Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGardiquimoddiTFACat.No.:HY-103697ACASNo.:1159840-61-5分?式:C??H??F?N?O?分?量:541.44作?靶點:Toll-likeReceptor(TLR);HIV作?通路:Immunology/Inflammation;Anti-infection儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(92.35mM;Needultrasonic)H2O:25mg/mL(46.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8469mL9.2346mL18.4693mL5mM0.3694mL1.8469mL3.6939mL10mM0.1847mL0.9235mL1.8469mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.62mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.62mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.62mM);Clearsolution4.請依序添加每種溶劑：PBSSolubility:50mg/mL(92.35mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性GardiquimoddiTFA，?種咪唑啉類似物，TLR7/8激動劑。GardiquimoddiTFA可抑制巨噬細胞和活化外周?單個核細胞(PBMCs)的HIV-1感染。當濃度低于10μM時，GardiquimoddiTFA特別激活TLR7。IC50&TargetTLR7TLR8HIV-1體外研究GardiquimoddiTFA(6-60?μM)significantlyinhibitscDNAsynthesisbyHIV-1reversetranscriptase[1].體內(nèi)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