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Riluzole

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纯度: 99.88%

货号 T0349Cas号 1744-22-5

别名 利鲁唑, RP-54274, PK 26124

Riluzole (RP-54274) 是一种谷氨酸拮抗剂,用作抗惊厥药并延长肌萎缩侧索硬化症患者的生存期。它还抑制 GABA 摄取,IC50值为 43 μM。

Riluzole
其他形式的 “Riluzole”:

Riluzole

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Rating icon 很棒

纯度: 99.88%

货号 T0349 别名 利鲁唑, RP-54274, PK 26124Cas号 1744-22-5

Riluzole (RP-54274) 是一种谷氨酸拮抗剂,用作抗惊厥药并延长肌萎缩侧索硬化症患者的生存期。它还抑制 GABA 摄取,IC50值为 43 μM。

规格价格库存数量
5 mg
¥ 165
现货
10 mg
¥ 223
现货
25 mg
¥ 346
现货
50 mg
¥ 493
现货
100 mg
¥ 797
现货
500 mg
¥ 2,380
现货
1 mL x 10 mM (in DMSO)
¥ 257
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产品介绍


Riluzole AI Summary
Riluzole exhibits a diverse range of bioactivities, indicating potential therapeutic applications across multiple domains. It functions as a sodium channel blocker with an IC50 of 4730 nM and a voltage-gated Ca2+ channel blocker in rat brain synaptosomes with an IC50 of 0.0 nM, showing potent inhibition of K+-evoked and veratridine-induced glutamate release. Additionally, Riluzole protects against seizures and has neuroprotective activity, demonstrated by efficacy in rat models of glutamate-induced convulsions (ED50 of 3.2 mg/kg) and focal stroke (effective at 4.0 mg/kg and 30.0 mg/kg). The compound shows considerable metabolic stability, liver enzyme modulation, and potential for therapeutic applications in neuroprotection and stroke. It has a partition coefficient (logD7.4) of 3.43, high plasma protein binding of 97.13%, and demonstrates moderate lipophilicity (LogP 3.2). Additionally, it interferes with various cellular processes, including mitochondrial function, NFkB signaling, and Lamin A splicing, and inhibits several enzymes like BSEP (IC50 139000 nM) and human UGT1A1. In terms of antibacterial and antifungal activity, Riluzole shows efficacy against Escherichia coli, Enterococcus faecalis, Staphylococcus aureus, and several Candida species. It also demonstrates antivirals by inhibiting SARS-CoV-2 3CL-Pro protease and virus-induced cytotoxicity in VERO-6 cells. Moreover, Riluzole has cytotoxic effects in some cell lines but displays neuroprotective properties against excitotoxic and oxidative stress in neuronal cells. Its high aqueous solubility, moderate passive permeability, and good liver microsomal stability underscore its potential as a drug candidate. Overall, Riluzole’s broad bioactivity profile underscores its potential for therapeutic development in treating neurological disorders, infectious diseases, and metabolic conditions..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Riluzole (RP-54274) is a glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
靶点活性
GABA:43 μM
体外活性

Tiluzole保护培养的神经元免受缺氧损伤,减少肌萎缩性侧索硬化患者CSF中毒性因子的损伤。Riluzole在非洲爪蟾卵母细胞中表达的离体兴奋性氨基酸受体的电生理学试验中抑制N-甲基-D-天冬氨酸(IC50 = 18 μM)和红藻氨酸(IC50 = 167 μM)诱发的电流。Riluzole能够稳定蛙坐骨神经和大鼠小脑颗粒细胞中激活的钠离子通道。Riluzole抑制谷氨基酸从培养的神经元和脑片释放。Riluzole通过非竞争性N-甲基-D-天冬氨酸受体也会阻断一些谷氨酸的突触后作用。

体内活性

Riluzole能够轻易穿过血脑屏障.用8 mg/kg i.p. Riluzole治疗短暂性脑缺血的啮齿动物,可以完全抑制局部缺血诱发的谷氨基酸大量释放.

别名利鲁唑, RP-54274, PK 26124
化学信息
分子量234.2
分子式C8H5F3N2OS
CAS No.1744-22-5
SmilesNC1=NC2=C(S1)C=C(OC(F)(F)F)C=C2
密度1.572 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 240 mg/mL (1024.77 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 43 mg/mL (183.6 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (21.35 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM4.2699 mL21.3493 mL42.6985 mL213.4927 mL
5 mM0.8540 mL4.2699 mL8.5397 mL42.6985 mL
10 mM0.4270 mL2.1349 mL4.2699 mL21.3493 mL
20 mM0.2135 mL1.0675 mL2.1349 mL10.6746 mL
50 mM0.0854 mL0.4270 mL0.8540 mL4.2699 mL
100 mM0.0427 mL0.2135 mL0.4270 mL2.1349 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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