Acetaminophen-Paracetamol-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAcetaminophenCat.No.:HY-66005CASNo.:103-90-2Synonyms:Paracetamol;4-Acetamidophenol;4'-Hydroxyacetanilide分⼦式:C₈H₉NO₂分⼦量:151.16作⽤靶点:COX;HistoneAcetyltransferase;EndogenousMetabolite;Bacterial;Parasite作⽤通路:Immunology/Inflammation;Epigenetics;MetabolicEnzyme/Protease;Anti-infection储存⽅式:Powder-20°C3years4°C2years*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:250mg/mL(1653.88mM;Needultrasonic)H2O:10mg/mL(66.16mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM6.6155mL33.0775mL66.1551mL5mM1.3231mL6.6155mL13.2310mL10mM0.6616mL3.3078mL6.6155mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：0.5%CMC-Na/salinewaterSolubility:10mg/mL(66.16mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(13.76mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(13.76mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(13.76mM);Clearsolution5.请依序添加每种溶剂：PBSSolubility:6.67mg/mL(44.13mM);Clearsolution;Needultrasonic6.请依序添加每种溶剂：saline>>0.5%Tween-80Solubility:10mg/mL(66.16mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Acetaminophen(Paracetamol)选择性环氧合酶-2(COX-2)的抑制剂，IC50值为25.8μM。Acetaminophen⼀种有效的肝N-⼄酰转移酶2(NAT2)抑制剂。Acetaminophen⼴泛使⽤的解热和⽌痛剂[1][2][3][4]。IC50&TargetCOX-2COX-125.8μM(IC50)113.7μM(IC50)体外研究Invitro,acetaminophenelicitesa4.4-foldselectivitytowardCOX-2inhibition(IC50113.7μMforCOX-1;IC5025.8μMforCOX-2).Followingoraladministrationofthedrug,maximalexvivoinhibitionsare56%(COX-1)and83%(COX-2).AcetaminophenplasmaconcentrationsremaineabovetheinvitroIC50forCOX-2foratleast5hpostadministration.ExvivoIC50values(COX-1:105.2μM;COX-2:26.3μM)ofacetaminophencomparedfavorablywithitsinvitroIC50values.Incontrasttopreviousconcepts,acetaminopheninhibitedCOX-2bymorethan80%,i.e.,toadegreecomparabletononsteroidalantiinflammatorydrugs(NSAIDs)andselectiveCOX-2inhibitors.However,a>95%COX-1blockaderelevantforsuppressionofplateletfunctionisnotachieved[1].MTTassayshowsthatAcetaminophen(APAP)inadoseof50mMsignificantly(p[2].体内研究AdministeringAcetaminophen(250ꢀmg/kg,orally)tothemicecausessignificant(p[3].PROTOCOLCellAssay[2]HumanhepatomacelllineHepG2isculturedinlowglucoseDMEMsupplementedwith10%fetalbovineserum(FBS),100U/mLPenicillinand100μg/mLStreptomycinand2mMl-glutamine.Thecellsaremaintainedin75cm2flasksat37°Cinahumidifiedatmospherecontaining5%CO2andsplitat80%confluenceevery5days.Cellsareseededin24-wellplate(2×105cells)andincubatedat37°CovernightfollowedbycellspretreatmentwithcompleteDMEMcontaininghighglucoseconcentrationinordertodownregulateautophagy.After6h,cellsaretreatedwithdifferentconcentrationsofpostbioticsobtainedfromLactobacillusfermentumBGHV110strain(HV110)inordertoselectappropriatedoseforfurther2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEexperiments.PostbioticisdissolvedincompleteDMEMmediumandaddedtothecellsinspecificfinalconcentration.Inallotherexperimentsseededcellsaretreatedwith50mMAcetaminophenaloneorco-treatedwith50mMAcetaminophenandselecteddoseoflyophilizedHV110.Toanalyzeautophagicflux,simultaneouslywithtreatments,cellsareexposedtolysosomotropicagentChloroquineataconcentrationof25μM,toinhibitautophagosome-lysosomefusion[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[3]Administration[3]MaleSwissmice(30-40ꢀg)areused.Theexperimentalanimalsaredividedintosixgroupsoffiveanimalseach.Firstly,eachgroupreceiveorallyduringsevendaysthefollowingtreatment:GroupI:themicedonotreceiveanytreatment(normal).GroupII:themicereceivecitralvehicle(0.1%Tween80solution).GroupsIII-V:themicearepretreatedwithcitralatdosesof125,250,and500ꢀmg/kg,respectively.GroupVI:themicearepretreatedwiththehepatoprotectivestandarddrugSilymarin(SLM)(200ꢀmg/kg).Afterthistime,theanimalsfastedfor8ꢀhandthenreceiveoralAcetaminophenontheseventhdayatadoseof250ꢀmg/kginGroupsII-VI.GroupIorallyreceivesalinethatcontained0.1%Tween80solution(Acetaminophenvehicle).Thestocksolutionisusedasthefirstconcentrationof50ꢀmg/mLandafterthatisdilutedin0.1%Tween80solutiontopreparethesolutionsof25and12.5ꢀmg/mL.After12ꢀhofAcetaminophenadministration,serumsamplesandlivertissuearecollectedfollowedbybiochemistryandhistologicalanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2021Sep20;12(1):5548.•NatCommun.2021Aug26;12(1):5131.•NatCommun.2021May17;12(1):2863.•Hepatology.2022Jun17.•Theranostics.2017Sep26;7(17):4135-4148.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Hinz,B,etal.Acetaminophen(paracetamol)isaselectivecyclooxygenase-2inhibitorinman.FASEBJ,2008.22(2):p.383-90.[2].MiroslavDinić,etal.LactobacillusfermentumPostbiotic-inducedA