Felbamate-W-554-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFelbamateCat. No.: HY-B0184CAS No.: 25451-15-4Synonyms: W-554; ADD-03055分式: CHNO分量: 238.24作靶点: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性数据体外实验 DMSO : 100 mg/mL (419.74 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.1974 mL 20.9872 mL 41.9745 mL5 mM 0.8395 mL 4.1974 mL 8.3949 mL10 mM 0.4197 mL 2.0987 mL 4.1974 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制

3、前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (11.54 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (11.54 mM); Clear solution

4、1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (11.54 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Felbamate (W-554)镇静性抗痉挛剂，活性与NMDA受体相关。IC50 & Target NMDA Receptor 1.体外研究 Felbamate (W-554) is an anti-epileptic drug used in the treatment of epi

5、lepsy. It is used to treat partialseizures (with and without generalization) in adults and partial and generalized seizures associated withLennox-Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/orliver failure limit the drugs usage to severe refracto

6、ry epilepsy 1. Felbamate (W-554) has been proposed toa unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDAreceptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does causepharmacological inhibition of NMDA rec

7、eptor of relevance of NMDA receptor blockade as a strategy for thetreatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate onNMDA receptors to its therapeutic action in epilepsy is uncertain 2.REFERENCES1. Kuo CC, et al. Use-dependent inhibition of the N

8、-methyl-D-aspartate currents by felbamate: a gating modifier with selective binding tothe desensitized channels. Mol Pharmacol. 2004 Feb;65(2):370-80.2. Harty TP, et al. Felbamate block of recombinant N-methyl-D-aspartate receptors: selectivity for the NR2B subunit. Epilepsy Res. 2000Mar;39(1):47-55.McePdfHeightCaution: Product has not been fully validated for medical applications