Laninamivir-octanoate-CS-8958-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELaninamiviroctanoateCat.No.:HY-14818ACASNo.:203120-46-1Synonyms:CS-8958分?式:C??H??N?O?分?量:472.53作?靶點(diǎn):InfluenzaVirus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:100mg/mL(211.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1163mL10.5813mL21.1627mL5mM0.4233mL2.1163mL4.2325mL10mM0.2116mL1.0581mL2.1163mL請根據(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?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.29mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.29mM);ClearsolutionBIOLOGICALACTIVITY?物活性Laninamiviroctanoate(CS-8958)，Laninamivir的前藥，?種長效的神經(jīng)氨酸酶(neuraminidase,NA)抑制劑，具有抗流感病毒活性。Laninamiviroctanoate對耐Oseltamivir的病毒以及對?流?性流感病毒均具有抗流感活性。體外研究Laninamiviroctanoate(CS-8958)showsinhibitoryactivitywithanIC50of631-1170nM,39.2-221nMand128nMtotheH1N1virusesstrains,H3N2virusesstrainsandH2N2(A/Singapore/1/57)virus,respectively[1].體內(nèi)研究Laninamiviroctanoate(CS-8958;95μg/kg;intranasaladministration;threedose;at4hbeforeand4hand17hpostinfection)treatmentshowssignificantlylife-prolongingeffectininfectedmodel[1].AnimalModel:FemaleBALB/cmice(5-6weeksold)infectedwithinfluenzaAvirusA/PR/8/34[1]Dosage:0.2μmol/kg(95μg/kg)Administration:Intranasaladministration;threedose;at4hbeforeand4hand17hpostinfectionResult:Showedlife-prolongingeffectininfectedmodel.REFERENCES[1].MakotoYamashita,etal.CS-8958,aprodrugofthenewneuraminidaseinhibitorR-125489,showslong-actinganti-influenzavirusactivity.AntimicrobAgentsChemother.2009Jan;53(1):186-92.[2].HideyukiIkematsu,etal.Laninamiviroctanoate:anewlong-actingneuraminidaseinhibitorforthetreatmentofinfluenza.ExpertRevAntiInfectTher.2011Oct;9(10):851-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc