Ibrexafungerp-citrate-MK-3118-citrate-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIbrexafungerpcitrateCat.No.:HY-107126ACASNo.:1965291-08-0Synonyms:MK3118citrate;SCY-078citrate分⼦式:C₅₀H₇₅N₅O₁₁分⼦量:922.16作⽤靶点:Fungal作⽤通路:Anti-infection储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(108.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0844mL5.4221mL10.8441mL5mM0.2169mL1.0844mL2.1688mL10mM0.1084mL0.5422mL1.0844mL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(protectfromlight)。-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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(2.71mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(2.71mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(2.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Ibrexafungerpcitrate(MK3118citrate)⼀种⼝服活性β-1,3-葡聚糖合成(β-1,3-glucansynthesis)抑制剂，具有潜在的抗真活性。Ibrexafungerpcitrate⼀种⽤于治疗念珠和曲霉感染的研究药物。体外研究Ibrexafungerpcitrate(MK3118citrate)leadstofungicidalactivityagainstvariousCandidaspp.,withaminimuminhibitoryconcentration(MIC50)of0.5µg/mL[2].体内研究PharmacokineticAnalysisIbrexafungerpcitrate(MK3118citrate)exhibitsoralbioavailability(mouse51%,rat45%,dog35%)followingoraladministration(mouse1mg/kg,rat5mg/kganddog5mg/kg)[3].Ibrexafungerpcitrate(MK3118citrate)exhibitsmoderatehalf-lives(mouse5.5,rat8.7and,dog9.3h)duetohighplasmaclearance(0.68,0.44,and0.45L/h/kgrespectively)combinedwithlargevolumesofdistribution(5.3,4.7,and4.1L/kgrespectively)followingintravenousadministration(mouse1mg/kg,rat5mg/kganddog5mg/kg)[3].AnimalModel:FemaleCD1mice,MaleandfemaleHanWisterrats,Maleandfemalebeagledogs[3]Dosage:Mice(1mg/kg),rats(5mg/kg)anddogs(5mg/kg)Administration:Intravenous(i.v.)ororalgavageResult:T1/2sof5.5,8.7,and9.3hformice,rats,anddogs,respectively.REFERENCES[1].JamesMApgar,etal.Ibrexafungerp:Anorallyactiveβ-1,3-glucansynthesisinhibitor.BioorgMedChemLett.2021Jan15;32:127661.[2].MahmoudGhannoum,etal.Ibrexafungerp:ANovelOralTriterpenoidAntifungalinDevelopmentfortheTreatmentofCandidaaurisInfections.Antibiotics(Basel).2020Aug25;9(9):539.[3].StephenAWring,etal.PreclinicalPharmacokineticsandPharmacodynamicTargetofSCY-078,aFirst-in-ClassOrallyActiveAntifungalGlucanSynthesisInhibitor,inMurineModelsofDisseminatedCandidiasis.AntimicrobAgentsChemother.2017Mar24;61(4):e02068-16.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo