Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEL-KynurenineCat.No.:HY-104026CASNo.:2922-83-0分?式:C??H??N?O?分?量:208.21作?靶點:ArylHydrocarbonReceptor;EndogenousMetabolite作?通路:Immunology/Inflammation;MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗H2O:20mg/mL(96.06mM;Needultrasonic)DMSO:12.5mg/mL(60.04mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.8028mL24.0142mL48.0284mL5mM0.9606mL4.8028mL9.6057mL10mM0.4803mL2.4014mL4.8028mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.83mg/mL(3.99mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥0.83mg/mL(3.99mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(9.99mM);ClearsolutionBIOLOGICALACTIVITY?物活性L-KynurenineL-?氨酸的代謝物。它?種芳?烴受體(arylhydrocarbonreceptor)激動劑。IC50&TargetHumanEndogenousMetabolite體外研究Kynurenineanditsfurtherbreakdownproductscarryoutdiversebiologicalfunctions,includingdilatingbloodvesselsduringinflammationandregulatingtheimmuneresponse.Somecancersincreasekynurenineproduction,whichincreasestumorgrowth.L-kynurenine(Kyn)isanarylhydrocarbonreceptor(AHR)agonistthatactivatesAHR-directed,naiveTcellpolarizationtotheanti-inflammatoryTregphenotype.KynurenineactivatesAHRsignalingatphysiologicalconcentrationsinH1L7.5c3cellsandactsasanAHRagonistaftera24-hrexposurebyinducingtheAHR-regulatedluciferasegeneinH1L7.5c3mousehepatocytecells[1].體內研究KynureninedilatesarteriesfromratsaswellashumansviaKv7channelsinthevascularsmoothmuscle.Inrats,thistryptophanmetabolitecauseshypotension,whichispartlycounteractedbyKv7channelinhibition[2].L-kynurenineadministered1hbeforethehypoxia-ischemiashowsadose-dependentsignificantneuroprotectiveeffect,withcompleteprotectionatadoseof300mg/kg.Theinductionofc-fosimmunoreactivityincerebralcortexisalsoblockedbythisdoseofL-kynurenine[3].PROTOCOLCellAssay[1]LuciferaseassaysarecarriedoutusingtheH1L7.5c3cells.Attheindicatedtimes(0.5,2,4,6,12,18,24h)andconcentrations(0.1,1,10,100μM)ofexposurestoKynurenine,cellsareremovedfromincubationandallowedtoequilibratetoroomtemperaturefor15min.Afterequilibration,themediumisremovedandthecellsarewashedtwicewithatroomtemperaturewithDPBS.Thecellsarelysedwith20μL/well1×PassiveLysisBufferandshakenfor20minatroomtemperature.LuciferaseactivityisrecordedusinganLuminometerMicroplateReader[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats[3]Administration[3]TheeffectsofincreasingdosesofL-kynureninewithorwithoutprobenecidonconcentrationsofkynurenicacidincerebralcortexareexaminedin7-day-oldrats.Sixanimalsareexaminedineachgroup.AnimalsaretreatedwithL-kynurenineatdosesof100,200,300,and400mg/kgorkynurenine,200mg/kgwithprobenecid,50mg/kg.Animalsarekilledat1h,thebrainspromptlyremoved,andthecerebralcortexisdissectedandplacedin0.5mLofchilled0.1MHCl.Kynurenicacidmeasurementsaremadebyhigh-performanceliquidchromatographywithfluorescencedetection.Proteinmeasurementsaremadeusinga2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEfluorometricassay[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發表的科研?獻?ACSNano.2020Nov25.?NatCommun.2022Sep26;13(1):5644.?PLoSPathog.2020Jul17;16(7):e1008664.?DNACellBiol.2022Apr;41(4):447-455.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MoyerBJ,etal.InhibitionofthearylhydrocarbonreceptorpreventsWesterndiet-inducedobesity.ModelforAHRactivationbykynurenineviaoxidized-LDL,TLR2/4,TGFβ,andIDO1.ToxicolApplPharmacol.2016Jun1;300:13-24.[2].SakakibaraK,etal.KynureninecausesvasodilationandhypotensioninducedbyactivationofKCNQ-encodedvoltage-dependentK(+)channels.JPharmacolSci.2015Sep;129(1):31-7.[3].NozakiK,etal.NeuroprotectiveeffectsofL-kynurenineonhypoxia-ischemiaandNMDAlesionsinneonatalrats.JCerebBlood