L-Kynurenine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEL-KynurenineCat.No.:HY-104026CASNo.:2922-83-0分⼦式:C₁₀H₁₂N₂O₃分⼦量:208.21作⽤靶点:ArylHydrocarbonReceptor;EndogenousMetabolite作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:20mg/mL(96.06mM;Needultrasonic)DMSO:12.5mg/mL(60.04mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.8028mL24.0142mL48.0284mL5mM0.9606mL4.8028mL9.6057mL10mM0.4803mL2.4014mL4.8028mL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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥0.83mg/mL(3.99mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥0.83mg/mL(3.99mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(9.99mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性L-KynurenineL-⾊氨酸的代谢物。它⼀种芳⾹烃受体(arylhydrocarbonreceptor)激动剂。IC50&TargetHumanEndogenousMetabolite体外研究Kynurenineanditsfurtherbreakdownproductscarryoutdiversebiologicalfunctions,includingdilatingbloodvesselsduringinflammationandregulatingtheimmuneresponse.Somecancersincreasekynurenineproduction,whichincreasestumorgrowth.L-kynurenine(Kyn)isanarylhydrocarbonreceptor(AHR)agonistthatactivatesAHR-directed,naiveTcellpolarizationtotheanti-inflammatoryTregphenotype.KynurenineactivatesAHRsignalingatphysiologicalconcentrationsinH1L7.5c3cellsandactsasanAHRagonistaftera24-hrexposurebyinducingtheAHR-regulatedluciferasegeneinH1L7.5c3mousehepatocytecells[1].体内研究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—您⾝边的抑制剂⼤师www.MedChemEfluorometricassay[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•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