Felbamate-W-554-DataSheet-生命科學試劑-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作靶點: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性數據體外實驗 DMSO : 100 mg/mL (419.74 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制

3、前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (11.54 mM); Clear solution2. 請依序添加每種溶劑： 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 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (11.54 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Felbamate (W-554)鎮(zhèn)靜性抗痙攣劑，活性與NMDA受體相關。IC50 & Target NMDA Receptor 1.體外研究 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