A-967079-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEA-967079Cat.No.:HY-108463CASNo.:1170613-55-4分⼦式:C₁₂H₁₄FNO分⼦量:207.24作⽤靶点:TRPChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(482.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.8253mL24.1266mL48.2532mL5mM0.9651mL4.8253mL9.6506mL10mM0.4825mL2.4127mL4.8253mL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%salineSolubility:≥2.5mg/mL(12.06mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(12.06mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性A-967079⼀种选择性TRPA1受体拮抗剂，对⼈和⼤⿏TRPA1受体的IC50分别为67nM和289nM，并且具有良好的CNS穿透性。IC50&TargetIC50:67nM(humanTRPA1receptor),289nM(ratTRPA1receptor)[1]体内研究SystemicinjectionofA-967079(30μmol/kg,i.v.)decreasestheresponsesofwidedynamicrange(WDR),andnociceptivespecific(NS)neuronsfollowingnoxiouspinchstimulationoftheipsilateralhindpawinuninjuredandCFA-inflamedrats.Similartoitsactionsinuninjuredrats,administrationofA-967079(30μmol/kg,i.v.)tocompleteFreund'sadjuvant(CFA)-inflamedratssignificantlyreducesWDRneuronalresponsestonoxiouspinchstimulationcomparedtobaselinefiring(p=0.0013,repeated-measuresANOVA)andthevehiclegroup(p=0.0001,two-wayANOVA).Themaximumobservedeffect(61.1±10.97%decreasefrombaselinelevels)onpinch-evokedactivityininflamedratsoccur35minafterinjection.Incontrasttouninjuredrats,injectionofA-967079toCFA-inflamedratsalsosignificantly(p=0.0004,andp=0.0001fortherepeated-measuresandtwo-wayANOVA's,respectively)reducesresponsesofWDRneuronsto10-gvonFreyhairstimulation.ThemaximalobserveddecreaseinvonFrey-evokedactivityis67.69±18.39%frombaselinelevels(35minpost-injection),andisthuscomparabletotheeffectsofA-967079onpinch-evokedactivityininflamedrats[1].PROTOCOLAnimalRats[1]Administration[1]MaleSprague-Dawleyrats(250-400g)areusedforallexperimentsandarehousedinatemperaturecontrolledroomwitha12/12-hrday/nightcycle.Foodandwaterareavailableadlibitum.Spontaneousandevokedneuronalactivityisthenmeasured5,15,25,and35minaftersystemicinjectionofA-967079(30μmol/kg,i.v.)orvehicle(polyethyleneglycol).TheintravenousinjectionofA-967079orvehicleiscompletedovera6-7minperiod.Thei.v.doseofA-967079isselectedbasedonextrapolatedplasmalevelsthatareeffectiveinbehavioralstudies[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CancerLett.2020Jan28;469:287-300.•FrontMolNeurosci.2021Jun4;14:690858.•PestManagSci.2020Sep;76(9):3003-3011.•MolCellBiochem.2020Oct;473(1-2):179-192.•CellStressChaperones.2020Nov;25(6):955-968.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].McGaraughtyS,etal.TRPA1modulationofspontaneousandmechanicallyevokedfiringofspinalneuronsinuninjured,osteoarthritic,andinflamedrats.MolPain.2010Mar5;6:14.McePdfHeightCaution:Produ