MK-571-L-660711-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEMK-571Cat.No.:HY-19989CASNo.:115104-28-4Synonyms:L-660711分子式:C₂₆H₂₇ClN₂O₃S₂分子量:515.09作用靶点:LeukotrieneReceptor;LPLReceptor作用通路:GPCR/GProtein储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 MK-571(L-660711)是一种口服有效、选择性的和竞争性的白三烯D4(LTD4)受体拮抗剂，在豚鼠和人肺膜中的Ki值分别为0.22和2.1nM。MK-571也是一种MRP4和ABCC1(MRP1)抑制剂。MK-571可抑制构成性和抗原刺激的S1P释放。IC50&Target LTD40.22nM(Ki,Inguineapiglung)

LTD4LTD4LTE42.1nM(Ki,Inhuman10.5(pA2,onguinea10.4(pA2,onguinealung)pigileum)pigileum)体外研究MK571(15μM,1h)markedlysuppressesconstitutiveandAg-stimulatedS1PsecretionfromRBL-2H3cellsandmastcells,andinhibitsFluo-3efflux[3].CellViabilityAssay[3]CellLine:RBL-2H3cells,humanLAD2mastcellsConcentration:15μMIncubationTime:1hResult:InhibitedS1PsecretionbyvectorandSphK1transfectedRBL-2H3cells,whereasitdidnotaffectuptakeandintracellularconversionof[3H]SphtoS1P.InhibitedFluo-3efflux,inhibitedS1PexportbyLAD2cells,andblockedAg-stimulatedreleaseofS1P.1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE体内研究MK-571(0-0.5mg/kg,orally,once)producesdose-dependentinhibitionofthedurationofantigen-induceddyspneainconscioussensitizedratstreatedwithmethysergide(3μg/kg)[1].MK-571(0-1mg/kg,orally,once)blocksLTD4-andAscaris-inducedbronchoconstrictioninconscioussquirrelmonkeys[1].MK-571(0-25mg/kg,orally,daily,for2moreweeks)showsreversalofhypoxicpulmonaryhypertension(PH),andprotectsmicefromhypoxicPH[2].AnimalModel:Hyperreactiverats(maleandfemale,200-400g,pretreatedintravenouslywith3μg/kgmethysergide,5minbeforeantigenchdlenge)[1]Dosage:0.5,0.15,and0.05mg/kgAdministration:Orally,once,1or4hbeforechallengeResult:Produceddose-dependentinhibitionofthedurationofantigen-induceddyspnea,withED50valuesof0.13(95%confidenceinterval(CI),0.03-0.62)and0.11(95%CI,0.009-1.47)mg/kg,respectively.MK-571wasevenmoreactivewhenadministeredorallyasasuspensionin1%Methocel(4hpretreatment),withanED50of0.068(95%CI,0.83-0.14)mg/kg.AnimalModel:Csnscisussquirrelmsnkeys[1]Dosage:0.1,0.5,and1mg/kgAdministration:Orally,once,2hpriortochallengewithAscarisantigenResult:Producedsignificantinhibitionofthebronchoconstrictionat0.5mg/kg,producedsignificantinhibitionoftheincreasesinRLanddecreasesinCdynat1mg/kg.AnimalModel:FVB(FriendvirusB-type)mice(Mrp4–/–andWT,6weeksold,exposedtochronichypoxia(10%O2)inaventilatedchamberfor28days)[2]Dosage:0,5,and25mg/kgAdministration:Orally,daily,for2moreweeks,maintaininhypoxicconditionsResult:Showedreversalofhypoxicpulmonaryhypertension(PH),andmicewereprotectedfromhypoxicPH.MK-571-treatedmicedisplayedlowerRVSPandFultonindexandadecreaseinthemedialthickeningofsmallpulmonaryarteriesandarterioles.客户使用本产品发表的科研文献NatCommun.2023Sep19;14(1):5709.IntJNanomedicine.2019Nov27;14:9217-9234.BiomedPharmacother.2020Sep;129:110506.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEBiomedPharmacother.2018Oct;106:1563-1569.ArchToxicol.2020Nov;94(11):3799-3817.Seemorecustomervalidationsonwww.MedChemEREFERENCESMitraP,etal.RoleofABCC1inexportofsphingosine-1-phosphatefrommastcells.ProcNatlAcadSciUSA.2006Oct31;103(44):16394-9.JonesTR,etal.PharmacologyofL-660,711(MK-571):anovelpotentandselectiveleukotrieneD4receptorantagonist.CanJPhysiolPharmacol.1989Jan;67(1):17-28.HaraY,etal.InhibitionofMRP4preventsandreversespulmonaryhypertensioninmice.JClinInvest.2011Jul;121(7):2888-97.McePdfHeightCaution: