Free fatty acid receptor 1 (FFA1/GPR40) antagonist. Inhibits FFA-induced increases in intracellular Ca2+
levels and suppresses palmitic acid potentiated glucose-stimulated insulin secretion in Min6 pancreatic β
cells in vitro
. Decreases serum insulin levels, improves insulin sensitivity and reduces the number of apoptotic pancreatic β
cells in obese diabetic (db/db
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DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats.
Zhang et al.
DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic β-Cells dysfunction in db/db mice.
Sun et al.
PLoS ONE, 2013;8:e66744
A novel class of antagonists for the FFAs receptor GPR40.
Hu et al.