N-(4-butylphenyl)-4-fluorobenzenesulfonamide

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].

Store at -20°C

[1] HUI HU . A novel class of antagonists for the FFAs receptor GPR40[J]. Biochemical and biophysical research communications, 2009, 390 3: Pages 557-563. DOI:10.1016/j.bbrc.2009.10.004
[2] XIAODONG ZHANG . DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats[J]. Biomedicine & Pharmacotherapy, 2010, 64 9: Pages 647-651. DOI:10.1016/j.biopha.2010.06.008
[3] PENG SUN. DC260126: a small-molecule antagonist of GPR40 that protects against pancreatic β-Cells dysfunction in db/db mice.[J]. PLoS ONE, 2013: e66744. DOI:10.1371/journal.pone.0066744
[4] JINWEI WU. Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis[J]. Journal of cellular biochemistry, 2011, 113 4: 1152-1158. DOI:10.1002/jcb.23450