- Riluzole
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2026-03-25
- CAS:1744-22-5
- Min. Order:
- Purity: 0.99
- Supply Ability:
- Riluzole
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- $0.00 / 1KG
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2026-03-25
- CAS:1744-22-5
- Min. Order: 1KG
- Purity: 98.0%
- Supply Ability: 5kg/month
- Riluzole
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- $45.00 / 50mg
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2026-03-13
- CAS:1744-22-5
- Min. Order:
- Purity: 99.71%
- Supply Ability: 10g
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| | Riluzole Chemical Properties |
| Melting point | 116-118°C | | Boiling point | 296.3±50.0 °C(Predicted) | | density | 1.572±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: ≥25 mg/mL | | pka | 2.96±0.10(Predicted) | | form | solid | | color | white | | Merck | 14,8223 | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months. | | InChI | 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) | | InChIKey | FTALBRSUTCGOEG-UHFFFAOYSA-N | | SMILES | S1C2=CC(OC(F)(F)F)=CC=C2N=C1N |
| Hazard Codes | T,Xi | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1/PG 3 | | WGK Germany | 3 | | RTECS | DL2830000 | | Hazard Note | Irritant | | HazardClass | 6.1 | | PackingGroup | II | | HS Code | 29342000 | | Storage Class | 6.1A - Combustible acute toxic Cat. 1 and 2 very toxic hazardous materials | | Hazard Classifications | Acute Tox. 2 Oral | | Toxicity | LD50 in mice (mg/kg): 46 i.p.; 67 orally (Mizoule) |
| | Riluzole Usage And Synthesis |
| Description | Riluzole belongs to the derivative of benzothiazole with neuroprotective, potential anti-depressant and anxiolytic activities, which is used in the treatment of a certain type of nerve disease called amyotrophic lateral sclerosis (ALS, also known as Lou Gehrig's disease). It is effective to delay the onset of ventilator-dependence or tracheostomy in selected patients, slow down the deterioration of this disease and probably prolong survival by approximately two to three months. Besides, studies have proved that riluzole has anti-depressant activity for refractory depression and serves as an anxiolytic in the treatment of obsessive-compulsive disorder and generalized anxiety disorder.
However, riluzole does not cure the ALS and reverse nerve damage or muscle weakness. It is believed to function as an inhibitor of a natural substance called glutamate. It helps protect the nerves in the brain and spinal cord from too much of glutamate which may contribute to the nerve damage. Riluzole is available in both tablet and liquid form. The liquid formulation may be more suitable for patients with swallowing difficulties.
| | References | https://en.wikipedia.org/wiki/Riluzole
http://www.medicinenet.com/riluzole_oral_tablets/article.htm
https://pubchem.ncbi.nlm.nih.gov/compound/5070#section=Top
| | Description | Rilutek was launched in Germany, the UK and US (orphan drug status) for
treatment of amyotrophic lateral sclerosis (ALS) and is the first drug approved for this
indication. A one step synthesis from 4-(trifluoromethoxy)aniline provides a supply of
the compound. The source of its neuroprotective and anticonvulsant activity is not
clearly understood. It antagonizes excitatory amino acids and blocks presynaptic
release of glutamate, is an antagonist of NMDA-induced acetylcholine release and
inhibited glutamate and quisqualate induced increases in cGMP but does not bind to
NMDA or Kainic receptors. Rilutek has no affinity for glutamate, GABAbenzodiazepine,
glycine and adenosine receptors. It easily crosses the blood brain
barrier and depresses glutamatergic neurotransmission, stabilizes voltagedependent
Na channels in their inactive form and activates G-protein dependent processes. | | Chemical Properties | White Crystalline Solid | | Originator | Rhone-Poulenc Rorer (France) | | Uses | A neuroprotective agent. Modulates glutamatergic transmission. A glutamate release inhibitor. An anticonvulsant. | | Uses | anticonvulsant, glutamate release inhibitor, anti-ALS | | Uses | Labeled Riluzole, intended for use as an internal standard for the quantification of Riluzole by GC- or LC-mass spectrometry. | | Uses | A neuroprotective agent. A glutamate release inhibitor. An anticonvulsant | | Definition | ChEBI: Riluzole is a member of benzothiazoles. | | Brand name | Rilutek (Sanofi Aventis). | | Biological Activity | Novel psychotropic agent with anticonvulsant, hypnotic, anxiolytic, anti-ischemic and anesthetic properties. Riluzole is able to act as a glutamate release inhibitor, blocks voltage-dependent Na + channels and inhibits GABA uptake by striatal synaptosomes. | | Biochem/physiol Actions | Glutamate release inhibitor; anticonvulsant | | storage | Room temperature | | References | [1] BELLINGHAM M C. A Review of the Neural Mechanisms of Action and Clinical Efficiency of Riluzole in Treating Amyotrophic Lateral Sclerosis: What have we Learned in the Last Decade[J]. CNS Neuroscience & Therapeutics, 2011, 17 1: 4-31. DOI:10.1111/j.1755-5949.2009.00116.x [2] ANDREA URBANI Ottorino B. Riluzole inhibits the persistent sodium current in mammalian CNS neurons[J]. European Journal of Neuroscience, 2001, 12 10: 3567-3574. DOI:10.1046/j.1460-9568.2000.00242.x [3] MARCOS EMÍLIO DOS SANTOS FRIZZO. Riluzole enhances glutamate uptake in rat astrocyte cultures.[J]. Cellular and Molecular Neurobiology, 2004, 24 1: 123-128. DOI:10.1023/b:cemn.0000012717.37839.07 [4] DOBLE A. The pharmacology and mechanism of action of riluzole.[J]. Neurology, 1996, 47 6 Suppl 4: S233-41. DOI:10.1212/wnl.47.6\_suppl\_4.233s [5] CHRISTOPHER PITTENGER. Riluzole in the treatment of mood and anxiety disorders.[J]. CNS drugs, 2008, 22 9: 761-786. DOI:10.2165/00023210-200822090-00004 [6] JIN NAMKOONG. Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma.[J]. Cancer research, 2007, 67 5: 2298-2305. DOI:10.1158/0008-5472.can-06-3665 [7] CHI ZHANG. Anti-cancer effect of metabotropic glutamate receptor 1 inhibition in human glioma U87 cells: involvement of PI3K/Akt/mTOR pathway.[J]. Cellular Physiology and Biochemistry, 2015: 419-432. DOI:10.1159/000369707 [8] SWETLANA SPERLING. Riluzole: a potential therapeutic intervention in human brain tumor stem-like cells.[J]. Oncotarget, 2017: 96697-96709. DOI:10.18632/oncotarget.18043 |
| | Riluzole Preparation Products And Raw materials |
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