Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEDegarelixacetateCat.No.:HY-16168CASNo.:934016-19-0Synonyms:FE200486分子式:C??H???ClN??O??分子量:1692.31作用靶點:GnRHReceptor作用通路:GPCR/GProtein儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Degarelixacetate(FE200486)是一種對人類促性腺激素釋放激素(GnRH)受體具有高親和力/選擇性的十肽(IC50=3nM)。Degarelixacetate(FE200486)用于前列腺癌的研究。體外研究Degarelix(FE200486)showsonlyveryweakhistamine-releasingpropertiesandthelowestcapacityforhistaminereleaseamongtheantagonistsofLHRH,includingCetrorelix(HY-P0009),Abarelix(HY-13534),andGanirelix(HY-P1628)[3].Degarelix(1nM-10μM,0-72h)reducescellviabilityinallprostatecelllines(WPE1-NA22,WPMY-1,BPH-1,VCaPcells),withtheexceptionofthePC-3cells[4].Degarelix(10μM,0-72h)exertsadirecteffectonprostatecellgrowththroughapoptosis[4].CellViabilityAssay[4]CellLine:WPMY-1,WPE1-NA22,BPH-1,LNCaPandVCaP.Concentration:1nM-10μM.IncubationTime:48-72hResult:WPMY-1cellsat48and72h,WPE1-NA22cellsat72hours,BPH-1cellsat48and72h,LNCaPcellsat48and72h.Reducedcellviabilityinallprostatecelllines,withtheexceptionofthePC-3cells.ApoptosisAnalysis[4]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:WPE1-NA22,BPH-1,LNCaPandVCaP.Concentration:10μM.IncubationTime:24,48and72h.Result:Inducedasignificantincreaseoncaspase3/7activation.體內(nèi)研究Degarelix(FE200486freebase)(0-10μg/kg;s.c.;once)decreasesplasmaLHlevelsandplasmatestosteronelevelsinadose-dependentmannerincastratedrats[5].Degarelix(FE200486freebase)isstablewhenincubatedinmicrosomesandcryopreservedhepatocytesfromanimallivertissue.Inratanddog,mostofthedegarelixdoseiseliminatedwithin48hviaurineandfecesinequalamounts(40-50%ineachmatrix),whereasinmonkeythemajorrouteofexcretionisfecal(50%)andrenal(22%)[6].AnimalModel:MaleSprague-Dawleyrats,castrated[5].Dosage:0.3,1,3and10μg/kgor12.5,50,and200μg/kg.Administration:Subcutaneousinjection,once.Result:Forthe50μg/kgand200μg/kgdoses,t1/2ofabsorptionvalueswere4minand30min,Tmaxvalueswere1hand5h,andapparentplasmadisappearancet1/2valueswere12hand67h,respectively.Producedadose-dependentdecreaseinplasmatestosteronelevelswithaminimaleffectivedoseof1μg/kg.客戶使用本產(chǎn)品發(fā)表的科研文獻CancerLett.2023May9;216209.ArteriosclerThrombVascBiol.2024Jan11.FASEBJ.2023Feb;37(2):e22772.JImmunol.2022Dec21;ji2200696.Prostate.2021Jul1.Seemorecustomervalidationsonwww.MedChemEREFERENCESAndersSonesson,etal.InVitroandInVivoHumanMetabolismofDegarelix,aGonadotropin-ReleasingHormoneReceptorBlocker.DrugMetabolismandDisposition.July2013,41(7)1339-1346.Degarelix.RickFG,etal.Anupdateontheuseofdegarelixinthetreatmentofadvancedhormone-dependentprostatecancer.OncoTargetsTher.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE2013Apr16;6:391-402.SakaiM,etal.InsearchofthemolecularmechanismsmediatingtheinhibitoryeffectoftheGnRHantagonistdegarelixonhumanprostatecellgrowth.PLoSOne.2015Mar26;10(3):e0120670.BroquaP,etal.Pharmacologicalprofileofanew,potent,andlong-actinggonadotropin-releasinghormoneantagonist:degarelix.JPharmacolExpTher.2002Apr;301(1):95-102.SonessonA,etal.Metaboliteprofilesofdegarelix,anewgonadotropin-releasinghormonereceptorantagonist,inrat,dog,andmonkey.DrugMetabDispos.2011Oct;39(10):1895-903.McePdfHeightCaution:Product