Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemECaspofunginAcetateCat.No.:HY-17006CASNo.:179463-17-3分?式:C??H??N??O??分?量:1213.42作?靶點:Fungal;Antibiotic作?通路:Anti-infection儲存?式:-20°C,sealedstorage,awayfrommoistureandlight*該產品在溶液狀態不穩定，建議您現?現配，即刻使?。溶解性數據體外實驗H2O:≥100mg/mL(82.41mM)掃描?維碼，DMSO:≥83.3mg/mL(68.65mM)運?溶解?案計算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.8241mL4.1206mL8.2412mL5mM0.1648mL0.8241mL1.6482mL10mM0.0824mL0.4121mL0.8241mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產品在溶液狀態不穩定，建議您現?現配，即刻使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(1.71mM);Clearsolution此?案可獲得≥2.08mg/mL(1.71mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(1.71mM);Clearsolution此?案可獲得≥2.08mg/mL(1.71mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.08mg/mL(1.71mM);Clearsolution此?案可獲得≥2.08mg/mL(1.71mM，飽和度未知)的澄溶液，此?案不適?于實驗周期在半個?以上的實驗。4.以1mL?作液為例，取100μL20.8mg/mL的澄請依序添加每種溶劑：PBSDMSO儲備液加到900μL??油中，混合均勻。Solubility:100mg/mL(82.41mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性CaspofunginAcetate(MK-0991Acetate)?種抗真藥，能夠?競爭性地抑制1，3-β-d葡聚糖合酶的合成。體內研究Miceinjectedwithcaspofunginatvitrealconcentrationsfrom0.41to4.1μMdonothavesignificantalterationsintheirERGwaveforms,andtheirretinashavenodetectablemorphologicchangesorlossofcells.Atthevitrealconcentrationof41μM,caspofunginreducestheamplitudesofthea-waves,b-waves,andscotopicthresholdresponsesoftheERGandalsoproducesadecreaseinthenumberofcellsintheganglioncelllayer[1].Caspofungin(8mg/kg)oramphotericinBat1mg/kggiveni.p.oncedailyfor7daysbeginningat30hafterinfectionresultedin100%survivalthroughday28relativetovehiclecontroltreatment,whichresultsin100%mortalitybyday11afterinfectiouschallenge.CaspofunginreducesrecoveryofviableCandidafromkidneyandbraintissuescomparedtovehiclecontroltreatmentonday5,whencontrolburdenpeaked.Caspofungin-treatedmicedosedwith2mg/kgorgreaterhavesignificantlylowerbrainburdenthanamphotericin-B-treatedmiceatday5.AmphotericinBandcaspofungintreatmentreducekidneyfungalburdenby1.7logCFU/gand2.46to3.64logCFU/g,respectively[2].PROTOCOLAnimalAntifungaltherapyisinitiatedat30hafterinfectiouschallengeandisgivenbyintraperitoneal(i.p.)injectionAdministration[2]oncedailyfor7days.Micearetreatedwithcaspofunginat1,2,4,or8mg/kg/day,amphotericinBat1mg/kg/day,orvehiclecontrol(steriledistilledwater).Efficacyinthismodelisassessedin3ways:bymonitoringsurvivalinagroupof10animalsineachtreatmentgroup,bymonitoringCandidaburdeninkidneyandbraintissuesinasecondsetoftreatedanimals,andbyhistologicallyevaluatingthekidneysandbrainsinathirdsetoftreatedanimals.MiceareeuthanizedbyCO2inhalation,andtissuesforbothcultureandhistologyaresampledat30h(vehicle-treatedcontrolonly)andatdays5(24hafter4thdose),8(24hafterlastdose),14,21(caspofungin-treatedonly),and28afterchallenge.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3www.MedChemEwww.MedChemE戶使?本產品發表的科研?獻?CellPhysiolBiochem.2016Aug12;39(3):939-949.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MojumderDK,etal.Evaluatingretinaltoxicityofintravitrealcaspofungininthemouseeye.InvestOphthalmolVisSci.2010Nov;51(11):5796-803.[2].Flattery,AmyM.etal.Efficacyofcaspofungininajuvenilemousemodelofcentralnervoussystemcandidiasis.AntimicrobialAgentsandChemotherapy(2011),55(7),3491-3497.McePdfHeight關注MCE中國公眾號，

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