GS-443902-GS-441524-triphosphate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGS-443902Cat.No.:HY-126303CASNo.:1355149-45-9Synonyms:GS-441524triphosphate;Remdesivirmetabolite分?式:C??H??N?O??P?分?量:531.2作?靶點(diǎn):DNA/RNASynthesis;SARS-CoV;RSV;HCV;DrugMetabolite作?通路:CellCycle/DNADamage;Anti-infection;MetabolicEnzyme/Protease儲(chǔ)存?式:-20°C,storedundernitrogen*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:100mg/mL(188.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8825mL9.4127mL18.8253mL5mM0.3765mL1.8825mL3.7651mL10mM0.1883mL0.9413mL1.8825mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.BIOLOGICALACTIVITY?物活性GS-443902(GS-441524triphosphate)?種有效的病毒RNA依賴的RNA聚合酶(RdRp)抑制劑，對(duì)RSVRdRp和HCVRdRp的IC50分別為1.1μM和5μM。GS-443902Remdesivir的活性三磷酸鹽代謝產(chǎn)物。IC50&TargetIC50:1.1μM(RSVRdRp)and5μM(HCVRdRp)[1][2]體外研究Inacontinuous72hincubationof1μMRemdesivir(GS-5734),theGS-443902(GS-441524triphosphate;1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemERemdesivirmetabolite;compound4tp)levelismeasuredat2,24,48and72h,andreachesaCmaxof300,110,and90pmol/millioncellsinmacrophages,HMVEC,andHeLacellslinesrespectively[1].GS-443902(compound8a)isatriphosphates(TP)derivative[2].GS-443902(NTP;0.01,0.1,1,10,100μM)inhibitsRSVRdRp-catalysedRNAsynthesisbyincorporatingintothenascentviralRNAtranscriptandcausingitsprematuretermination.GS-5734selectivelyinhibitsEBOVreplicationbytargetingitsRdRpandinhibitingviralRNAsynthesisfollowingefficientintracellularconversiontoGS-443902[3].體內(nèi)研究Remdesivir(GS-5734;10?mg?kg;i.v.)rapidlydistributesintoperipheralbloodmononuclearcells(PBMCs),andefficientconversiontoGS-443902(GS-441524triphosphate;Remdesivirmetabolite;NTP)isapparentwithin2?hofdoseadministrationinrhesusmonkeys.InPBMCs,GS-443902representsthepredominantmetaboliteandispersistentwithat1/2of14?handlevelsrequiredfor>50%virusinhibitionfor24?hours[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Cell.2022Nov10;185(23):4347-4360.e17.?NatCommun.2021Oct4;12(1):5811.?ActaPharmSinB.2021Mar22.?IntJMolSci.2022,23(15),8302.?ChemBiolInteract.2021Apr19;109480.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SiegelD,etal.DiscoveryandSynthesisofaPhosphoramidateProdrugofaPyrrolo[2,1-f][triazin-4-amino]AdenineC-Nucleoside(GS-5734)fortheTreatmentofEbolaandEmergingViruses.MedChem.2017Mar9;60(5):1648-1661.[2].ChoA,etal.Synthesisandantiviralactivityofaseriesof1'-substituted4-aza-7,9-dideazaadenosineC-nucleosides.BioorgMedChemLett.2012Apr15;22(8):2705-7.[3].WarrenTK,etal.TherapeuticefficacyofthesmallmoleculeGS-5734againstEbolavirusinrhesusmonkeys.Nature.2016Mar17;531(7594):381-5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi