Description
DC260126 is a free fatty acid receptor 1 (FFAR1/GPR40) antagonist that inhibits GPR40-mediated Ca
2+ elevations stimulated by linoleic, oleic, palmitoleic, and lauric acid (Item Nos.
90150,
90260,
10009871, and
10006626, respectively) with IC
50 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.
References
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
