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PotentandselectiveGRK2/3inhibitor(IC50valuesare32and54nMforGRK3andGRK2,respectively).ExhibitsselectivityforGRK2/3overGRK1/5.ReducesDAMGO-induceddesensitizationandinternalizationofμ-opioidreceptors.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight466.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Loweetal(2015)RoleofGprotein-coupledreceptorkinases2and3inμ-opioidreceptordesensitizationandinternalization.Mol.Pharmacol.88347PMID:26013542
Thaletal(2011)MolecularmechanismofselectivityamongGprotein-coupledreceptorkinase2inhibitors.Mol.Pharmacol.80294PMID:21596927
Keywords:CMPD101,supplier,potent,selective,GRK2,GRK3,inhibitors,inhibits,receptors,GPCRs,desensitization,kinases,G,Protein,(Heterotrimeric),G,Protein,(Heterotrimeric),TocrisBioscience
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