Amphotericin-B-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAmphotericinBCat.No.:HY-B0221CASNo.:1397-89-3分⼦式:C₄₇H₇₃NO₁₇分⼦量:924.08作⽤靶点:Fungal;Antibiotic;Bacterial;Parasite作⽤通路:Anti-infection储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:50mg/mL(54.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0822mL5.4108mL10.8216mL5mM0.2164mL1.0822mL2.1643mL10mM0.1082mL0.5411mL1.0822mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:10mg/mL(10.82mM);Suspendedsolution;Needultrasonicandwarming2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:10mg/mL(10.82mM);Suspendedsolution;Needultrasonicandwarming1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性AmphotericinB针对多种真病原体的多烯抗真(fungal)剂。它与麦⾓甾醇不可逆地结合，导致膜完整性破坏并最终导致细胞死亡。IC50&TargetFungal[1]体外研究AmphotericinBadministrationislimitedbyinfusion-relatedtoxicity,includingfeverandchills,aneffectpostulatedtoresultfromproinflammatorycytokineproductionbyinnateimmunecells.AmphotericinBinducessignaltransductionandinflammatorycytokinereleasefromcellsexpressingTLR2andCD14[1].AmphotericinBinteractswithcholesterol,themajorsterolofmammalmembranes,thuslimitingtheusefulnessofAmphotericinBduetoitsrelativelyhightoxicity.AmphotericinBisdispersedasapre-micellarorasahighlyaggregatedstateinthesubphase[2].AmphotericinBonlykillsunicellularLeishmaniapromastigotes(LPs)whenaqueousporespermeabletosmallcationsandanionsareformed.AmphotericinB(0.1mM)inducesapolarizationpotential,indicatingK+leakageinKCl-loadedliposomessuspendedinaniso-osmoticsucrosesolution.AmphotericinB(0.05mM)exhibitsanearlytotalcollapseofthenegativemembranepotential,indicatingNa+entryintothecells[3].体内研究AmphotericinBresultsinprolongingtheincubationtimeanddecreasingPrPScaccumulationinthehamsterscrapiemodel.AmphotericinBmarkedlyreducesPrPSclevelsinmicewithtransmissiblesubacutespongiformencephalopathies(TSSE)[4].AmphotericinBexertsadirecteffectonPlasmodiumfalciparumandinfluenceseryptosisofinfectederythrocytes,parasitemiaandhostsurvivalinmurinemalaria.AmphotericinBtendstodelaytheincreaseofparasitemiaandsignificantlydelayshostdeathplasmodiumberghei-infectedmice[5].PROTOCOLKinaseAssay[1]THP-1andHEK293cellsaretransientlytransfectedusingDEAE-dextranandPolyfectreagent,respectively.PlasmidstransfectedcontaingenescodingfortheNF-κB-dependentpELAM-lucluciferasereporter,TLR2,TLR4,CD14,andMD2.Cells(5×105THP-1or1×105HEK293)areaddedto12-wellplates,washedafter18h,andstimulatedfor5h.Cellsarethenlysedwithreporterlysisbufferasdirected,andlysatesareanalyzedforluminescenceusingPromegaluciferasesubstrateandaMonolight3010luminometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[3]ThekineticsofcelldeathinducedbyAmBagainstLeishmaniapromastigotesisfollowedbyusingfluorometrywiththeDNA-bindingcompoundethidiumbromide(EB).FluorescencemeasurementsareperformedonaSPEXFluorologIIspectrophotometerat365-580nmexcitation-emissionwavelengths.Promastigotesatafinalconcentrationof25×106cells/mLareincubatedfor5minwithgentlestirringinthefluorescencecuvettewith2mLofdifferentbufferedsolutionsbutalwayscontaining10mMglucoseandEB(50mM).Aftersignalstabilizationisachieved,AmBisaddedanddissolvedindimethylsulfoxide.MaximalEBincorporationisalwaysobtainedbyaddingdigitonin(50mg/mL).Allsolutionsusedarebufferedwith75mMTRIS(pH47.6)andcontain150mMNaCl(BNa+),150mMKCl(BK+),150mMcholinechloride,and100mMsucrose,1002/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEmMNaCl.Theosmolarityofallsolutionsisalwaysadjustedto390±5mOsmusinganadvancedinstrumentSW2osmometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Cell.2022Aug18;185(17):3124-3137.e15.•Cancers(Basel).2022,14(14),3550.•JVirol.2020Nov23;94(24):e01350-20.•FrontCellInfectMicrobiol.2020Jun26;10:320.•AmJPhysiolCellPhysiol.2019Aug1;317(2):C277-C286.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SauK,etal.TheantifungaldrugamphotericinBpromotesinflammatorycytokinereleasebyaToll-likereceptor-andCD14-dependentmechanism.JBiolChem.2003Sep26;278(39):37561-8.Epub2003Jul14.[2].BarwiczJ,etal.Theeffectofaggregationstateofamphotericin-Bonitsinteractionswithcholesterol-orergosterol-containingphosphatidylcholinemonolayers.ChemPhysLipids.1997Feb28;85(2):145-55.[3].RamosH,etal.AmphotericinBkillsunicellularleishmaniasbyformingaqueousporespermeabletosmallcationsandanions.JMembrBiol.1996Jul;152(1):65-75.[4].DemaimayR,etal.Pharma