Evenamide-NW-3509-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEvenamideCat.No.:HY-17612CASNo.:1092977-61-1Synonyms:NW-3509分?式:C??H??N?O?分?量:278.39作?靶點:SodiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(359.21mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.5921mL17.9604mL35.9208mL5mM0.7184mL3.5921mL7.1842mL10mM0.3592mL1.7960mL3.5921mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(8.98mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.98mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.98mM);ClearsolutionBIOLOGICALACTIVITY?物活性Evenamide(NW-3509)，?種有效的，具有?服活性的電壓門控鈉通道(sodiumchannel,VGSC)阻滯劑，Ki為0.4μM，可?于?于精神分裂癥研究。在精神病，躁狂癥，抑郁和攻擊性的各種嚙齒動物模型中具有顯著功效[1][2]。IC50&TargetSodiumchannel[1]體外研究Evenamideselectivelyblocksvoltage-gatedsodiumchannels(VGSCs)inavoltage-anduse-dependentmanner(Ki=0.4μM)andmodulatessustainedrepetitivefiringwithoutinducingimpairmentofthenormalneuronalexcitability.Evenamidedoesnotbind,inhibitorinteractwithover130receptors,enzymes,ortransporters[2].體內(nèi)研究Evenamideisactiveinawiderangeofpsychiatricanimalmodelsinmonotherapyandaddontoantipsychotics.EvenamideiseffectiveinattenuatingthesocialinteractiondeficitinCl395(PCP)-impairedrats(MED=1mg/kgpo)[2].REFERENCES[1].ValentinaZuliani,etal.AdvancesinDesignandDevelopmentofSodiumChannelBlockers.IonChannelsandTheirInhibitorspp79-115.[2].Faravelli,etal.P.3.f.022Evenamide(formerlyNW-3509)targetsnewmechanisms,andrepresentsanewapproachtothemanagementofuntreatedsymptomsinschizophrenia.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu