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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(diǎn):Fungal;Antibiotic作?通路:Anti-infection儲(chǔ)存?式:-20°C,sealedstorage,awayfrommoistureandlight*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)?現(xiàn)配,即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:≥100mg/mL(82.41mM)掃描?維碼,DMSO:≥83.3mg/mL(68.65mM)運(yùn)?溶解?案計(jì)算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.8241mL4.1206mL8.2412mL5mM0.1648mL0.8241mL1.6482mL10mM0.0824mL0.4121mL0.8241mL請(qǐng)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(chǔ)備液;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)?現(xiàn)配,即刻使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液,再依次添加助溶劑:為保證實(shí)驗(yàn)結(jié)果的可靠性,澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的?式助溶1.請(qǐng)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(chǔ)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(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請(qǐng)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(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中,混合均勻。請(qǐng)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(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。4.以1mL?作液為例,取100μL20.8mg/mL的澄請(qǐng)依序添加每種溶劑:PBSDMSO儲(chǔ)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(jìng)爭(zhēng)性地抑制1,3-β-d葡聚糖合酶的合成。體內(nèi)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(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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(guān)注MCE中國(guó)公眾號(hào),

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