G protein-coupled receptors are seven-transmembrane proteins that can be activated by free fatty acid. GW950 is a small-molecule agonist of GPR40 and GPR120 with pEC50 values of 7.32±0.03 and 5.46±0.09, respectively. It also induced intracellular Ca2+ mobilization in HEK293 cells expressing GPR40 (pEC50=7.32±0.03) or GPR120 (pEC50=5.46±0.09). In MIN6 mouse insulinoma cell line, GW9508 induced a concentration-dependent increase in high glucose (25mM)-stimulated insulin secretion with a pEC50 of 6.14±0.03[3]. The administration of 200mM GW9508 to the ear 1h before each DNFB treatment significantly attenuated ear swelling in BALB/c mice compared with the controls. GW9508 treatment also significantly reduced the expression of CCL5 and eosinophils infiltrating in the skin compared to the vehicle-treated group. In C57BL/6 mice subjected to DNFB-induced CHS, application of GW9508 at 10-100μM suppressed ear swelling in a dose-dependent manner[4].
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