Amphotericin-B-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAmphotericinBCat.No.:HY-B0221CASNo.:1397-89-3分?式:C??H??NO??分?量:924.08作?靶點:Fungal;Antibiotic;Bacterial;Parasite作?通路:Anti-infection儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(54.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.0822mL5.4108mL10.8216mL5mM0.2164mL1.0822mL2.1643mL10mM0.1082mL0.5411mL1.0822mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:10mg/mL(10.82mM);Suspendedsolution;Needultrasonicandwarming2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:10mg/mL(10.82mM);Suspendedsolution;Needultrasonicandwarming1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性AmphotericinB針對多種真病原體的多烯抗真(fungal)劑。它與麥?甾醇不可逆地結(jié)合，導(dǎo)致膜完整性破壞并最終導(dǎo)致細(xì)胞死亡。IC50&TargetFungal[1]體外研究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].體內(nèi)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?邊的抑制劑?師www.MedChemEmMNaCl.Theosmolarityofallsolutionsisalwaysadjustedto390±5mOsmusinganadvancedinstrumentSW2osmometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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