Cabotegravir-sodium-GSK-1265744-sodium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECabotegravirsodiumCat.No.:HY-15592ACASNo.:1051375-13-3Synonyms:GSK-1265744sodium;S/GSK1265744sodium分⼦式:C₁₉H₁₆F₂N₃NaO₅分⼦量:427.33作⽤靶点:HIV;HIVIntegrase作⽤通路:Anti-infection;MetabolicEnzyme/Protease储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:6.9mg/mL(16.15mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3401mL11.7006mL23.4011mL5mM0.4680mL2.3401mL4.6802mL10mM0.2340mL1.1701mL2.3401mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性Cabotegravir(GSK-1265744)sodium⼀种具有⼝服活性且长效的HIV整合酶(HIVintegrase)链转移抑制剂，也有机离⼦转运蛋⽩1/3(OAT1/OAT3)抑制剂，对HIVADA、OAT3和OAT1的IC50分别为2.5nM、0.41μM和0.81μM。Cabotegravirsodium主由尿苷⼆磷酸葡萄糖醛酸转移酶(UGT)1A1代谢，与其他抗逆转录病毒药物(ARVs)相互作⽤的可能性较低。Cabotegravirsodium可⽤于艾滋病(AIDS)的研究。1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetIC50:2.5nM(HIVADA)[1]IC50:0.41μM(OAT3),0.81μM(OAT1)[2]体外研究Cabotegravir(GSK-1265744)inhibitstheHIV-1integrasecatalyzedstrandtransferreactionwithanIC50of3.0nMinvitro.TheantiviralEC50againstHIV-1Ba-Lis0.22nMandthatagainstNL432is0.34nMinPBMCs,0.57nMusingCellTiter-Gloand1.3nMusingMTTinMT-4,and0.5nMinthePHIVassay,whichusesapseudotypedself-inactivatingvirus[3].CellViabilityAssay[3]CellLine:MT-4cellsConcentration:0-32nMIncubationTime:4or5daysResult:ShowedantiviralactivitywithanEC50of1.3nM.体内研究Thehalf-lifeofCabotegravirisupto54daysinmice[1].Cabotegravir(25or50mg/kg;i.v.;singledoseortwice)protectsMacaquesagainstintravenouschallengewithSIVmac251[4].户使⽤本产品发表的科研⽂献•IntJAntimicrobAgents.2019Dec;54(6):814-819.•JInfectDis.2022Sep19;jiac386.•Pharmaceutics.2022,14(9),1761.•AntimicrobAgentsChemother.2019Dec20;64(1):e01717-19.•DrugMetabDispos.2019May;47(5):535-544.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhouT,etal.Creationofananoformulatedcabotegravirprodrugwithimprovedantiretroviralprofiles.Biomaterials.2018Jan;151:53-65.[2].ReeseMJ,etal.DruginteractionprofileoftheHIVintegraseinhibitorcabotegravir:assessmentfrominvitrostudiesandaclinicalinvestigationwithmidazolam.Xenobiotica.2016;46(5):445-56.[3].YoshinagaT,etal.AntiviralcharacteristicsofGSK1265744,anHIVintegraseinhibitordosedorallyorbylong-actinginjection.AntimicrobAgentsChemother.2015Jan;59(1):397-406.[4].AndrewsCD,etal.CabotegravirlongactinginjectionprotectsmacaquesagainstintravenouschallengewithSIVmac251.AIDS.2017Feb20;31(4):461-467.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform