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Felbamate

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纯度: 99%

货号 T1946Cas号 25451-15-4

别名 非尔氨酯, 非巴马特, W-554, ADD-03055

Felbamate (W-554) 是非镇静性抗痉挛剂,可通过降低中枢神经系统紊乱的电活动起作用。

Felbamate
其他形式的 “Felbamate”:

Felbamate

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Rating icon 很棒

纯度: 99%

货号 T1946 别名 非尔氨酯, 非巴马特, W-554, ADD-03055Cas号 25451-15-4

Felbamate (W-554) 是非镇静性抗痉挛剂,可通过降低中枢神经系统紊乱的电活动起作用。

规格价格库存数量
5 mg
¥ 298
现货
10 mg
¥ 477
现货
25 mg
¥ 871
现货
50 mg
¥ 1,536
待询
100 mg
¥ 2,294
待询
1 mL x 10 mM (in DMSO)
¥ 330
现货
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产品介绍


Felbamate AI Summary
Felbamate demonstrates notable anticonvulsant activity by blocking both clonic and tonic seizures induced by audiogenic stimuli and NMDA in DBA/2 mice. The compound also exhibits high potency in blocking seizures following D-serine pretreatment. Additionally, it shows bioactivity as a potent NR2B receptor inhibitor with significant inhibitory effects on various mutations expressed in Xenopus oocytes and strong binding affinity to different mutant forms. In relation to GABAA receptors, Felbamate has an IC50 of 95.0 nM in displacing [35S]TBPS from rat brain GABAA receptors and shows an Imax value of 18.0%, suggesting interactions that may affect GABAergic neurotransmission. The compound also exhibits excellent solubility in aqueous solutions, with a solubility of 600 µM after 24 hours in 0.1 M phosphate buffer at pH 7.4, indicating good potential for effective formulation and bioavailability. Though it shows some antiviral activities against SARS-CoV-2, including inhibitory activity against the 3CL-Pro protease and viral cytotoxicity in various cell lines, these effects are relatively modest. The compound demonstrates inhibition percentages between 7.68% and 37.11% at 20 µM concentration for the protease and varied inhibition of cytotoxicity. Liver toxicity potential is significant for Felbamate, indicated by a DILI severity score of 7.0 and elevated serum enzyme levels suggesting an impact on liver function. It has been observed to cause minimal motor impairment in rats, with a TD50 greater than 500.0 mg/kg, but also demonstrates protective indices in various models of induced seizures in mice and rats, such as an ED50 of 25.0 mg/kg for maximal electroshock-induced seizures. Furthermore, Felbamate shows complex bioactivities, including roles as an SMN2 splice variant enhancer, activator and inhibitor of human muscle pyruvate kinase, antagonist of various receptors, inhibitor of Cytochrome P450 2D6, and involvement in histone lysine methyltransferase G9a inhibition. It exhibits a range of interactions with various biochemical and cellular pathways, although it also displays moderate to high potential for human intestinal absorption with a log10(%HIA +10) value of 2.0. Overall, while the compound shows promising pharmacological profiles, its therapeutic application may be limited by its potential liver toxicity..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Felbamate (W-554) is an Anti-epileptic Agent. The physiologic effect of felbamate is by means of Decreased Central Nervous System Disorganized Electrical Activity.
靶点活性
NMDAR:1.8 mM
别名非尔氨酯, 非巴马特, W-554, ADD-03055
化学信息
分子量238.24
分子式C11H14N2O4
CAS No.25451-15-4
SmilesC(COC(N)=O)(COC(N)=O)C1=CC=CC=C1
密度1.275 g/cm3
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: 23.8 mg/mL (99.9 mM), Sonication is recommended.
Ethanol: 23.8 mg/mL (99.9 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.39 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
DMSO/Ethanol
1mg5mg10mg50mg
1 mM4.1974 mL20.9872 mL41.9745 mL209.8724 mL
5 mM0.8395 mL4.1974 mL8.3949 mL41.9745 mL
10 mM0.4197 mL2.0987 mL4.1974 mL20.9872 mL
20 mM0.2099 mL1.0494 mL2.0987 mL10.4936 mL
50 mM0.0839 mL0.4197 mL0.8395 mL4.1974 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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