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PotentandselectiveGPR39agonist(EC50valuesare0.4and0.8nMforratandhumanreceptorsrespectively).Selectiveoverapanelofkinases(IC50s>10μM)anddisplaysminimalbindingaffinityforghrelinandneurotensin-1receptors(IC50s>30μM).IncreasesGLP-1levelsinvitroandinvivo.Orallybioavailable.
TC-G1008isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight418.9.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Peukertetal(2014)Discoveryof2-pyridylpyrimidinesasthefirstorallybioavailableGPR39agonists.ACSMed.Chem.Lett.51114PMID:25313322
Keywords:TC-G1008,supplier,TC-G1008,potent,selective,GPR39,agonists,agonism,Orphan,7-TM,Receptors,Orphan,7-TM,Receptors,TocrisBioscience
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