GPR40 agonist 6

GPR40 agonist 6 (Compound 7a) is a potent and selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist with an EC50 of 0.058 μM[1].

Signaling Pathways >> GPCR/G Protein >> GPR40

Research Areas >> Metabolic Disease

EC50: 0.058 μM (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 aEach value is an average of n = 4, measured at c = 1 µM. bEach value is an average of n = 2. cEach value is an average of n = 5, measured at c = 2 µM. dEach value is an average of n = 2, measured at c = 10 µM.

[1]. Zahanich I, et al. Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40). Bioorg Med Chem Lett. 2015 Aug 15;25(16):3105-11.