ZD-9379-sodium-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEZD9379sodiumCat.No.:HY-106969ACASNo.:170142-29-7分子式:C₁₉H₁₄ClN₃NaO₄分子量:406.77作用靶点:GlycineReceptor(GlyR);iGluR作用通路:MembraneTransporter/IonChannel;NeuronalSignaling储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性ZD9379sodium是一种竞争性甘氨酸/NMDA受体(glycine/NMDAreceptor)拮抗剂，IC50(谷氨酸位点)为75nM。ZD9379sodium选择性拮抗NMDA受体上的甘氨酸结合位点(GlyB位点)，抑制甘氨酸与NMDA受体结合，缓解兴奋性毒性。ZD9379sodium通过抑制皮质扩散性抑制(SDs)的频次，减轻缺血半暗带能量耗竭，延缓梗死扩展。ZD9379sodium在小鼠模型中减少梗死体积并改善神经功能。ZD9379sodium可用于急性缺血性卒中等研究。体内研究ZD9379(5mg/kg,i.v.,for4hours)sodiumsignificantlyreducestheinfarctvolumeintheratmodelofpermanentmiddlecerebralarteryocclusion(MCAO),inhibitsSDs,andimprovesneurologicalfunction[1].AnimalModel:MCAOmodelestablishedinmaleSprague-Dawleyrats(weighing290-340grams)[1]Dosage:5mg/kgAdministration:Intravenousinjection(i.v.),for4hoursResult:Significantlyreducedinfarctionvolume,andthenumberofSDswassignificantlydecreased.Significantlyimprovedneurologicalscores,withoutcausingsignificantchangesinphysiologicalparametersorbehavioralsideeffects.REFERENCES[1].TatlisumakT,etal.AglycinesiteantagonistZD9379reducesnumberofspreadingdepressionsandinfarctsizeinratswithpermanent1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEmiddlecerebralarteryocclusion.ActaNeurochirSuppl.2000;76:331-3.[2].CatarziD,ColottaV,VaranoF.CompetitiveGly/NMDAreceptorantagonists.CurrTopMedChem.2006;6(8):809-21.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-5