您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Riluzole(RP-54274,PK 26124)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Riluzole(RP-54274,PK 26124)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Riluzole(RP-54274,PK 26124)图片
CAS NO:1744-22-5
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)234.2
FormulaC8H5F3N2OS
CAS No.1744-22-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 47 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: 47 mg/mL (200.7 mM)
Other info

Chemical Name: 6-(trifluoromethoxy)-1,3-benzothiazol-2-amine

InChi Key: FTALBRSUTCGOEG-UHFFFAOYSA-N

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)

SMILES: NC1=NC2=CC=C(OC(F)(F)F)C=C2S1

SynonymsPK 26124, RP 54274, PK26124, RP54274, RP-54274, PK-26124; Rilutek
实验参考方法
In Vitro

In vitro activity: 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.


Cell Assay: In HEKGLT1, HEKGLAST or HEKEAAC1 cells, riluzole increased Na+-dependent uptake in a dose-dependent manner, with significant effects at concentrations as low as 0.01–0.1 μM and the highest effect at 100 μM. The increase in glutamate uptake induced by 100 μM riluzole was similar in all cell lines (+27% in HEKGLAST, +38% in HEKGLT1, +39% in HEKEAAC1). Higher riluzole concentrations (300 and 1000 μM) were toxic, since at the end of experiments the majority of cells were floating, and specific and non-specific glutamate uptake were reduced by more than 50%.

In VivoRiluzole 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.).
Animal modelRodent model of transient global cerebral ischemia
Formulation & Dosage8 mg/kg i.p.
References

Neurology. 1996 Dec;47(6 Suppl 4):S233-41; Naunyn-Schmiedeberg's Archives of Pharmacology