Baloxavir-Baloxavir-acid-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBaloxavirCat.No.:HY-109025ACASNo.:1985605-59-1Synonyms:Baloxaviracid;S-033447分?式:C??H??F?N?O?S分?量:483.49作?靶點(diǎn):InfluenzaVirus作?通路:Anti-infection儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:41.67mg/mL(86.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0683mL10.3415mL20.6830mL5mM0.4137mL2.0683mL4.1366mL10mM0.2068mL1.0341mL2.0683mL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(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%salineSolubility:≥2.08mg/mL(4.30mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.30mM);ClearsolutionBIOLOGICALACTIVITY?物活性Baloxavir(Baloxaviracid)，衍??前藥Baloxavirmarboxil，甲型和?型流感病毒聚合酶PA亞內(nèi)的?種?創(chuàng)，有效且選擇性的帽依賴性核酸內(nèi)切酶(CEN)抑制劑。Baloxavir抑制病毒RNA的轉(zhuǎn)錄和復(fù)制，并具有強(qiáng)?的抗病毒活性[1][2]。IC50&TargetInfluenzavirus[1]Cap-dependentendonuclease(CEN)[1][2]體外研究ThemedianEC50valuesatbaselineforBaloxavir(BXA)are17.96nMforA/H1N1pdm,4.48nMforA/H3N2,and18.67nMfortypeBvirus[1].Baloxavir(BXA)inhibitsviralRNAtranscriptionviaselectiveinhibitionofcap-dependentendonuclease(CEN)activityinenzymaticassays,andinhibitsviralreplicationininfectedcellswithoutcytotoxicityincytopathiceffectassays.BaloxavirshowsbroadpotencyagainstvarioussubtypesofinfluenzaAviruses(H1N2,H5N1,H5N2,H5N6,H7N9andH9N2).Additionally,serialpassagesofthevirusesinthepresenceofBaloxavirresultinisolationofPA/I38TvariantswithreducedBXAsusceptibility[2].Baloxavir(BXA)inhibitscap-dependentendonuclease(CEN)andCEN/RdRpactivitieswithIC50valuesof2.5nMand1.6nM,respectively,whilelowpotency(IC50>40nM)isobservedagainstRdRpactivity[2].Baloxavir(BXA)hasahighinhibitorypotencyagainstCENactivityofthetestedviralribonucleoproteincomplexes(vRNPs)frominfluenzaAandBviruseswithmeanIC50valuesof1.4-3.1nMand4.5-8.9nM,respectively,indicatingthatBaloxavirhasbroadspectrumactivities.BaloxavirshowshighpotencyagainstinfluenzaAandBviruseswithmeanEC90of0.46-0.98nMand2.2-3.4nM,respectively[2].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatMicrobiol.2020Jan;5(1):27-33.?NatCommun.2020Jan9;11(1):164.?ProcNatlAcadSciUSA.2020Apr14;117(15):8593-8601.?PLoSPathog.2022Jul13;18(7):e1010698.?JVirol.2020Oct27;94(22):e00319-20.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].OmotoS,etal.Characterizationofinfluenzavirusvariantsinducedbytreatmentwiththeendonucleaseinhibitorbaloxavirmarboxil.SciRep.2018Jun25;8(1):9633.[2].NoshiT,etal.Invitrocharacterizationofbaloxaviracid,afirst-in-classcap-dependentendonucleaseinhibitoroftheinfluenzaviruspolymerasePAsubunit.AntiviralRes.2018Dec;160:109-117.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeen