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PotentandselectiveTRPV1antagonist.BlocksCa2+uptakebyCHOcellsexpressingTRPV1receptors(IC50valuesare0.6and0.8nMforcapsaicin(Cat.No.0462)andacid-inducedCa2+uptake,respectively).Exhibits>4000-foldselectivityforTRPV1overotherTRPchannels.Blockscapsaicin-inducedflinchresponseandcauseshyperthermiainrats.Orallyavailableandnon-CNSpenetrant.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight472.42.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Tamayoetal(2008)Designandsynthesisofperipherallyrestrictedtransientreceptorpotentialvanilloid1(TRPV1)antagonists.J.Med.Chem.512744PMID:18386885
Gavvaetal(2007)ThevanilloidreceptorTRPV1istonicallyactivatedinvivoandinvolvedinbodytemperatureregulation.J.Neurosci.273366PMID:17392452
Keywords:AMG21629,supplier,AMG21629,transient,receptor,potential,vanilloid,TRPV1,antagonists,antagonism,orally,available,potent,selective,hyperthermia,TRPV,TRPV,TocrisBioscience
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