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Medchemexpress/TAK-242(Synonyms: Resatorvid)/HY-11109/10mM*1mL in DMSO
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TAK-242isapotentTLR4signalinginhibitor,selectivelyinhibitstheTLR4-mediatedproductionofcytokinesandNO.

CustomerValidation

  • •CancerRes.2016Nov15;76(22):6631-6642.
  • •JAutoimmun.2017Jun;80:28-38.
  • •BrainBehavImmun.2017Jan;59:322-332.
  • •BasicResCardiol.2017Jan;112(1):9.
  • •Oncotarget.2017May9;8(19):31802-31814.
  • •Oncotarget.2017May2;8(18):29996-30007.
  • •Oncotarget.2017Mar28;8(13):21044-21053.
  • •CellPhysiolBiochem.2017Mar29;41(4):1675-1683.
  • •SciRep.2017Mar8;7:43834.
  • •SciRep.2017Mar8;7:43796.
  • •SciRep.2016Aug4;6:30957.
  • •SciRep.2016Jun9;6:27866.
  • •JNeuRochem.2017Oct;143(2):225-235.
  • •JNeurochem.2016May;137(4):576-88.
  • •ExpCellRes.2015Feb15;331(2):320-30.
  • •MolPain.2014Feb6;10(1):10.
  • •AmJPhysiolGastrointestLiverPhysiol.2016Dec1;311(6):G1091-G1104.
  • •AmJPhysiolGastrointestLiverPhysiol.2014Feb;306(3):G244-52.
  • •Neuroscience.2017Sep30;360:128-138.
  • •FoodFunct.2017May24;8(5):1905-1914.
  • •Vaccine.2017Feb15;35(7):1037-1045.
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  • •LifeSci.2017Feb1;170:25-32.
  • •Molecules.2017Jul15;22(7).pii:E1187.
  • •PLoSOne.2017Jul24;12(7):e0181796.
  • •PLoSOne.2017May24;12(5):e0178147.
  • •OncolRep.2017Jun;37(6):3341-3350.
  • •VetMicrobiol.2017May;203:158-166.
  • •JSciFoodAgric.2017Nov;97(14):4727-4736.
  • •PhotochemPhotobiol.2016Nov;92(6):816-825.
  • •JBiochem.2017Oct18.
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  • •BMCMusculoskeletDisord.2014Jan15;15(1):18.
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  • •BiochemBiophysRep.2017Sep;11:147-153.
  • •HainanMedJ,Aug.2017,Vol.28,No.15.
  • •ChineseJournalofPublicHealth.2016,32(11):1480-1484.
  • •UniversitätWürzburg.2016.
  • •SeitokuUniversity.2014.
Description

TAK-242isapotentTLR4signalinginhibitor,selectivelyinhibitstheTLR4-mediatedproductionofcytokinesandNO.

IC50&Target

TLR4[1]

InVitro

InRAW264.7cellsandmouseperitonealmacrophages,TAK-242suppresseslipopolysaccharide(LPS)-inducedproductionofNO,tumornecrosisfactor-α(TNF-α),andinterleukin(IL)-6,withIC50of1.1to11nM.TAK-242alsosuppressestheproductionofthesecytokinesfromLPS-stimulatedhumanperipheralbloodmononuclearcells(PBMCs)atIC50valuesfrom11to33nM[1].

InVivo

TAK-242apparentlyreducestheserumanti-dsDNAlevelsinbothgenotypemice.Alternatively,IFN-γ,TNF-α,andIL-1βproductionismarkedlyinhibitedbyTAK-242,buttheirconcentrationsarestillgreatlyhigherthanthoseinNS-treatedcounterparts[2].TAK-242pre-stressadmiNISTrationpreventstheaccumulationofpotentiallydeleteriousinflammatoryandoxidative/nitrosativemediatorsinthebrainfrontalcortexofrats.TAK-242i.v.administrationatthebeginningofthestresssessioncompletelyblocksTLR-4mRNAandproteinupregulationafterstressexposure[3].

ClinicalTrial
ViewMoreCollapse
References

  • [1].IiM,etal.Anovelcyclohexenederivative,ethyl(6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate(TAK-242),selectivelyinhibitstoll-likereceptor4-mediatedcytokineproductionthroughsuppressionofintracellularsignaling.

    [2].NiJQ,etal.Roleoftoll-likereceptor4onlupuslunginjuryandatherosclerosisinLPS-challengeApoE⁻/⁻mice.ClinDevImmunol.2013;2013:476856.

    [3].GárateI,etal.Toll-like4receptorinhibitorTAK-242decreasesneuroinflammationinratbrainfrontalcortexafterstress.JNeuroinflammation.2014Jan11;11:8.

    [4].WangL,etal.Doxorubicin-InducedSystemicInflammationIsDrivenbyUpregulationofToll-LikeReceptorTLR4andEndotoxinLeakage.CancerRes.2016Nov15;76(22):6631-6642.

    [5].ShibataA,etal.Toll-likereceptor4antagonistTAK-242inhibitsautoinflammatorysymptomsinDITRA.JAutoimmun.2017Jun;80:28-38.

    [6].JandaJ,etal.Resatorvid-basedPharmacologicalAntagonismofCutaneousTLR4BlocksUV-inducedNF-κBandAP-1SignalinginKeratinocytesandMouseSkin.PhotochemPhotobiol.2016Nov;92(6):816-825.

    [7].RAOXiao-jiao,etal.EffectofTLR4onexpressionofinflammatorycytokineinaorticarteryinmicewithinsulinresistance[J].ChineseJournalofPublicHealth,2016,32(11):1480-1484.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.7638mL13.8190mL27.6381mL
5mM0.5528mL2.7638mL5.5276mL
10mM0.2764mL1.3819mL2.7638mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

TAK-242isdissolvedinN,N-dimethylformamide,andthendilutedwithappropriatemediumbeforeuse[1].

RAW264.7cellsareseededatadensityof3×106cells/wellinsix-wellcultureplateandincubatedovernight.AfterwashingwithRPMI1640mediumsupplementedwith1%FCSand10μg/mLKanamycin,thecellsarestimulatedwith5ng/mLLPSand1U/mLIFN-γinthepresenceorabsenceofTAK-242(1-100nM)fortheindicatedtime.Culturesupernatantsareremoved,andtotalRNAisisolatedusingthetotalRNAisolationreagentISOGEN.TotalRNAisreversetranscribedintoCDNAbyusingTaqManreversetranscriptionreagents.Quantitativereal-timePCRanalysisofTNF-αandIL-6isperformedonABIPrism7700usingpredevelopedTaqManassayreagentsandUniversalPCRmastermix.QuantitationofmRNAisperformedusingthecomparativethresholdcyclemethod.Thehighestcontrollevelattainedbythestimulation(withoutTAK-242)isregardedas100%,andthelevelsofcontrolgroupatothertimepointsandTAK-242-addedgroupareexpressedasthepercentageofthehighestcontrollevel[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[2][3]

TAK-242isdissolvedinvehicle(saline)(Mice)[2].
TAK-242isdissolvedinvehicle(0.9%DMSO)(Rat)[3].

Mice[2]
ThirtyApoE-/-andthirtywild-typemiceonC57BL/6background(female,10weeksold)arefedonahigh-fatdietcontaining0.25%cholesteroland15%cocoabutterunderstandardizedlightingconditions(12hlight-darkcycle)andtemperature(21±1°C).Andmineralwaterisadministeredadlibitum.MiceofbothgenotypesarerandomlyassignedtoLPSorLPS+TAK-242orsalineadministration.LPS(2.5mg/kg),LPS(2.5mg/kg)plusTAK-242(0.3mg/kg)andsalineareadministeredrespectivelybyintraperitonealinjection,twiceaweekfor4weeks.Attheendofexperiments,allmiceunderwenteuthanasiawithinjectionofoverdosepentobarbital(50mg/kg).
Rat[3]
MaleoutbredWistarHannoverrats,initiallyweighing200to225g,areused.TAK-242isi.v.injectedinthetailveinatadoseof0.5mg/kgimmediatelyafter(approximately10seconds)introducingtheanimaltotheplasticrestrainer.Thisdoseischosenonthebasisofpreviousinvivostudiesreportingitsanti-inflammatory/antioxidantandneuroprotectiveprofileinmicrogliaexposedtohypoxia.Dimethylsulphoxideataconcentrationof0.9%isusedasvehicle.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].IiM,etal.Anovelcyclohexenederivative,ethyl(6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate(TAK-242),selectivelyinhibitstoll-likereceptor4-mediatedcytokineproductionthroughsuppressionofintracellularsignaling.

    [2].NiJQ,etal.Roleoftoll-likereceptor4onlupuslunginjuryandatherosclerosisinLPS-challengeApoE⁻/⁻mice.ClinDevImmunol.2013;2013:476856.

    [3].GárateI,etal.Toll-like4receptorinhibitorTAK-242decreasesneuroinflammationinratbrainfrontalcortexafterstress.JNeuroinflammation.2014Jan11;11:8.

    [4].WangL,etal.Doxorubicin-InducedSystemicInflammationIsDrivenbyUpregulationofToll-LikeReceptorTLR4andEndotoxinLeakage.CancerRes.2016Nov15;76(22):6631-6642.

    [5].ShibataA,etal.Toll-likereceptor4antagonistTAK-242inhibitsautoinflammatorysymptomsinDITRA.JAutoimmun.2017Jun;80:28-38.

    [6].JandaJ,etal.Resatorvid-basedPharmacologicalAntagonismofCutaneousTLR4BlocksUV-inducedNF-κBandAP-1SignalinginKeratinocytesandMouseSkin.PhotochemPhotobiol.2016Nov;92(6):816-825.

    [7].RAOXiao-jiao,etal.EffectofTLR4onexpressionofinflammatorycytokineinaorticarteryinmicewithinsulinresistance[J].ChineseJournalofPublicHealth,2016,32(11):1480-1484.

MolecularWeight

361.82

Formula

C₁₅H₁₇ClFNO₄S

CASNo.

243984-11-4

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥360mg/mL

TAK-242isdissolvedinafatemulsion(i.v.injection)[4].
TAK-242dissolvedinDMSO(10mg/mL)isdilutedinDW[5].
TAK-242ispreparedin0.5%acetone[6].
TAK-242isprepareinvehicle(sterilesaline)[7].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References

  • [1].IiM,etal.Anovelcyclohexenederivative,ethyl(6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate(TAK-242),selectivelyinhibitstoll-likereceptor4-mediatedcytokineproductionthroughsuppressionofintracellularsignaling.

    [2].NiJQ,etal.Roleoftoll-likereceptor4onlupuslunginjuryandatherosclerosisinLPS-challengeApoE⁻/⁻mice.ClinDevImmunol.2013;2013:476856.

    [3].GárateI,etal.Toll-like4receptorinhibitorTAK-242decreasesneuroinflammationinratbrainfrontalcortexafterstress.JNeuroinflammation.2014Jan11;11:8.

    [4].WangL,etal.Doxorubicin-InducedSystemicInflammationIsDrivenbyUpregulationofToll-LikeReceptorTLR4andEndotoxinLeakage.CancerRes.2016Nov15;76(22):6631-6642.

    [5].ShibataA,etal.Toll-likereceptor4antagonistTAK-242inhibitsautoinflammatorysymptomsinDITRA.JAutoimmun.2017Jun;80:28-38.

    [6].JandaJ,etal.Resatorvid-basedPharmacologicalAntagonismofCutaneousTLR4BlocksUV-inducedNF-κBandAP-1SignalinginKeratinocytesandMouseSkin.PhotochemPhotobiol.2016Nov;92(6):816-825.

    [7].RAOXiao-jiao,etal.EffectofTLR4onexpressionofinflammatorycytokineinaorticarteryinmicewithinsulinresistance[J].ChineseJournalofPublicHealth,2016,32(11):1480-1484.

Purity:99.95%ee.:98.00%

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