GI50 |
10 μM
Compound: 1b
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Cytotoxicity against human A549 cells after 48 hrs by Celltiter-glo assay
Cytotoxicity against human A549 cells after 48 hrs by Celltiter-glo assay
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[PMID: 30908048] |
| CHO | IC50 |
2.2 μM
Compound: 2 (PK-26124)
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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
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10.1016/0960-894X(95)00392-7 |
| CHO-K1 | IC50 |
310 μM
Compound: Riluzole
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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
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[PMID: 27287370] |
| CHO-K1 | IC50 |
480 μM
Compound: Riluzole
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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
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[PMID: 27287370] |
| COS-7 | EC50 |
139.4 μM
Compound: 1
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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
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[PMID: 26588045] |
| HEK293 | IC50 |
160 μM
Compound: Riluzole
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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
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[PMID: 21030469] |
| HEK293 | IC50 |
180 μM
Compound: Riluzole
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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
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[PMID: 21030469] |
| HEL | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| KG-1 | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| MCF7 | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| MDA-MB-231 | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| MOLT-4 | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| MRC5 | ED50 |
27.88 μg/mL
Compound: 5c
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Cytotoxicity against human MRC5 cells after 72 hrs by Alamar blue assay
Cytotoxicity against human MRC5 cells after 72 hrs by Alamar blue assay
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[PMID: 21126022] |
| PC-3 | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| SK-N-BE(2) | IC50 |
>10 μM
Compound: Riluzole
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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
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[PMID: 37875056] |
| U2OS | GI50 |
>25 μM
Compound: 1b
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Cytotoxicity against human U2OS cells assessed as reduction in cell number
Cytotoxicity against human U2OS cells assessed as reduction in cell number
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[PMID: 30908048] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1744-22-5
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Appearance Solid
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Peso molecular 234.20
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Fòrmula C8H5F3N2OS
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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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Synonyms
PK 26124
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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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).
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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.
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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
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 -
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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 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 |
|---|---|---|---|---|---|
| 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
HY-B0211 Related Classifications
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