Resatorvid-TAK-242-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEResatorvidCat.No.:HY-11109CASNo.:243984-11-4Synonyms:TAK-242;CLI-095分⼦式:C₁₅H₁₇ClFNO₄S分⼦量:361.82作⽤靶点:Toll-likeReceptor(TLR);TNFReceptor;InterleukinRelated;Autophagy作⽤通路:Immunology/Inflammation;Apoptosis;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(276.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7638mL13.8190mL27.6381mL5mM0.5528mL2.7638mL5.5276mL10mM0.2764mL1.3819mL2.7638mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：1%DMSO>>99%salineSolubility:0.5mg/mL(1.38mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.75mg/mL(7.60mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.75mg/mL(7.60mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(7.60mM);Clearsolution5.请依序添加每种溶剂：10%DMSO>>90%salineSolubility:5mg/mL(13.82mM);Suspendedsolution;Needultrasonic6.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:5.5mg/mL(15.20mM);Suspendedsolution;Needultrasonic7.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:5.5mg/mL(15.20mM);Suspendedsolution;Needultrasonic8.请依序添加每种溶剂：5%DMSO>>95%salineSolubility:2.5mg/mL(6.91mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Resatorvid(TAK-242)⼀种选择性的TLR4信号传导抑制剂。Resatorvid抑制NO，TNF-α和IL-6的产⽣，其IC50值分别为1.8nM，1.9nM，1.3nM。Resatorvid下调TLR4下游信号分⼦MyD88和TRIF的表达。Resatorvid抑制⾃噬(autophagy)，并在各种炎症性疾病中起关键作⽤。IC50&TargetTLR4IL-6TNF-R1.3nM(IC50)1.9nM(IC50)体外研究ResatorvidsuppressestheproductionofNO,TNF-α,andIL-6fromLPS-stimulatedhumanperipheralbloodmononuclearcells(PBMCs)atIC50valuesfrom11to33nM[1].Resatorvid(1-100nM;4hours)inhibitsmRNAexpressionofIL-6andTNF-αinducedbyLPSandIFN-γinRAW264.7cells[1].Resatorvid(1-100nM;15minutes;PBMCscells)markedlyinhibitstheLPS-inducedphosphorylationofextracellularsignal-regulatedkinase1/2(Erk1/2),p38,andJNK/SAPKaswellasdegradationofIκBβataconcentrationof100nM[1].RT-PCR[1]CellLine:RAW264.7cellsConcentration:1nM,10nM,100nMIncubationTime:4hoursResult:TNF-αandIL-6mRNAexpressionlevelswereclearlysuppressedatconcentrationsof10to100nM.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEWesternBlotAnalysis[1]CellLine:PBMCscellsConcentration:1nM,10nM,100nMIncubationTime:15minutesResult:Thephosphorylationofmitogen-activatedproteinkinasesinducedbyLPSwasalsoinhibitedinaconcentration-dependentmanner.体内研究Resatorvid(TAK-242;3ꢀmg/kg;intraperitonealinjection;for2days;maleC57BL/6mice)pretreatmentmarkedlyandsignificantlyreversestheLPS-inducedbodyweightloss,TAmuscleloss,andmusclestrengthloss.TAK-242reversestheLPS-inducedshrinkageofmusclefibresandincreasestheinterstitialspace.TAK-242blockssystemiccataboliccytokinereleaseandskeletalmuscleproteolysisinLPS-administeredmice[3].AnimalModel:MaleC57BL/6mice(8-12weeksofage)treatedwithlipopolysaccharide(LPS)[3]Dosage:3ꢀmg/kgAdministration:Intraperitonealinjection;for2daysResult:PretreatmentofmicereducedorreversedallthedetrimentaleffectsofLPS.户使⽤本产品发表的科研⽂献•CellHostMicrobe.2021Feb10;29(2):222-235.e4.•NatBiomedEng.2021Nov8.•Gut.2020Oct29;70(8):1495-1506.•NatMetab.2020Dec;2(12):1427-1442.•JClinInvest.2022Feb3;e152780.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].IiM,etal.Anovelcyclohexenederivative,ethyl(6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate(TAK-242),selectivelyinhibitstoll-likereceptor4-mediatedcytokineproductionthroughsuppressionofintracellularsignaling.[2].YamadaM,etal.Discoveryofnovelandpotentsmall-moleculeinhibitorsofNOandcytokineproductionasantisepsisagents:synthesisandbiologicalactivityofalkyl6-(N-substitutedsulfamoyl)cyclohex-1-ene-1-carboxylate.JMedChem.2005Nov17;48(23)[3].YukoOno,etal.TAK-242,aSpecificInhibitorofToll-likeReceptor4Signalling,PreventsEndotoxemia-InducedSkeletalMuscleWastinginMice.SciRep.2020Jan20;10(1):694.McePdfHeight3/3Masterof