Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hyperglycemia in normal rabbits without affecting glycogenolysis in vivo. Also blocks endogenous glucagon-induced hyperglycemia in streptozocin diabetic rats.

HAEGTFTSD is the first N-terminal 1-9 residues of GLP-1 peptide.The GLP-1 (7-36) amide is a product of the preproglucagon gene, which is secreted from intestinal L-cells, in response to the ingestion of food.

PF-06882961 is an orally bioavailable glucagon-like peptide-1 receptor (GLP-1R) agonist. PF-06882961 shows mild to moderate damage to the heart, moderate to severe effects on the thymus gland (which helps with managing infection), mild to moderate stomach ulcers at the highest dose level given in the rat.