Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPPADStetrasodiumCat.No.:HY-101044CASNo.:192575-19-2分?式:C??H??N?Na?O??PS?分?量:599.3作?靶點:P2XReceptor;Na+/Ca2+Exchanger作?通路:MembraneTransporter/IonChannel儲存?式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗H2O:50mg/mL(83.43mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6686mL8.3431mL16.6861mL5mM0.3337mL1.6686mL3.3372mL10mM0.1669mL0.8343mL1.6686mL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(sealedstorage,awayfrommoisture)。-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PPADStetrasodiuma?種?選擇性P2X受體拮抗劑。PPADStetrasodiuma阻斷重組P2X1、-2、-3、-5，IC50范為1～2.6μM。PPADS-tetrasodiuma阻斷天然P2Y2樣(IC50~0.9mM)和重組P2Y4(IC50~15mM)受體。PPADStetrasodiuma豚??道平滑肌Na/Ca2交換逆模式的抑制劑。體外研究PPADStetrasodiuma(1-30μM;10-50minutes)inhibitsNa+/Ca2+exchangerreversemode(NCXREV)inatime-andconcentrationdependentmanner[2].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEPPADStetrasodiumaiseffectiveatothernativeandrecombinantP2XRs.AthumanP2XRssensitivitytoPPADStetrasodiumadependedonthesubtypeandishighestatthehP2X1,-2,-3,-5,and-7RswithanIC50of~1-3and~30μMforthehP2X4R[3].體內(nèi)研究PPADStetrasodiuma(15-60mg/100gbodyweight(BW);i.p.;every12hoursfor8days)inhibitsglomerularmesangialcells(MC)proliferationwithoutalteringproliferationofnon-MCinvivoinmesangialproliferativeglomerulonephritis[4].AnimalModel:MaleSprague-Dawleyratsweighing160to200g(anti-Thy1diseasemode)[4]Dosage:15mg/100gBW,30mg/100gBW,60mg/100gBWAdministration:i.p.;every12hoursfor8days(thefirstPPADSinjectionwasadministered60minutesafterdiseaseinduction,andtheloadingdosealwayscontaineddoubletheamountofPPADScomparedtothefollowinginjections.)Result:Specificallyanddose-dependentlyreducedearly(day3)glomerularmesangialcellproliferationwithoutalteringproliferationofnon-MC.戶使?本產(chǎn)品發(fā)表的科研?獻?JBiolChem.2021Sep3;101166.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Flores-SotoE,etal.PPADS,aP2Xreceptorantagonist,asanovelinhibitorofthereversemodeoftheNa/Ca2exchangeringuineapigairwaysmoothmuscle.EurJPharmacol.2012Jan15;674(2-3):439-44.[2].HuoH,etal.MappingthebindingsiteoftheP2XreceptorantagonistPPADSrevealstheimportanceoforthostericsitechargeandthecysteine-richheadregion.JBiolChem.2018Aug17;293(33):12820-12831.[3].EinflussvonATPundseinenDerivatenaufdieAktivierungvonMonozyten.[4].RostS,etal.P2receptorantagonistPPADSinhibitsmesangialcellproliferationinexperimentalmesangialproliferativeglomerulonephritis.KidneyInt.2002Nov;62(5):1659-71.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor