GW-1100 is a selective GPR40 and FFAR1 antagonist for the study of diabetes and metabolic diseases.

FFA1/GPR40:6.9 (pic50)

GW-1100 (1 μM) caused a significant right shift in the concentration-response curve of GW9508 (pEC50=7.17±0.08 in the absence, pEC50=6.79±0.09P<0.05 in the presence of 1 μM GW-1100; n=3); At GW-1100 concentrations (3 μM and above), the maximum response is significantly reduced, and the pEC50 response continues to shift to the right [2]; CHO-K1/bFFAR1 cells were incubated with 10 μM GW1100 or vehicle (0.1% DMSO) for 15 minutes, and then Stimulated with vehicle, oleic acid, linoleic acid, or GW9508. GW-1100 significantly reduced 300 μM oleic acid (AUC(60-150 s), p<0.05), 100 μM linoleic acid (AUC(60-150 s), p<0.05) and 10 μM GW9508 (AUC( 60 - 150 s), p<0.05); GW-1100 dose-dependently inhibited the GW9508- and linoleic acid-stimulated GPR40-mediated increase in Ca2+ (pIC50: 5.99±0.03 and 5.99±0.06)[3].

Intracerebroventricular administration of DHA (50 µg) and GW9508 (1.0 µg) significantly reduced mechanical and thermal hyperalgesia on day 7, but not on day 1, after CFA administration. These effects were inhibited by intracerebroventricular administration of the GPR40 antagonist GW-1100 (10 µg) [4].