DC260126 is a free fatty acid receptor 1 (FFAR1/GPR40) antagonist that inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic, oleic, palmitoleic, and lauric acid (Item Nos. 90150, 90260, 10009871, and 10006626, respectively) with IC50 values of 6.28, 5.96, 7.07, and 4.58 μM, respectively. At 10 mg/kg, it has been shown to inhibit glucose-stimulated insulin secretion, to reduce blood insulin levels, to improve insulin sensitivity, and to decrease the rate of pancreatic β-cell apoptosis in obese diabetic db/db mice.
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