A-967079-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA-967079Cat.No.:HY-108463CASNo.:1170613-55-4分?式:C??H??FNO分?量:207.24作?靶點(diǎn):TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(482.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.8253mL24.1266mL48.2532mL5mM0.9651mL4.8253mL9.6506mL10mM0.4825mL2.4127mL4.8253mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(12.06mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(12.06mM);ClearsolutionBIOLOGICALACTIVITY?物活性A-967079?種選擇性TRPA1受體拮抗劑，對(duì)?和??TRPA1受體的IC50分別為67nM和289nM，并且具有良好的CNS穿透性。IC50&TargetIC50:67nM(humanTRPA1receptor),289nM(ratTRPA1receptor)[1]體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].McGaraughtyS,etal.TRPA1modulationofspontaneousandmechanicallyevokedfiringofspinalneuronsinuninjured,osteoarthritic,andinflamedrats.MolPain.2010Mar5;6:14.McePdfHeightCaution:Produ