Pyrintegrin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEPyrintegrinCat.No.:HY-13306CASNo.:1228445-38-2分⼦式:C₂₃H₂₅N₅O₃S分⼦量:451.54作⽤靶点:Integrin作⽤通路:Cytoskeleton储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(553.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2146mL11.0732mL22.1464mL5mM0.4429mL2.2146mL4.4293mL10mM0.2215mL1.1073mL2.2146mL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，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.61mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.61mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性Pyrintegrin⼀种β1整合素(β1-integrin)激动剂，也⼀种2,4-⼆取代的嘧啶，可促进胚胎⼲细胞存活。Pyrintegrin能增强细胞-细胞外质(ECM)粘附介导的整联蛋⽩信号传导。Pyrintegrin可⽤作⾜细胞保护剂，并具有强⼤的成脂作⽤。IC50&Targetβ1-integrin[2]体外研究Pyrintegrin(0-10µM;1hour;hASCs)treatmentinhibitsBMP4-mediatedphosphorylationofBMPresponsiveSMAD1/5inadose-dependentmanner(IC50ꢀofꢀ1.14ꢀμM)[1].Invitro,Pyrintegrinstimulatshumanadiposestem/progenitorcells(hASCs)todifferentiateintolipid-ladenadipocytesbyupregulatingperoxisomeproliferator-activatedreceptor(PPARγ)andCCAAT/enhancer-bindingprotein-α(C/EBPα),withdifferentiatedcellsincreasinglysecretingadiponectin,leptin,glycerolandtotaltriglycerides.PyrintegrinattenuatesRunx2andOsxviaBMP-mediatedSMAD1/5phosphorylation[1].TreatmentwithPyrintegrinpreventsdamage-induceddecreasesinF-actinstressfibers,focaladhesions,andactiveβ1-integrinlevelsinculturedcells[2].WesternBlotAnalysisCellLine:Humanadiposestem/progenitorcells(hASCs)[2]Concentration:0µM,0.2µM,0.5µM,1µM,2µM,5µM,10µMIncubationTime:1hourResult:InhibitedBMP4-mediatedphosphorylationofBMPresponsiveSMAD1/5inadose-dependentmanner.体内研究Pyrintegrin(10mg/kg;intraperitonealinjection;once;C57BL/6Jmice)treatmentprotectsmicefromLPS-inducedpodocytefootprocesseffacementandproteinuria.AnalysisofthemurineglomerulishowsthatLPSadministrationreducesthelevelsofactiveβ1integrininthepodocytes,whichispreventedbycotreatmentwithPyrintegrin[2].Inrats,Pyrintegrinreducespeakproteinuriacausedbypuromycinaminonucleoside-inducednephropathy[2].Pyrintegrininducespostnataladiposetissueformationinvivooftransplantedadiposestem/progenitorcells(ASCs)andrecruitedendogenouscells.Invivo,Pyrintegrin-treatedhumanadiposestem/progenitorcells(ASCs)in3D-bioprintedscaffolds,whentransplantedinthedorsumofathymicmice,yieldedectopicallyformedadiposetissuethatexpressedhumanPPARγ.Remarkably,Pyrintegrin-adsorbedcollagengelimplantedintheinguinalfatpadpromotedadipogenesisformedbyhostendogenouscells,suggestingitsabilitytoinduceinsituadipogenesiswithouttheneedforcelltransplantation[1].AnimalModel:FemalewildtypeC57BL/6Jmice(10-week-old)injectedwithLPS[2]Dosage:10mg/kgAdministration:Intraperitonealinjection;onceResult:ProvidedasignificantprotectionfortheseanimalsfromLPS-inducedproteinuriaandfoot2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEprocesse(FP)effacement.REFERENCES[1].ShahBS,etal.PyrintegrinInducesSoftTissueFormationbyTransplantedorEndogenousCells.SciRep.2017Jan27;7:36402.[2].LeeHW,etal.APodocyte-BasedAutomatedScreeningAssayIdentifiesProtectiveSmallMolecules.JAmSocNephrol.2015Nov;26(11):2741-52.[3].XuY,etal.Revealingacoresignalingregulatorymechanismforpluripotentstemcellsurvivalandself-renewalbysmallmolecules.ProcNatlAcadSciUSA.2010May4;107(18):8129-34.McePdfHeig