PF-06291874 (PF-6291874) is a highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR.
PF-06291874 shows excellent selectivity against a panel of 69 receptors, ion channels, uptake sites and enzymes.
PF-06291874 reduces the glucagon-elicited glucose excursion in a dose-dep endent manner in rats.
PF-06291874 displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.
