Inarigivir-soproxil-SB9200-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEInarigivirsoproxilCat.No.:HY-109035CASNo.:942123-43-5Synonyms:SB9200;GS-9992分⼦式:C₂₅H₃₄N₇O₁₃PS分⼦量:703.62作⽤靶点:HCV;HBV作⽤通路:Anti-infection储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:80mg/mL(113.70mM;Needultrasonic)H2O:10mg/mL(14.21mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4212mL7.1061mL14.2122mL5mM0.2842mL1.4212mL2.8424mL10mM0.1421mL0.7106mL1.4212mL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,storedundernitrogen)。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥4mg/mL(5.68mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4mg/mL(5.68mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(7.11mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(3.55mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Inarigivirsoproxil(SB9200)⼀种先天免疫激动剂，对耐药HCV变异体具有有效的抗病毒活性，在因型1HCV复制⼦系统的细胞中，对HCV1a/1b的EC50分别为2.2和1.0μM。InarigivirsoproxilSB9000的⼝服⽣物可利⽤前药。Inarigivirsoproxil对RNA病毒具有⼴谱抗病毒活性，包括HCV、诺如病毒、呼吸道合胞病毒以及流感和HBV[1][2]。IC50&TargetEC50:2.2/1.0μM(HCV1a/1b)[1].体外研究Inarigivirsoproxil(SB9200)isafirst-in-classoralmodulatorofinnateimmunitythatactsviatheactivationoftheRIG-IandNOD2pathways[1].InarigivirsoproxilisaneffectiveinhibitorofHCVreplicationincellculture.TheantiviralactivityofInarigivirsoproxilagainstHCVwasassessedusinggenotype1HCVrepliconsystemsinduplicateexperimentsusing4drugconcentrations.InarigivirsoproxilinhibitsHCVreplicationwithEC50sof2.2and1.0µM,andEC90sof8.0and6.0µMforgenotype1Aand1B,respectively[1].Inarigivirsoproxil(SB9200),anorallybioavailabledinucleotide,activatestheviralsensorproteins,retinoicacid-induciblegene1(RIG-I)andnucleotide-bindingoligomerizationdomain-containingprotein2(NOD2)causingtheinductionoftheinterferon(IFN)signalingcascadeforantiviraldefense[2].体内研究TheinductionofhostimmuneresponsesbypretreatmentwithInarigivirsoproxil(SB9200)followedbyEntecavir(ETV)resultedinantiviralefficacythatwassuperiortothatobtainedusingthestrategyofviralreductionwithETVfollowedbyimmunomodulation[2].SequentialtreatmentofchronicWHVcarrierwoodchuckswithInarigivirsoproxil(30mg/kg)followedbyETVinducedmarkedsuppressionofserumviremiaandantigenemiaanddelayedrecrudescenceofviralreplicationcomparedtosequentialtreatmentwithETVfollowedbyInarigivirsoproxil[2].AnimalModel:Woodchuckschronicallyinfectedwithwoodchuckhepatitisvirus(WHV)[2]Dosage:30mg/kgAdministration:Orallytreatedoncedaily;group1receivedETVfor4weeksfollowedbyInarigivirsoproxilfor12weeks.Group2receivedInarigivirsoproxilfor12weeksfollowedbyETVfor4weeksResult:BothgroupsdemonstratedmarkedreductionsinhepaticWHVnucleicacidlevelswhich2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEweremorepronouncedinGroup2.户使⽤本产品发表的科研⽂献•IntJOncol.August19,2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MeleriJones,etal.SB9200,anovelagonistofinnateimmunity,showspotentantiviralactivityagainstresistantHCVvariants.JMedVirol.2017Sep;89(9):1620-1628.[2].ManasaSuresh,etal.AntiviralEfficacyandHostImmuneResponseInductionduringSequentialTreatmentwithSB9200FollowedbyEntecavirinWoodchucks.PLoSOne.2017Jan5;12(1):e0169631.MceP