AS2444697-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesAS2444697Cat.No.:HY-18992CASNo.:1287665-60-4分⼦式:C₁₉H₂₁ClN₆O₄分⼦量:432.86作⽤靶点:IRAK作⽤通路:Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:≥25mg/mL(57.76mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3102mL11.5511mL23.1022mL5mM0.4620mL2.3102mL4.6204mL10mM0.2310mL1.1551mL2.3102mL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。BIOLOGICALACTIVITY⽣物活性AS2444697⼀种具有⼝服活性的IRAK-4抑制剂，IC50为21nM[1]。AS2444697有效抑制⼈和⼤⿏IRAK-4活性。AS2444697通过抗炎作⽤表现出肾脏保护作⽤[2]。IC50&TargetIRAK421nM(IC50)体内研究AS2444697isefficaciousintheratadjuvant-inducedarthritis(ED502.7mg/kg,BID,PO)andtheratcollagen-inducedarthritis(ED501.6mg/kg,BID,PO)diseasemodels.Goodbioavailabilitywasseeninrat(F%50)anddog(F%78)pharmacokineticstudies[1].1/2AS2444697(0.3-3mg/kg)significantlyincreasestheplasmalevelsofIL-1β,IL-6,TNF-α,MCP-1,andaminotransferases(ALTandAST)inLPS/GalN-treatedmice.SingleadministrationofAS2444697(0.3-3mg/kg)dose-dependentlydecreasesplasmalevelsoftheseallparameters,andtheseeffectsweresignificantatdosesof1mg/kgorhigher[2].AfteroraladministrationofAS2444697(3mg/kg)to5/6Nxrats,plasma,andtissue(liverandkidney)concentrationsoftheunchangeddrugpeakedat1handthengraduallydecreased,withaterminalhalf-lifeof2.7-2.9h[2].AnimalModel:Male6-week-oldWistarratsandBalb/cmice[2]Dosage:0.3-3mg/kgAdministration:Singleadministration;orallyResult:TheplasmalevelsofIL-1β,IL-6,TNF-α,MCP-1,andaminotransferases(ALTandAST)weresignificantlyincreased.REFERENCES[1].JohnHynesJr,etal.ChapterNine-AdvancesintheDiscoveryofSmall-MoleculeIRAK4Inhibitors.AnnuRepMedChem.2014(49):117-133.[2].MitsuhiroKondo,etal.Renoprotectiveeffectsofnovelinterleukin-1receptor-associatedkinase4inhibitorAS2444697throughanti-inflammatoryactionin5/6nephrectomizedrats.NaunynSchmiedebergsArchPharmacol.2014Oct;387(10):909-19.McePdfHeightMedChemExpress(MCE)只为有资质的科研机构、医药企业基于科