ICA-069673-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEICA-069673Cat.No.:HY-101396CASNo.:582323-16-8分?式:C??H?ClF?N?O分?量:269.63作?靶點:PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥34mg/mL(126.10mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.7088mL18.5439mL37.0879mL5mM0.7418mL3.7088mL7.4176mL10mM0.3709mL1.8544mL3.7088mL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(fù)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?。BIOLOGICALACTIVITY?物活性ICA-069673KCNQ2/Q3鉀通道激活劑，IC50值為0.69μM。IC50&TargetIC50:0.69μM(KCNQ2/Q3potassiumchannel)[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究ICA-069673isfoundtobe20-foldselectiveforKCNQ2/Q3overKCNQ3/Q5andhasnomeasurableactivityagainstapanelofcardiacionchannels(IC50values>30μMforhERG,Nav1.5,Ltypechannels,andKCNQ1)aswellasnoactivityonGABA(A)gatedchannelsat10μM[1].ICA-069673exhibitsmuchstrongereffectsonKCNQ2channels,includingalargehyperpolarizingshiftofthevoltage-dependenceofactivation,an2-foldenhancementofpeakcurrentandpronouncedsubtypespecificityforKCNQ2overKCNQ3.BasedonICA73sensitivityofchimericconstructsofthetransmembranesegmentsofKCNQ2andKCNQ3,thisdrugappearstointeractwiththeKCNQ2voltagesensor(S1-S4)[2].戶使?本產(chǎn)品發(fā)表的科研?獻?ResearchSquarePrint.September6th,2022Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WickendenAD,etal.N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide(ICA-27243):anovel,selectiveKCNQ2/Q3potassiumchannelactivator.MolPharmacol.2008Mar;73(3):977-86.Epub2007Dec18.[2].WangAW,etal.Sequencedeterminantsofsubtype-specificactionsofKCNQchannelopeners.JPhysiol.2017Feb1;595(3):663-676.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4