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Using stable cell lines of GPR40-CHO and MCHR2-CHO, we have identified 8 sulfadimide derivatives as GPR40 antagonists from the tested compounds (Table 1). As an example, Fig. 3B illustrated that DC260126, the most active compound, produced a concentration-dependent inhibition of FFAs stimulated increase of intracellular Ca2+ levels mediated by GPR40. And the IC50 values for approximate EC50 concentration FFAs, linoleic EGFR 985-996 (5 μM), oleic acid (5 μM), palmitoleic acid (3 μM) and lauric acid (4 μM) are 6.28 ± 1.14, 5.96 ± 1.12, 7.07 ± 1.42, 4.58 ± 1.14 μM, respectively. To confirm that the inhibition of the FFAs response by DC260126 is specifically through GPR40, we carried out MCHR2-CHO cells line using MCH as agonist. In contrast to the effect of DC260126 on the FFAs concentration–response curve, DC260126 at concentration up to 10 μM had no significant effect on the EC50 value of the MCH concentration–response curve (Fig. 3C).