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InhibitoroftheneuronalK-Clcotransporter,KCC2(IC50=560nMforK+uptakeassayinKCC2-overexpressingcells).ExhibitsselectivityovertheNa-K-2Clcotransporter,NKCCl.AlsoinhibitshERGandL-typeCa2+channels.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight342.43.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Delpireetal(2009)Small-moleculescreenidentifiesinhibitorsoftheneuronalK-ClcotransporterKCC2.Proc.Natl.Acad.Sci.USA1065383PMID:19279215
Delpireetal(2012)FurtheroptimizationoftheK-ClcotransporterKCC2antagoNISTML077:developmentofahighlyselectiveandmorepotentinvitroprobe.Bioorg.Med.Chem.Lett.224532PMID:22727639
Deiszetal(2014)EffectsofVU0240551,anovelKCC2antagonist,andDIDSonchloridehomeostasisofneocorticalneuronsfromratsandhumans.Neuroscience277831PMID:25086309
Keywords:VU0240551,supplier,cotransporter,potassium,chloride,transport,KCC2,Neuronal,cotransport,SLC12A5,Na+/2Cl-/K+,NKCC1,NKCC2,inhibitors,inhibits,Ion,Pumps,K-Cl,VU0240551,epilepsy,K+/Cl-,Cotransporter,2,K+/Cl-,Cotransporter,2,TocrisBioscience
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