BemPPOX is an orally active, potent dog gastric lipase (DGL) inhibitor with X l50 (the inhibitor molar excess leading to 50% lipase inhibition) of 0.5. BemPPOX is also a good inhibitor of GPLRP2 (x l50 =0.64). BemPPOX efficiently regulates the gastrointestinal lipolysis and slows down the overall lipolysis process in rats. BemPPOX has the potential for obesity research.