SM-276001-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESM-276001Cat.No.:HY-123291CASNo.:473930-22-2分⼦式:C₁₆H₂₁N₇O分⼦量:327.38作⽤靶点:Toll-likeReceptor(TLR);IFNAR作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(381.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0546mL15.2728mL30.5455mL5mM0.6109mL3.0546mL6.1091mL10mM0.3055mL1.5273mL3.0546mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.35mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.35mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性SM-276001⼀种有效的选择性TLR7激动剂，可以诱导抗肿瘤免疫反应。SM-276001⼀种具有⼝服活性的⼲扰素(IFN)诱导剂[1][2]。IC50&TargetTLR7;IFN[1][2]体外研究SM-276001(1nM-10μM)dose-dependentlyactivatesNF-κBthroughhumanTLR7[2].体内研究SM-276001demonstratespotentIFN-inducingactivityatadoseof0.1mg/kgbyoraladministrationinmice[1].OraladministrationofSM-276001,leadstotheinductionofaninflammatorycytokineandchemokinemilieuandtotheactivationofadiversepopulationofimmuneeffectorcellsincludingTandBlymphocytes,NKandNKTcells[2].SM-276001(3mg/kgPObiweekly)significantlyinhibitstumorgrowthintheRencarenalcellcancerandCT26colorectalmodels[2].SM-276001(orally;0.1,1or10mg/kg)leadstotheactivationofadiversepopulationofspleen-residentimmuneeffectorcellsinBalb/candC57BL/6Jmice.Whenadministeredat1mg/kgorgreater,theplasmaconcentrationofSM-276001exceedstheMECof30nM[2].AnimalModel:C57BL/6andB6C3F1micebearingRencaorCT26tumors[2]Dosage:3mg/kgAdministration:Oraladministrationtwiceweeklyfor25daysResult:SignificantlyreduceddiseaseburdeninmicebearingeitherRencaorCT26tumors.REFERENCES[1].IsobeY,etal.Synthesisandbiologicalevaluationofnovel9-substituted-8-hydroxyadeninederivativesaspotentinterferoninducers.JMedChem.2006Mar23;49(6):2088-95.[2].Koga-YamakawaE,etal.IntratrachealandoraladministrationofSM-276001:aselectiveTLR7agonist,leadstoantitumorefficacyinprimaryandmetastaticmodelsofcancer.IntJCancer.2013Feb1;132(3):580-90.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication