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PotentandselectiveTRPV4antagonist(IC50valuesare2and40nMforratandhumanreceptors,respectively);inhibitsCa2+influxthroughTRPV4channels.Preventsandreversespulmonaryedemaaftermyocardialinfarctioninvivomodels.Selectiveoverapanelof~200humanreceptors,channelsandenzymes.Orallyactive.
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
GSK2193874isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight691.62.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Thorneloeetal(2012)AnorallyactiveTRPV4channelblockerpreventsandresolvespulmonaryedemainducedbyheartfailure.Sci.Transl.Med.4159PMID:23136043
Cheungetal(2017)DiscoveryofGSK2193874:anorallyactive,potent,andselectiveblockeroftransientreceptorpotentialvanilloid4.ACSMed.Chem.Lett.8549PMID:28523109
Keywords:GSK2193874,supplier,GSK2193874,potent,selectiveTRPV4,inhibitors,antagonists,orally,active,transient,receptors,potential,vanilloids,channels,myocardial,infarction,pulmonary,oedema,edema,inhibits,TRPV,TRPV,TocrisBioscience
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