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当前位置: 首页 > 产品中心 > Small_molecule > Medchemexpress/Amphotericin B/HY-B0221/500mg
商品详细Medchemexpress/Amphotericin B/HY-B0221/500mg
Medchemexpress/Amphotericin B/HY-B0221/500mg
Medchemexpress/Amphotericin B/HY-B0221/500mg
商品编号: HY-B0221-10mM*1mLinDMSO
品牌: MedChemExp
市场价: ¥1100.00
美元价: 660.00
产地: 美国(厂家直采)
公司:
产品分类: 小分子
公司分类: Small_molecule
联系Q Q: 3392242852
电话号码: 4000-520-616
电子邮箱: info@ebiomall.com
商品介绍
AmphotericinBisanamphipathicpolyeneantibioticwhichpermeABIlizesergosterol-containingmembranes.
Description

AmphotericinBisanamphipathicpolyeneantibioticwhichpermeabilizesergosterol-containingmembranes.

InVitro

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].

InVivo

AmphotericinBresultsinprolongingtheincubationtimeanddecreasingPrPScaccumulationinthehamsterscrapiemodel.AmphotericinBmarkedlyreducesPrPSclevelsinmicewithtransmissIBLesubacutespongiformencephalopathies(TSSE)[4].AmphotericinBexertsadirecteffectonPlasmodiumfalciparumandinfluenceseryptosisofinfectederythrocytes,parasitemiaandhostsurvivalinmurinemalaria.AmphotericinBtendstodelaytheincreaseofparasitemiaandsignificantlydelayshostdeathplasmodiumberghei-infectedmice[5].

ClinicalTrial
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References
  • [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.PharmacologicalstudiesofanewderivativeofamphotericinB,MS-8209,inmouseandhamsterscrapie.JGenVirol.1994Sep;75(Pt9):2499-503.

    [5].AdamsML,etal.AmphotericinBencapsulatedinmicellesbasedonpoly(ethyleneoxide)-block-poly(L-aminoacid)derivativesexertsreducedinvitrohemolysisbutmaintainspotentinvivoantifungalactivity.Biomacromolecules.2003May-Jun;4(3):750-7.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.0822mL5.4108mL10.8216mL
5mM0.2164mL1.0822mL2.1643mL
10mM0.1082mL0.5411mL1.0822mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[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]

AmphotericinBisdissolvedinDMSO.

ThekineticsofcelldeathinducedbyAmBagainstLeishmaniapromastigotesisfollowedbyusingfluorometrywiththeDNA-bindingcompoundethidiumbromide(EB).FluorescencemeasurementsareperformedonaSPEXFluorologIIspectrophotometerat365-580nmexcitation-emissionwavelengths.Promastigotesatafinalconcentrationof25×106cells/mLareincubatedfor5minwithgentlestirringinthefluorescencecuvettewith2mLofdifferentbufferedsolutionsbutalwayscontaining10mMglucoseandEB(50mM).Aftersignalstabilizationisachieved,AmBisaddedanddissolvedindimethylsulfoxide.MaximalEBincorporationisalwaysobtainedbyaddingdigitonin(50mg/mL).Allsolutionsusedarebufferedwith75mMTRIS(pH47.6)andcontain150mMNaCl(BNa+),150mMKCl(BK+),150mMcholinechloride,and100mMsucrose,100mMNaCl.Theosmolarityofallsolutionsisalwaysadjustedto390±5mOsmusinganadvancedinstrumentSW2osmometer.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [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.PharmacologicalstudiesofanewderivativeofamphotericinB,MS-8209,inmouseandhamsterscrapie.JGenVirol.1994Sep;75(Pt9):2499-503.

    [5].AdamsML,etal.AmphotericinBencapsulatedinmicellesbasedonpoly(ethyleneoxide)-block-poly(L-aminoacid)derivativesexertsreducedinvitrohemolysisbutmaintainspotentinvivoantifungalactivity.Biomacromolecules.2003May-Jun;4(3):750-7.

MolecularWeight

924.08

Formula

C₄₇H₇₃NO₁₇

CASNo.

1397-89-3

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO;H2O:<0.1="">

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:>98.00%