AmphotericinBisanamphipathicpolyeneantibioticwhichpermeabilizesergosterol-containingmembranes.

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].

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

• [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.

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.

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.

• [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.

924.08

C₄₇H₇₃NO₁₇

1397-89-3

RoomtemperatureincontinentalUS;mayvaryelsewhere

10mMinDMSO;H₂O:<0.1="">

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

Purity:>98.00%

SelectBatch:HY-B0221-13062HY-B0221-13063

DataSheet(123KB)SDS(389KB)

COA(96KB)HNMR(335KB)

HandlingInstructions(1252KB)

• [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.

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托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

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类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

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