PPADS-tetrasodium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPPADStetrasodiumCat.No.:HY-101044CASNo.:192575-19-2分⼦式:C₁₄H₁₀N₃Na₄O₁₂PS₂分⼦量:599.3作⽤靶点:P2XReceptor;Na+/Ca2+Exchanger作⽤通路:MembraneTransporter/IonChannel储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验H2O:50mg/mL(83.43mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6686mL8.3431mL16.6861mL5mM0.3337mL1.6686mL3.3372mL10mM0.1669mL0.8343mL1.6686mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性PPADStetrasodiuma⼀种⾮选择性P2X受体拮抗剂。PPADStetrasodiuma阻断重组P2X1、-2、-3、-5，IC50范为1～2.6μM。PPADS-tetrasodiuma阻断天然P2Y2样(IC50~0.9mM)和重组P2Y4(IC50~15mM)受体。PPADStetrasodiuma豚⿏⽓道平滑肌Na/Ca²交换逆模式的抑制剂。体外研究PPADStetrasodiuma(1-30μM;10-50minutes)inhibitsNa+/Ca2+exchangerreversemode(NCXREV)inatime-andconcentrationdependentmanner[2].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEPPADStetrasodiumaiseffectiveatothernativeandrecombinantP2XRs.AthumanP2XRssensitivitytoPPADStetrasodiumadependedonthesubtypeandishighestatthehP2X1,-2,-3,-5,and-7RswithanIC50of~1-3and~30μMforthehP2X4R[3].体内研究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.户使⽤本产品发表的科研⽂献•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