Daclatasvir-dihydrochloride-BMS-790052-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDaclatasvirdihydrochlorideCat.No.:HY-10465CASNo.:1009119-65-6Synonyms:BMS-790052dihydrochloride;EBP883dihydrochloride分⼦式:C₄₀H₅₂Cl₂N₈O₆分⼦量:811.8作⽤靶点:HCV作⽤通路:Anti-infection储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥56mg/mL(68.98mM)H2O:50mg/mL(61.59mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.2318mL6.1592mL12.3183mL5mM0.2464mL1.2318mL2.4637mL10mM0.1232mL0.6159mL1.2318mL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(sealedstorage,awayfrommoisture)。-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)1/3MasterofBioactiveMolecules—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:≥1mg/mL(1.23mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(1.23mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1mg/mL(1.23mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Daclatasvirdihydrochloride(BMS-790052dihydrochloride)⼀种有效的具有⼝服活性的HCVNS5A蛋⽩抑制剂，多种HCV复制⼦因型的EC50范为9-146pM。Daclatasvirdihydrochloride也有机离⼦转运多肽1B(OATP1B)和OATP1B3抑制剂，IC50分别为1.5µM和3.27µM。IC50&TargetEC50:50pM(HCVreplicongenotype1a),9ꢀpM(HCVreplicongenotype1b),71pM(HCVreplicongenotype2a),146pM(HCVreplicongenotype3a),12pM(HCVreplicongenotype4a)and33pM(HCVreplicongenotype5a)[1]Kd:8nM(NS5A33-202)and210nM(NS5A26-202)[2]IC50:1.5µM(OATP1B)and3.27µM(OATP1B3)[3]体外研究Daclatasvir(BMS-790052)demonstratespotentinhibitoryactivitytowardsallgenotypestested,withEC50valuesrangingfrom9pMto146ꢀpM.DaclatasvirinhibitsHCVreplicongenotype1a,1b,2a,3a,4aand5awithEC50valuesof50pM,9ꢀpM,71pM,146pM,12pMand33pM,respectively.DaclatasvirisapotentinhibitoroftheJFH-1genotype2ainfectiousvirusthatreplicatesincellculture(EC50=28pM)[1].Daclatasvir(BMS-790052)bindstightlytoNS5A33-202andNS5A26-202withKdsof8nMand210nM,respectively[2].体内研究Daclatasvir(BMS-790052;30ꢀmg/kg;oraladministration;daily;for27days)treatmentreducesserumHCVRNAtitersveryrapidlyby~1.5log10atday3[4].AnimalModel:NOD/SCIDmalemice(5weeksofage,18-20ꢀg)bearingHCVRNA-transfectedcells[4]Dosage:30ꢀmg/kgAdministration:Oraladministration;daily;for27daysResult:ReducedserumHCVRNAtitersveryrapidlyby~1.5log10atday3.户使⽤本产品发表的科研⽂献•Hepatology.2019May;69(5):1861-1872.•IntJAntimicrobAgents.2015Oct;46(4):381-8.•AntiviralRes.2020May;177:104734.•AntiviralRes.2017Dec;148:5-14.•AntiviralRes.2017Oct;146:191-200.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].MinGao,etal.ChemicalgeneticsstrategyidentifiesanHCVNS5Ainhibitorwithapotentclinicaleffect.Nature.2010May6;465(7294):96-100.[2].DavidBAscher,etal.PotenthepatitisCinhibitorsbinddirectlytoNS5AandreduceitsaffinityforRNA.SciRep.2014Apr23;4:4765.[3].TomomiFurihata,etal.Differentinteractionprofilesofdirect-actinganti-hepatitisCvirusagentswithhumanorganicaniontransportingpolypeptides.AntimicrobAgentsChemother.2014Aug;58(8):4555-64.[4].Seung-HoonLee,etal.HA1077displayssynergisticactivitywithdaclatasviragainsthepatitisCvirusandsuppressestheemergenceofNS5Aresistance-associatedsubstitutionsinmice.SciRep.2018Aug20;8(1):12469.McePdfHeightCa