A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect

We present a novel free fatty acid receptor 1 (FFA1) agonist, named PAFA, with a strong agonist potency (EC50 = 6.04 nM) and good serum stability. PAFA significantly stimulates insulin secretion in INS-1 cells in a glucose-dependent manner and exhibits high antihyperglycemic effects in db/db mice without adverse effects.