Inarigivir-soproxil-SB9200-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEInarigivirsoproxilCat.No.:HY-109035CASNo.:942123-43-5Synonyms:SB9200;GS-9992分?式:C??H??N?O??PS分?量:703.62作?靶點(diǎn):HCV;HBV作?通路:Anti-infection儲(chǔ)存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:80mg/mL(113.70mM;Needultrasonic)H2O:10mg/mL(14.21mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4212mL7.1061mL14.2122mL5mM0.2842mL1.4212mL2.8424mL10mM0.1421mL0.7106mL1.4212mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥4mg/mL(5.68mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4mg/mL(5.68mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(7.11mM);Clearsolution4.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(3.55mM);ClearsolutionBIOLOGICALACTIVITY?物活性Inarigivirsoproxil(SB9200)?種先天免疫激動(dòng)劑，對(duì)耐藥HCV變異體具有有效的抗病毒活性，在因型1HCV復(fù)制?系統(tǒng)的細(xì)胞中，對(duì)HCV1a/1b的EC50分別為2.2和1.0μM。InarigivirsoproxilSB9000的?服?物可利?前藥。Inarigivirsoproxil對(duì)RNA病毒具有?譜抗病毒活性，包括HCV、諾如病毒、呼吸道合胞病毒以及流感和HBV[1][2]。IC50&TargetEC50:2.2/1.0μM(HCV1a/1b)[1].體外研究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].體內(nèi)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?邊的抑制劑?師www.MedChemEweremorepronouncedinGroup2.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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