受注:045-509-1970 |
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Synonyms | RP-54274, PK 26124 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C8H5F3N2OS |
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分子量 | 234.2 | CAS No. | 1744-22-5 | |
Solubility (25°C)* | 体外 | DMSO | 47 mg/mL (200.68 mM) | |
Ethanol | 47 mg/mL (200.68 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities. |
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in vitro | Riluzole inhibits the release of glutamic acid from cultured neurons, and from brain slices. These effects may be partly due to inactivation of voltage-dependent sodium channels on glutamatergic nerve terminals, as well as activation of a G-protein-dependent signal transduction process. Electrophysiologic experiments performed on isolated excitatory amino acid receptors expressed in the Xenopus oocyte have revealed that Riluzole inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). Riluzole has been shown to stabilize inactivated sodium channels in frog sciatic nerve, in rat cerebellar granule cells, and on recombinant rat sodium channels expressed in Xenopus oocytes (Ki = 0.2 μM). Riluzole also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. Tiluzole protects cultured neurons from anoxic damage, from the toxic effects of glutamic-acid-uptake inhibitors, and from the toxic factor in the CSF of patients with amyotrophic lateral sclerosis. [1] |
in vivo | Riluzole can easily cross the blood-brain barrier. Riluzole has neuroprotective, anticonvulsant, and sedative properties in vivo. In a rodent model of transient global cerebral ischemia, a complete suppression of the ischemia-evoked surge in glutamic acid release has been observed by Riluzole treatment (8 mg/kg i.p.). [1] |
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Data from [Data independently produced by , , J Neuroimmune Pharmacol, 2013, 8(5):1098-105.]
Data from [Data independently produced by , , Int J Mol Sci, 2016, 17(3):357]
BDNF Augmentation Using Riluzole Reverses Doxorubicin-Induced Decline in Cognitive Function and Neurogenesis [ Neurotherapeutics, 2023, none] | PubMed: 36720792 |
Riluzole Suppresses Growth and Enhances Response to Endocrine Therapy in ER+ Breast Cancer [ J Endocr Soc, 2023, 7(10):bvad117] | PubMed: 37766843 |
Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain [ Front Bioeng Biotechnol, 2022, 10:855755] | PubMed: 35372313 |
Small-Molecule-Driven Direct Reprogramming of Fibroblasts into Functional Sertoli-Like Cells as a Model for Male Reproductive Toxicology [ Adv Biol (Weinh), 2022, e2101184] | PubMed: 35212192 |
Reduction of glutamate neurotoxicity: A novel therapeutic approach for Niemann-Pick disease, type C1 [ Mol Genet Metab, 2021, S1096-7192(21)00826-X] | PubMed: 34802899 |
Concurrent Targeting of Glutaminolysis and Metabotropic Glutamate Receptor 1 (GRM1) Reduces Glutamate Bioavailability in GRM1+ Melanoma [ Cancer Res, 2019, 79(8):1799-1809] | PubMed: 30987979 |
Treatment with the glutamate modulator riluzole prevents early life stress-induced cognitive deficits and impairments in synaptic plasticity in APPswe/PS1dE9 mice [ Neuropharmacology, 2019, 150:175-183] | PubMed: 30794835 |
The new role of riluzole in the treatment of pancreatic cancer through the apoptosis and autophagy pathways [ J Cell Biochem, 2019, 10.1002/jcb.29533] | PubMed: 31709624 |
Targetable Clinical Nanoparticles for Precision Cancer Therapy Based on Disease-Specific Molecular Inflection Points. [ Nano Lett, 2017, 17(11):7160-7168] | PubMed: 29035540 |
Exploiting ROS and metabolic differences to kill cisplatin resistant lung cancer [ Oncotarget, 2017, 8(30):49275-49292] | PubMed: 28525376 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。