产品描述:
Adomeglivant is an allosteric antagonist of the glucagon receptor.{47796,47797} It inhibits glucagon-induced increases in cAMP levels in HEK293 cells expressing the rat glucagon or GLP-1 receptors (IC50s = 1.8 and 1.2 µM, respectively) but has no effect on cAMP levels when used alone.{47797} Adomeglivant also inhibits increases in cAMP levels induced by GLP-1 or exendin-4 (48-86) amide (Item No. 11096) in HEK293 cells expressing the GLP-1 receptor (IC50s = 7 and 12 µM, respectively). It decreases glucose-stimulated insulin secretion when used at a concentration of 1 µM in combination with the GLP-1 receptor antagonist exendin (9-39) in isolated human islets but not glucose-stimulated glucagon secretion when used alone or in combination with exendin (9-39) in isolated mouse islets.{47798}