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PotentandselectiveinhibitoroftheneuronalK-Clcotransporter,KCC2(IC50=61nM);displays>100-foldselectivityversustheNa-K-2Clcotransporter1(NKCC1)andnoactivityagainstapanelof68GPCRs,ionchannelsandtransporters.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight382.5.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Delpireetal(2012)FurtheroptimizationoftheK-ClcotransporterKCC2antagoNISTML077:developmentofahighlyselectiveandmorepotentinvitroprobe.Bioorg.Med.Chem.Lett.224532PMID:22727639
Sivakumaranetal(2015)SelectiveinhibitionofKCC2leadstohyperexcitABIlityandepileptiformdischargesinhippocampalslicesandinvivo.J.Neurosci.358291PMID:26019342
Keywords:VU0463271,supplier,VU0463271,potent,selective,inhibitors,inhibits,neuronal,K-Cl,cotransporters,KCC2,K+/Cl-,Cotransporter,2,K+/Cl-,Cotransporter,2,TocrisBioscience
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