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Medchemexpress/TAK-242(Synonyms: Resatorvid)/HY-11109/10mg

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Medchemexpress/TAK-242(Synonyms: Resatorvid)/HY-11109/10mg

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MedChemExpress

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HY-11109-10mM*1mLinDMSO

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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.
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•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.
•Vaccine.2015Apr15;33(16):1923-33.
•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.
•Cytotechnology.2017Apr;69(2):229-244.
•BMCMusculoskeletDisord.2014Jan15;15(1):18.
•MolMedRep.2017Sep;16(3):3111-3116.
•OncolLett.2016Aug;12(2):1034-1040.
•BiosciBiotechnolBiochem.2016Jul;80(7):1393-402.
•ChinMedJ(Engl).2017Apr20;130(8):906-913.
•UniversityofArizona.02-Nov-2017.
•BiochemBiophysRep.2017Sep;11:147-153.
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•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

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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

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.7638mL	13.8190mL	27.6381mL
5mM	0.5528mL	2.7638mL	5.5276mL
10mM	0.2764mL	1.3819mL	2.7638mL

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

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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