diABZI-STING-agonist-1-trihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEdiABZISTINGagonist-1trihydrochlorideCat.No.:HY-112921BCASNo.:2138299-34-8分⼦式:C₄₂H₅₄Cl₃N₁₃O₇分⼦量:959.32作⽤靶点:STING作⽤通路:Immunology/Inflammation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:90mg/mL(93.82mM;Needultrasonic)H2O:25mg/mL(26.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0424mL5.2120mL10.4241mL5mM0.2085mL1.0424mL2.0848mL10mM0.1042mL0.5212mL1.0424mL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:≥2.08mg/mL(2.17mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(2.17mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(2.17mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:33.33mg/mL(34.74mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性diABZISTINGagonist-1(trihydrochloride)⼀个选择性的⼲扰素因刺激受体(STING)的激动剂，其在⼈和⼩⿏中的EC50值分分别为130nM和186nM。IC50&TargetSTING[1].体外研究diABZISTINGagonist-1isaselectivestimulatorofinterferongenes(STING)receptoragonist,withEC50sof130,186nMforhumanandmouse,respectively.Ataconcentrationof1μM,diABZISTINGagonist-1(compound3)demonstrateshighselectivityagainstmorethan350kinasestested[1].体内研究diABZISTINGagonist-1trihydrochloride(subcutaneousinjection;2.5mg/kg)inducesSTING-dependentactivationoftype-Iinterferonandpro-inflammatorycytokinesinvivo[1].diABZISTINGagonist-1trihydrochloride(intravenousinjection;3mg/kg)exhibitssystemicexposurewithahalf-lifeof1.4handachievessystemicconcentrationsgreaterthanthehalf-maximaleffectiveconcentration(EC50)formouseSTING(200ng/ml)[1].diABZISTINGagonist-1trihydrochloride(intravenousinjection;1.5mg/kg;days1,4and8;43days)resultsinsignificanttumourgrowthinhibitionandsignificantlyimprovessurvival(Pꢀ[1].AnimalModel:WildandSting−/−C57Blk6mice[1]Dosage:2.5mg/kgAdministration:Subcutaneousinjection;2.5mg/kgResult:ActivatedsecretionofIFNβ,IL-6,TNF,andCXCL1inwild-typebutnotSting−/−mice.AnimalModel:Syngeneicmousemodelofcolorectaltumours(CT-26)inBALB/cmice[1]Dosage:3mg/kgAdministration:Intravenousinjection;3mg/kgResult:Exhibitedahalf-lifeof1.4hoursandachievedsystemicconcentrationsgreaterthanEC50formouseSTING(200ng/ml).AnimalModel:Syngeneicmousemodelofcolorectaltumours(CT-26)inBALB/cmice[1]Dosage:1.5mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intravenousinjection;1.5mg/kg;43daysResult:Resultedinsignificanttumourgrowthinhibitionandimprovedsurvival.户使⽤本产品发表的科研⽂献•CellRes.2022Oct24.•NatNanotechnol.2021Sep30.•ProteinCell.2021Oct22;1-21.•CancerLett.20August2022,215885.•CellDeathDis.2022Jul28;13(7):653.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RamanjuluJM,etal.DesignofamidobenzimidazoleSTINGreceptoragonistswithsystemicactivity.Nature.2018Nov7.McePdfHeightCaution:Product