Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemENeotame(GMPLike)Cat.No.:HY-W011053GLCASNo.:165450-17-9分子式:C??H??N?O?分子量:378.46作用靶點(diǎn):TasteReceptor;Apoptosis;DrugDerivative作用通路:GPCR/GProtein;Apoptosis;Others儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Neotame(GMPLike)是類GMP級別的Neotame(HY-W011053)，可用作藥用輔料。Neotame是Aspartame(HY-B0361)的衍生物，是一種風(fēng)味增強(qiáng)劑和低熱量，無營養(yǎng)，高強(qiáng)度的人工甜味劑，比糖甜7000-13000倍。Neotame在較高濃度下可造成腸上皮細(xì)胞死亡。Neotame誘導(dǎo)Caco-2細(xì)胞凋亡(Apoptosis)。體外研究Neotame(GMPLike)(100μMandhigher,6-24h)causesintestinalepithelialcelldeathathighconcentrationsandleakacrosstheepithelialmonolayeratlowerconcentrations(1-100μM)[3].Neotame(GMPLike)(0-1000μMandhigher,6-24h)-induceddamagetotheintestinalepitheliuminvitro,bothbarrierdisruptionandcelldeathviaapoptosis,ismediatedbythesweettastereceptor,T1R3[3].Neotame(GMPLike)(0-100μM,24h)reducesClaudin3expressionobservedatCaco-2cellsurface[3].6hIncreasedcelldeathfrom100μMandhigher.IncreasedsignificantapoptosisofCaco-2cellsfrom10μMandhigher.0,10,100μM24hReducedClaudin3expressionobservedatCaco-2cellsurface.CellViabilityAssay[3]CellLine:Caco-2cellsConcentration:0,0.01,0.1,1,10,100,1000,10000μMIncubationTime:24hResult:Showedverylittlecellviabilityathighconcentrations.ApoptosisAnalysis[3]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:Caco-2cellsConcentration:0,0.01,0.1,1,10,100,1000,10000μMIncubationTime:6hResult:Increasedcelldeathfrom100μMandhigher.IncreasedsignificantapoptosisofCaco-2cellsfrom10μMandhigher.WesternBlotAnalysis[3]CellLine:Caco-2cellsConcentration:0,10,100μMIncubationTime:24hResult:ReducedClaudin3expressionobservedatCaco-2cellsurface.體內(nèi)研究Neotame(GMPLike)(0.75mg/kg,p.o.,daily,4weeks)consumptionperturbsthediversitiesaswellasthecommunitycompositionsofgutmicrobiomeandaltersmetaboliteprofilesinfecalsamplesofmaleCD-1mice[1].AnimalModel:TenmaleCD-1micearound7weeksold[1].Dosage:0.75mg/kgAdministration:p.o.,daily,4weeksResult:Inducedloweralpha-diversityofgutmicrobiomethanthecontrolgroup.EnrichedphylumBacteroidetes,whiledecreasedFirmicutes.InducedmultiplecomponentsoffamilyLachnospiraceaeandfamilyRuminococcaceaelowerthancontrols,suchasBlautia,Dorea,OscillospiraandRuminococcus.Enrichedaminoacidmetabolism,LPSbiosynthesis,antibioticsbiosynthesisandfolatebiosynthesispathways.Inducedlowerfattyacidmetabolism,carbohydratemetabolism,lipidmetabolismandABCtransportersthanincontrols.Decreasedmostofthealteredmetabolites,suchasmalicacid,mannose-6-phosphate,5-aminovalericacidandglycericacid.Decreasedmostoftheidentifiedlipidsandfattyacids,including1,3-dipalmitate,1-monopalmitin,linoleicacidandstearicacid.Increasedtheconcentrationsofcholesterol,campesterolandstigmastanolinthefecalsamples.REFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemELiangChi,etal.EffectsoftheArtificialSweetenerNeotameontheGutMicrobiomeandFecalMetabolitesinMice.Molecules.2018Feb9;23(2):367.AnuradhaKumari,etal.StabilityofAspartameandNeotameinPasteurizedandIn-BottleSterilizedFlavouredMilk.FoodChem.2016Apr1;196:533-8.ShilA,etal.TheartificialsweetenerneotamenegativelyregulatestheintestinalepitheliumdirectlythroughT1R3-signalingandindirectlythroughpathogenicchangestomodelgutbacteria.FrontNutr.2024Apr24;11:1366409.McePdfHeightCaution:Produc