ASB14780-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEASB14780Cat.No.:HY-119019CASNo.:1069046-00-9分?式:C??H??N?O?分?量:582.69作?靶點:Phosphatase作?通路:MetabolicEnzyme/Protease儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性ASB14780?類4-苯氧衍?物，胞質(zhì)磷脂酶cPLA2α抑制劑，IC50為20nM。IC50&TargetIC50:20nM(cPLA2α);0.54μM(guineapigcPLA2α);0.64μM(humancPLA2α)[1]體外研究ASB14780showsselectivitytocPLA2α(IC50=20nM)overtypeIIsPLA2(IC50>10μM)[1].ASB14780(30minpre-incucation)inhibitscPLA2αinguineapigwholeblood(GWB)andhumanwholeblood(HWB)inaspecies-deriveddifferences,withIC50sof0.54μMand0.64μM,respectively,15minafterbeingstimulatedby5μMcalciumionophoreA23187[1].體內(nèi)研究TPA(tetradecanoylphorbolacetate)causesacuteinflammationwithear,resultinginedema[1].ASB14780(50mg/kg;p.o.;once)suppressestheincreaseintheearthicknesselicitedbytheapplicationofTPA(tetradecanoylphorbolacetate)inmouse[1].ASB14780(5mg/kg;20mg/kg;p.o.;oncedaily)attenuatesAHR(airwayhyperreactivity),andinhibitsIAR(immediateasthmaticresponse)andLAR(lateasthmaticresponse)inadose-dependentmanner[1].ASB14780showswelloralactivityof89.6%inmousecalculatedfromtheratiooforaladministration’sAUC(10mg/kg;p.o.)andintravenonousadministration’sAUC(1mg/kg;i.v.)[1].OralBioavailabilitiesandPharmacokineticParametersofASB14780[1]ModelF(%)AUC(h?μg/mL)Cmax(μg/mL)mouse2dog34.317.14.96monkey30.94.962.29Note:Basedon10mg/kgp.o.dosingdata.AnimalModel:TPA(TetradecanoylPhorbolAcetate)-inducedEarEdemaModelinmouse(femaleC57BL/6mice)[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:50mg/kgAdministration:Oralgavage;30minbeforeTPAstimulationResult:Showedhighpotencyandinhibitedearswellingby30%andindicatedtheinvivoanti-inflammatoryactivity.AnimalModel:GuineaPigOvalbumin(OVA)-inducedAsthmaModel[1]Dosage:5mg/kg,20mg/kgAdministration:Oralgavage;twosingledoses;1hbeforeand8hafterpassivelysensitizedadministrationResult:ExhibitssuppressiononIAR(immediateasthmaticresponse)andLAR(lateasthmaticresponse)inadose-dependentmanner.REFERENCES[1].TomooT,etal.Design,synthesis,andbiologicalevaluationof3-(1-Aryl-1H-indol-5-yl)propanoicacidsasnewindole-basedcytosolicphospholipaseA2αinhibitors.JMedChem.2014.57(17):7244-62.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo