AT-130-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAT-130Cat.No.:HY-100028CASNo.:211364-06-6分⼦式:C₂₂H₂₂BrN₃O₅分⼦量:488.33作⽤靶点:HBV;DNA/RNASynthesis作⽤通路:Anti-infection;CellCycle/DNADamage储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(51.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0478mL10.2390mL20.4780mL5mM0.4096mL2.0478mL4.0956mL10mM0.2048mL1.0239mL2.0478mL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。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.12mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性AT-130⼀种苯丙烯酰胺衍⽣物，⼀种有效的⼄型肝炎病毒(HBV)复制的⾮核苷抑制剂。AT-130抑制病毒DNA的合成，EC50为0.13μM。AT-130可以抑制野⽣型和突变型HBV。AT-130在肝癌细胞中具有抗HBV活性。体外研究AT-130inhibitsWtHBV(IC50=2.4μM),rtL180MHBV(IC50=9.8μM),rtM204IHBV(IC50=35.6μM)[1].AT-130(0.1,1,5,10,100μM;for7days)causesdose-dependentinhibitionofwtHBVreplicationinHepG2cellstransducedwithHBVbaculovirus.AT-130ataconcentrationof2.5μM,reducesencapsidatedHBVDNAby50%(IC50)andat18.5μMby90%(IC90)[1].AT-130hasnotoxictoeitherHepG2orHuh-7cellsatconcentrationsofupto250μM[1].AT-130(0.005,0.05,0.5,5,50μM)doesnotinhibitHBVDNAsynthesisbyblockingtheHBVendogenousDNApolymerasereactiondirectlyinHuh7orHepG2cells.AT-130inhibitsHBVDNAreplicationinhepatomacellsbuthasnoeffectonviralDNApolymeraseactivityorcoreproteintranslation[3].AT-130(2.5,18.5μM)hasnoeffectontotalHBVRNAproductionbutdoesreduceencapsidatedRNA.AT-130doesnotaffectcoreproteinornucleocapsidproductionandtheactivityoftheproteinexpressionvector[3].REFERENCES[1].WilliamEDelaney4th,etal.PhenylpropenamidederivativesAT-61andAT-130inhibitreplicationofwild-typeandlamivudine-resistantstrainsofhepatitisBvirusinvitro.AntimicrobAgentsChemother.2002Sep;46(9):3057-60.[2].RBPerni,etal.PhenylpropenamidederivativesasinhibitorsofhepatitisBvirusreplication.BioorgMedChemLett.2000Dec4;10(23):2687-90.[3].JJFeld,etal.ThephenylpropenamidederivativeAT-130blocksHBVreplicationatthelevelofviralRNApackaging.AntiviralRes.2007Nov;76(2):168-77.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio