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Description | TAK-242isapotentTLR4signalinginhibitor,selectivelyinhibitstheTLR4-mediatedproductionofcytokinesandNO. |
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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 |
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Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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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]. Mice[2] | ||||||||||||||||
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MolecularWeight | 361.82 | ||||||||||||
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Formula | C₁₅H₁₇ClFNO₄S | ||||||||||||
CASNo. | 243984-11-4 | ||||||||||||
Storage |
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | DMSO:≥360mg/mL TAK-242isdissolvedinafatemulsion(i.v.injection)[4]. *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> | ||||||||||||
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Purity:99.95%ee.:98.00%