Islatravir-MK-8591-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIslatravirCat.No.:HY-104012CASNo.:865363-93-5Synonyms:MK-8591分⼦式:C₁₂H₁₂FN₅O₃分⼦量:293.25作⽤靶点:HIV;ReverseTranscriptase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DMSO:100mg/mL(341.01mM;Needultrasonic)H2O:3.57mg/mL(12.17mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4101mL17.0503mL34.1006mL5mM0.6820mL3.4101mL6.8201mL10mM0.3410mL1.7050mL3.4101mL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:≥2.08mg/mL(7.09mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.09mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.09mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥1.1mg/mL(3.75mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥1.1mg/mL(3.75mM);Clearsolution6.请依序添加每种溶剂：PBSSolubility:1.35mg/mL(4.60mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Islatravir(MK-8591)⼀种核苷逆转录酶(reversetranscriptase)抑制剂，具有抗HIV-1活性，对HIV-1(WT)，HIV-1(M184V)，HIV-1(MDR)的EC50值分别为0.068nM，3.1nM和0.15nM。IC50&TargetHIV-1(WT)HIV-1(MDR)HIV-1(M184V)0.068nM(EC50)0.15nM(EC50)3.1nM(EC50)体外研究Islatravir(MK-8591)(4'Ed2FA)isapotentanti-HIV-1agent,actingasanucleosidereversetranscriptaseinhibitor,withEC50sof0.068nM,3.1nMand0.15nMforHIV-1(WT),HIV-1(M184V),HIV-1(MDR),respectively[1].REFERENCES[1].OhruiH,etal.2'-deoxy-4'-C-ethynyl-2-fluoroadenosine,anucleosidereversetranscriptaseinhibitor,ishighlypotentagainstallhumanimmunodeficiencyvirusestype1andhaslowtoxicity.ChemRec.2006;6(3):133-43.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch