Tecovirimat-monohydrate-ST-246-monohydrate-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemETecovirimatmonohydrateCat.No.:HY-14805ACASNo.:1162664-19-8Synonyms:ST-246monohydrate分子式:C₁₉H₁₇F₃N₂O₄分子量:394.34作用靶点:Orthopoxvirus;Arenavirus作用通路:Anti-infection储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Tecovirimat(ST-246)monohydrate是Tecovirimat(HY-14805)的一水合物形式。Tecovirimatmonohydrate是具有口服活性和选择性的抗正痘病毒化合物(包括牛痘、猴痘、骆驼痘、牛痘、鼠痘、天花和天花病毒)。Tecovirimatmonohydrate对牛痘，牛痘病毒，羊痘病毒的EC50值分别为0.01μM，0.48μM和0.05μM。Tecovirimatmonohydrate靶向正痘病毒蛋白VP37，该蛋白是细胞内成熟病毒颗粒膜包膜形成包膜病毒所必需的。Tecovirimatmonohydrate对牛痘病毒V061基因发挥抗病毒活性，该基因与牛痘病毒F13L同源，编码细胞外病毒产生所需的主要包膜蛋白(p37)。Tecovirimatmonohydrate可用于正痘病毒诱导疾病的研究[1][2][3][4][5]。体外研究Tecovirimatmonohydrate(0-50μM,3days)isapotentandspecificinhibitoroforthopoxvirusreplicationthatisactiveagainstabroadspectrumoforthopoxviruses[1].CellCytotoxicityAssay[1]CellLine:VerocellsConcentration:0-50μMIncubationTime:3daysResult:WasmorepotentrelativetoCidofovir(CDV)(HY-17438)aftervacciniavirusstrainNYCBHinfectionincytopathiceffect(CPE)-basedassaysinverocells.体内研究Tecovirimatmonohydrate(50mg/kg,oralgavage,twiceadayfor14days)mountsaprotectiveimmune1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEresponsetovacciniavirusinfectioninalethalintranasalvacciniaviruschallengemodelofmice[1].Tecovirimatmonohydrate(50mg/kg,oralgavage,5days)caninhibitvacciniavirus-inducedlesionformationfollowingi.v.viralinoculationinVacciniavirus-mousetaillesionmodel[1].Tecovirimatmonohydrate(100mg/kg,p.o.,dailyforvariousdurationsof5,7,10,or14days)significantlydecreasesinmortalityofcowpoxvirus(CV)-infectedmice[2].PharmacokineticparametersofST-246inmice[1]药代动力学分析[1]Dosage(mg/kg)Tmax(h)Cmax(μg/mL)AUC0-t(μg·h/mL)T1/2(h)302.732.5284.22.51001.062.2287.62.5AnimalModel:WeanlingBALB/cmicechallengedwithvacciniavirusstrain(4to6weeksofageandweighing15to20g)[1]Dosage:50mg/kgAdministration:oralgavage,twiceadayfor14daysResult:Tecovirimatmonohydrate-treatedmicemountedaprotectiveimmuneresponsetovacciniavirusinfectioninalethalintranasalvacciniaviruschallengemodel.AnimalModel:NMRImiceinoculatedviathetailveinwithvacciniavirus(4to6weeksofageandweighing15to20g)[1]Dosage:50mg/kgAdministration:oralgavage,5daysResult:Showedadose-dependentreductioninthenumbersoftaillesionsatday8postinfectionrelativetoplacebo-treatedcontrolanimalsinmice.REFERENCESTYAVANAGIMATTSR,etal.,Rehydrationofmicronizedtecovirimatmonohydrate.WO2015077143.YangG,etal.Anorallybioavailableantipoxviruscompound(ST-246)inhibitsextracellularvirusformationandprotectsmicefromlethalorthopoxvirusChallenge[J].JVirol.2005Oct;79(20):13139-49.QuenelleDC,etal.EfficacyofdelayedtreatmentwithST-246givenorallyagainstsystemicorthopoxvirusinfectionsinmice[J].AntimicrobAgentsChemother.2007Feb;51(2):689-95.RussoAT,etal.AnoverviewofTecovirimatmonohydrateforsmallpoxtreatmentandexpandedanti-orthopoxvirusapplications[J].ExpertRevAntiInfectTher.2021Mar;19(3):331-344.DeLaurentisCE,etal.NewPerspectivesonAntimicrobialAgents:TecovirimatmonohydrateforTreatmentofHumanMonkeypoxVirus[J].AntimicrobAgentsChemother.2022Dec20;66(12):e0122622.AlmehmadiM,etal.AGlanceattheDevelopmentandPatentLiteratureofTecovirimatmonohydrate:TheFirst-in-ClassTherapyforEmergingMonkeypoxOutbreak[J].Viruses.2022Aug25;14(9):1870.McePdfHeight2/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECaution:Pro