Fosravuconazole-L-lysine-ethanolate-BMS-379224-L-lysine-ethanolate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFosravuconazoleL-lysineethanolateCat.No.:HY-16779BCASNo.:914361-45-8Synonyms:BMS-379224L-lysineethanolate;E-1224L-lysineethanolate分⼦式:C₃₁H₄₀F₂N₇O₈PS分⼦量:739.73作⽤靶点:Fungal;Parasite作⽤通路:Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:50mg/mL(67.59mM;Needultrasonic)DMSO:50mg/mL(67.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3518mL6.7592mL13.5184mL5mM0.2704mL1.3518mL2.7037mL10mM0.1352mL0.6759mL1.3518mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.38mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.38mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FosravuconazoleL-lysineethanolate(BMS-379224L-lysineethanolate)，Ravuconazole的前药，⼀种具有⼝服活性的⼴谱抗真剂。FosravuconazoleL-lysineethanolate可⽤于念珠病，灰指甲病和寄⽣⾍病的研究。体外研究Fosravuconazolehaspotentinvitroantifungalactivityagainstawiderangeoffungalspecies,includingCandida,Aspergillus,andTrichophytonspecies[1].体内研究Fosravuconazole(E-1224;10-50mg/kg;oraladministration;daily;for20days)treatmentsuppressestheparasitemiaandpreventsdeathinmiceinfectedwiththeT.cruziYstrain[3].AnimalModel:Swissfemalemice(20-24g)inoculatedwithtrypomastigotes(Ystrain)[3].Dosage:10mg/kg,20mg/kg,30mg/kg,40mg/kg,50mg/kgAdministration:Oraladministration;daily;for20daysResult:Suppressedtheparasitemiaandpreventeddeath.REFERENCES[1].ShinichiWatanabe,etal.EfficacyandsafetyoffosravuconazoleL-lysineethanolate,anoveloraltriazoleantifungalagent,forthetreatmentofonychomycosis:Amulticenter,double-blind,randomizedphaseIIIstudy.JDermatol.2018Oct;45(10):1151-1159.[2].KatsuraHata,etal.DevelopmentofE1224byleveragingastrategicpartnershipforthemedicinescreationagainstneglectedtropicaldiseases.ParasitolInt.2020Dec25;81:102278.[3].LíviadeFigueiredoDiniz,etal.OutcomeofE1224-BenznidazoleCombinationTreatmentforInfectionwithaMultidrug-ResistantTrypanosomacruziStraininMice.AntimicrobAgentsChemother.2018May25;62(6):e00401-18.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica