Gardiquimod-diTFA-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGardiquimoddiTFACat.No.:HY-103697ACASNo.:1159840-61-5分⼦式:C₂₁H₂₅F₆N₅O₅分⼦量:541.44作⽤靶点:Toll-likeReceptor(TLR);HIV作⽤通路:Immunology/Inflammation;Anti-infection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:50mg/mL(92.35mM;Needultrasonic)H2O:25mg/mL(46.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8469mL9.2346mL18.4693mL5mM0.3694mL1.8469mL3.6939mL10mM0.1847mL0.9235mL1.8469mL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。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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.62mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.62mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.62mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:50mg/mL(92.35mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性GardiquimoddiTFA，⼀种咪唑啉类似物，TLR7/8激动剂。GardiquimoddiTFA可抑制巨噬细胞和活化外周⾎单个核细胞(PBMCs)的HIV-1感染。当浓度低于10μM时，GardiquimoddiTFA特别激活TLR7。IC50&TargetTLR7TLR8HIV-1体外研究GardiquimoddiTFA(6-60ꢀμM)significantlyinhibitscDNAsynthesisbyHIV-1reversetranscriptase[1].体内研究Dendriticcells(DCs)incombinationwithGardiquimod(1mg/kgpermouse;i.p.;dailyfor7days)improvestheanti-tumoreffectsofNKcells[2].AnimalModel:Maleathymicnudemice(Balb-nu/nu,5weeksold)(bearinghumanHepG2livercarcinomaxenografts)[2]Dosage:1mg/kgpermouseAdministration:i.p.;dailyfor7daysResult:SignificantlysuppressedthegrowthofhumanHepG2livercarcinomaxenografts.REFERENCES[1].BuitendijkM,etal.Gardiquimod:aToll-likereceptor-7agonistthatinhibitsHIVtype1infectionofhumanmacrophagesandactivatedTcells.AIDSResHumRetroviruses.2013Jun;29(6):907-18.[2].MaF,etal.TheTLR7agonistsimiquimodandgardiquimodimproveDC-basedimmunotherapyformelanomainmice.CellMolImmunol.2010Sep;7(5):381-8.[3].ZhouZ,etal.TLR7/8agonistspromoteNK-DCcross-talktoenhanceNKcellanti-tumoreffectsinhepatocellularcarcinoma.CancerLett.2015Dec28;369(2):298-306.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat