BTI-A-404 is a potent and selective competitive inverse agonist of human GPR43 (GPR43/Free Fatty Acid Receptor 2, FFAR2) that increases the cyclic AMP level and regulates and reduces acetate-induced cytoplasmic Ca2+ level. BTI-A-404 regulates the downstream signaling pathways of GPR43, including ERK, p38 MAPK, and NF-KB. BTI-A-404 stimulates GLP-1 release.