Azoramide is a modulator of the unfolded protein response with antidiabetic activity. It has dual activity: Azoramide improves endoplasmic reticulum (ER) protein-folding ability and stimulates the expression of ER chaperones that protect cells against ER stress. Azoramide was shown to protect cells from death and dysfunction in multiple models of ER stress. It showed antidiabetic activity in two independent mouse models of obesity by improving insulin sensitivity and protecting pancreatic β cell function against ER stress.