Ebastine-d6-LAS-W-090-d-sub-6-sub-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEEbastine-d6Cat.No.:HY-B0674S1Synonyms:LAS-W090-d6;RP64305-d6分子式:C₃₂H₃₃D₆NO₂分子量:475.69作用靶点:HistamineReceptor;Isotope-LabeledCompounds作用通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Ebastine-d6是氘代标记的Ebastine(HY-B0674)。Ebastine(LAS-W090)是一种具有口服活性的第二代组胺H1受体(histamineH1receptor)拮抗剂。Ebastine可用于过敏性鼻炎的症状和慢性特发性荨麻疹的研究。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Ebastine(10-500ng/mL;24-48hours)treatmentsignificantlyincreasestheproliferationofHFDPC[3].Ebastine(10-500ng/mL;24-48hours)treatmentshowsdose-dependentincreasesinCyclinD1,CyclinE1,andCyclinAexpressionlevels.AndtheexpressionlevelsofCdk4,Cdk2,andCdc2arealosincreased.Ebastinetreatmentelevatesexpressionlevelsofphospho-AKTandphospho-p44/42extracellularsignal-regulatedkinase[3].体内研究Inrats,afterintravenousadministrationof[14C]Ebastineat2mg/kg,theplasmalevelofradioactivitydecreasedbiphasicallywithα-phasehalf-life(t1/2α)of1.6handβ-phasehalf-life(t1/2β)of3.1h[4].Followingoraladministrationof[14C]Ebastineatadoseof2mg/kg,theplasmalevelreachedthemaximum(Cmax)of102ngeq./mlat2handdecreasedmonophasicallywitht1/2of3.9h.At20mg/kg,amonophasicdecreaseisalsoobservedwithCmaxof1110ngeq./mlat4handwitht1/2of4.0h[4].REFERENCESFu-MingTsai,etal.ExtracellularSignal-RegulatedKinaseMediatesEbastine-InducedHumanFollicleDermalPapillaCellProliferation.BiomedResInt.2019Feb11;2019:6360503.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEJSastre.Ebastineinallergicrhinitisandchronicidiopathicurticarial.Allergy.2008Dec;63Suppl89:1-20.Fujii,etal.Absorption,distribution,metabolismandexcretionof[14C]ebastineafterasingleadministrationinrats.Arzneimittelforschung.1994Apr;44(4):527-38.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr