CAB7-3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECAB7-3Cat.No.:HY-180524CASNo.:3014372-17-6分⼦式:C₂₈H₂₈BBrFN₅O₅S分⼦量:656.33作⽤靶点:HBV作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CAB7-3⼀种⼝服有效的HBV⾐组装调节剂。CAB7-3表现出卓越的抗病毒效⼒，其抑制HBVDNAEC50为70nM，CC50为32.3μM。CAB7-3在多种细胞模型中均显⽰出显著的抗HBV活性，其在HBV整合的HepDES19细胞、四环素诱导的HepAD38细胞以及HBV感染的HLCZ01细胞中的EC50值分别为70μM、1nM和2nM。CAB7-3在体内能有效降低肝脏HBV核⼼蛋⽩⽔平并抑制病毒复制。CAB7-3现出良好的类药性和安全性，可⽤于⼄型肝炎病毒研究[1]。体外研究CAB7-3(0.001-1μM,6days)showsanantiviralactivityinHepAD38cellswithEC50=1nM,CC50=26.54μM,SI=26540;inHepDES19cellswithEC50=7nM,CC50=32μM,SI=481;inHBV-infectedHLCZ01cellswithEC50=2nM,CC50=30.73μM,SI=15365[1].CAB7-3(0.0003-1μM,6days)blocksnewcccDNAformationwhileleavingHBsAgsecretionfrompre-existingcccDNAunaffectedinHepAD38andHLCZ01cells[1].CAB7-3(0.006-4μM,3days)inducesHBVCpdegradationanddisruptscapsidassemblyinHepG2cells[1].CAB7-3(1mgin1mLDMSOand0.5mgin0.5mLDMSO)showswatersolubility(257.42μg/mL,pH2.0;2.57μg/mL,pH7.0;4.14μg/mL,pH7.4)[1].CAB7-3(1μM,0-60min)showsT1/2=169min,CLint(mic)=8.2μL/min/mg,CLint(liver)=7.4mL/min/kgandRemaining(T=60min)=78.0%inhumanmicrosomesCAB7-3(10μM,)notinduceCYP3A4inprimaryhumanhepatocytes(PHHs)[1].CAB7-3(0.3-100μM)exhibitssignificantlylowinhibitoryratesonthehERGchannelinHEK293cellswithhERGinhibition=3.52,14.59,31.84,61.05,83.05,94.76%atconcentrationof0.3,1,3,10,30and100μM[1].ELISAAssay[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:HepAD38andHLCZ01cellsConcentration:0.0003,0.001,0.003,0.1,0.03,0.1and0.3μMIncubationTime:6daysResult:HadminimalimpactontheproductionofHBsAginbothHepAD38cellsandHLCZ01cells.WesternBlotAnalysis[1]CellLine:HepG2cellsConcentration:0.06,0.13,0.25,0.5,1.0,2.0,4.0μMIncubationTime:3daysResult:ReducedintracellularCpexpressioninadose-dependentmanner.体内研究CAB7-3(15mg/kg,p.o.,oncedailyfor18days)inhibitsthesecretionofviralDNAcontainingparticlesbyrepressingHBVcapsidassemblyintheHBVcarriermousemodel[1].AnimalModel:pAAVHBV1.2plasmid(6μg,hydrodynamicinjection)induced-maleC57BL/6J(6weeks)[1]Dosage:15mg/kgAdministration:p.o.,oncedailyfor18daysResult:SignificantlyreducedserumHBVDNAlevelsfromthevehiclebaselineof1.02×105IU/mLto1.06×104IU/mL.Displayedenhancedanti-HBVactivity,reducinghepaticHBcAgexpressiondespitenotnoticeablyaffectingserumHBsAgexpression.ShowednosignificantchangeintheSerumALTandASTlevels,aswellasHEstainingoflivertissue.REFERENCES[1].JinY,etal.Design,Synthesis,andBiologicalEvaluationofHighlyPotentBoronicAcid(BoronateEster)-BearingHeteroaryldihydropyrimidineDerivativesasHBVCapsidAssemblyModulators.JMedChem.2025Dec25;68(24):25939-25960.McePdfHeightCaution:Producthasnotbeenfullyvalidate