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

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEGS-443902trisodiumCat.No.:HY-126303CCASNo.:1355050-21-3Synonyms:GS-441524triphosphatetrisodium;Remdesivirmetabolitetrisodium分?式:C??H??N?Na?O??P?分?量:597.15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,protectfromlight,storedunderargon*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedunderargon)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:300mg/mL(502.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6746mL8.3731mL16.7462mL5mM0.3349mL1.6746mL3.3492mL10mM0.1675mL0.8373mL1.6746mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。BIOLOGICALACTIVITY?物活性GS-443902trisodium(GS-441524triphosphatetrisodium)?種有效的病毒RNA依賴(lài)的RNA聚合酶(RdRp)抑制劑，對(duì)RSVRdRp和HCVRdRp的IC50分別為1.1μM和5μM。GS-443902trisodium是Remdesivir(GS-5734)的活性三磷酸鹽代謝產(chǎn)物。IC50&TargetIC50:1.1μM(RSVRdRp)and5μM(HCVRdRp)[1][2]1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體外研究Inacontinuous72hincubationof1μMRemdesivir(GS-5734),theGS-443902trisodium(GS-441524triphosphatetrisodium;Remdesivirmetabolitetrisodium)levelismeasuredat2,24,48and72h,andreachesaCmaxof300,110,and90pmol/millioncellsinmacrophages,HMVEC,andHeLacellslinesrespectively[1].GS-443902trisodium(compound8a)isatriphosphates(TP)derivative[2].GS-443902trisodium(NTP;0.01,0.1,1,10,100μM)inhibitsRSVRdRp-catalysedRNAsynthesisbyincorporatingintothenascentviralRNAtranscriptandcausingitsprematuretermination.GS-5734selectivelyinhibitsEBOVreplicationbytargetingitsRdRpandinhibitingviralRNAsynthesisfollowingefficientintracellularconversiontoGS-443902sodium[3].體內(nèi)研究Remdesivir(GS-5734;10?mg?kg;i.v.)rapidlydistributesintoperipheralbloodmononuclearcells(PBMCs),andefficientconversiontoGS-443902trisodium(Remdesivirmetabolitetrisodium;NTP)isapparentwithin2?hofdoseadministrationinrhesusmonkeys.InPBMCs,GS-443902trisodiumrepresentsthepredominantmetaboliteandispersistentwithat1/2of14?handlevelsrequiredfor>50%virusinhibitionfor24?hours[3].REFERENCES[1].WarrenTK,etal.TherapeuticefficacyofthesmallmoleculeGS-5734againstEbolavirusinrhesusmonkeys.Nature.2016Mar17;531(7594):381-5.[2].SiegelD,etal.DiscoveryandSynthesisofaPhosphoramidateProdrugofaPyrrolo[2,1-f][triazin-4-amino]AdenineC-Nucleoside(GS-5734)fortheTreatmentofEbolaandEmergingViruses.MedChem.2017Mar9;60(5):1648-1661.[3].ChoA,etal.Synthesisandantiviralactivityofaseriesof1'-substituted4-aza-7,9-dideazaadenosineC-nucleosides.BioorgMedChemLett.2012Apr15;22(8):2705-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed