346692-04-4

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.

DC260126 is a potent antagonist of GPR40 (FFAR1). DC260126 dose-dependently inhibits GPR40-mediated Ca2+ elevations stimulated by linoleic acid, oleic acid, palmitoleic acid and lauric acid (IC50: 6.28, 5.96, 7.07, 4.58 μM, respectively)[1]. DC260126 could protect MIN6 β cells from palmitate-induced ER stress and apoptosis[2].

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1) Hu?et al. (2009),?A novel class of antagonist for the FFAs receptor GPR40; Biochem. Biophys. Res. Commun.,?390?557 2) Zhang?et al. (2010),?DC260126, a small molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats; Biomed. Pharmacother.,?64?647 3) Sun?et al. (2013),?DC260126: a small molecule antagonist of GPR40 that protects against pancreatic β-cells dysfunction in db/db mice; PLoS One.,?8(6)?e66744 4) Wu?et al. (2012), Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis; J. Biochem,?113?1152