A Novel Antidiabetic Drug, Fasiglifam/TAK-875, Acts as an Ago-Allosteric Modulator of FFAR1
Figure 1
Partial agonist activity of fasiglifam is affected by FFAR1/GPR40 expression levels.
(A) The chemical structure of fasiglifam. (B and C) FFAR1 agonist activities of fasiglifam and free fatty acids (FFAs) in the intracellular Ca2+ mobilization assay using CHO cell lines expressing hFFAR1 (clone #104) (B) or mFFAR1 (C). Data are representative of three experiments. (D) hFFAR1 mRNA levels of hFFAR1-expressing CHO clones were evaluated by qRT-PCR. (E-H) Relative Ca2+ influx activities of γ-LA and fasiglifam in CHO clones #104 (E), #19 (F), #2 (G), and #4 (H) with various hFFAR1 expression levels. Error bars indicate s.e.m. (n = 3).