Rilematovir-JNJ-678-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERilematovirCat.No.:HY-112180CASNo.:1383450-81-4Synonyms:JNJ-678;JNJ-53718678分?式:C??H??ClF?N?O?S分?量:500.92作?靶點(diǎn):RSV作?通路:Anti-infection儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:65mg/mL(129.76mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9963mL9.9816mL19.9633mL5mM0.3993mL1.9963mL3.9927mL10mM0.1996mL0.9982mL1.9963mL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。-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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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:≥2.17mg/mL(4.33mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.17mg/mL(4.33mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(4.33mM);ClearsolutionBIOLOGICALACTIVITY?物活性Rilematovir(JNJ-678)新型融合蛋?(fusionprotein)抑制劑，有潛??于呼吸道合胞病毒(RSV)的研究。IC50&TargetFusionprotein[1]體外研究Rilematovirisasmall-moleculerespiratorysyncytialvirus(RSV)fusioninhibitorcurrentlyunderclinicalevaluationininfantshospitalizedforRSVinfection.RilematovirbindstoRSVFproteininitsprefusionconformation.Rilematovirdisplaysverypotentantiviralactivityandlowcytotoxicity.InadditiontoitsactivityagainsttheRSVA2strain,RilematovirisalsohighlyactiveagainstanumberofRSVstrainsfrombothAandBsubtypes.TheEC50inanRSVinfectionassayusingHeLacellsis460?pM[1].體內(nèi)研究OraltreatmentofneonatallambswithRilematovir,orwithanequallyactivecloseanalog,efficientlyinhibitsestablishedacutelowerrespiratorytractinfectionintheanimals,evenwhentreatmentisdelayeduntilexternalsignsofrespiratorysyncytialvirusillnesshavebecomevisible[1].PROTOCOLCellAssay[1]TheantiviralactivityofJNJ-678(JNJ-53718678)againsthMPVisevaluatedusingacellularinfectiousassayin96-wellplatesinwhichVero/TMPRSS2cellsareinfectedwithrecombinanthMPV65.CellsaretreatedwithdifferentconcentrationsofJNJ-678(JNJ-53718678)andtheninfectedwithrecombinanthMPV(1×104PFUperwell).Threedayspost-virusexposure,viralreplicationisquantifiedbymeasuringfluorescenceandtheEC50iscalculated[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats[1]Administration[1]Cottonratsreceiveeitherasingledoseat24?hafterviralinfectionoronce-dailydosesof40?mg/kgJNJ-678(JNJ-53718678)byoralgavage,at24,48,and72?hafterviralinfection.Thedecreaseofviralreplicationinallexperimentsiscomparedtochallengedanimalsthatreceivedonlythevehicle[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ACSNano.2021Jul22.?JVirol.2021Aug11;JVI0120521.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].RoymansD,etal.Therapeuticefficacyofarespiratorysyncytialvirusfusioninhibitor.NatCommun.2017Aug1;8(1):167.McePdfHeightCaution:Producthasnot