GPR40 agonist 6 (Compound 7a) is a potent and selective agonist of free fatty acid receptor 1 ( FFAR1 or GPR40 ) with an EC 50 of 0.058 μM against GPR40 [1].

GPR40 agonist 6 (Compound 7a) shows a very favorable ADME profile, and shows no significant inhibition of the principal cytochrome P450 isoforms (1A2, 2C9, 2C19, 2D6 and 3A4) at 5 μM [1]. ADME profile for GPR40 agonist 6 (Compound 7a) [1] GPR40 agonist 6 (Compound 7a) Plasma protein binding (human) a 98.6% Aqueous solubility (PBS, pH 7.4) b 404 μM Microsomal stability (mouse, t1/2) c 434 min A-B permeability (Caco-2, cm s -1 ) d 15.2 10 -6 a Each value is an average of n = 4, measured at c = 1 μM. b Each value is an average of n = 2. c Each value is an average of n = 5, measured at c = 2 μM. d Each value is an average of n = 2, measured at c = 10 μM.