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Oral administration of PF-06882961 shows evidence of glucose-lowering in healthy human study participants PF-06882961 was selected as a candidate for clinical studies based on its in vitro and in vivo pharmacologic and disposition profile, including potent agonism of the GLP-1R, preclinical disposition attributes (e.g., low metabolic CL int in human hepatocytes), good safety margins versus the hERG channel (IC 50 = 4.3 M, Table S4) and broad panel screening (Table S8), and selectivity versus related class B GPCRs (Table S9)

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Cornu M, Yang J-Y, Jaccard E, Poussin C, Widmann C, Thorens B

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