tcsc0023823 FAA1 agonist-1

FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC₅₀ of 7.54.

IC50 & Target: pEC₅₀: 7.54 (FFA1/GPR40)^[1]

In Vitro: FAA1 agonist-1 (compound 20) (10 mg/kg) presents superior pharmacokinetic (PK) profiles, in particular, a high maximum concentration (C_max=2563.52 μg/L), low clearance (CL=0.154 L/h/kg), long plasma half-life (T_1/2=5.57 h) and results in a high exposure (AUC_0-24h=30204.43 μg/L•h). FAA1 agonist-1 also tends to have a low risk of activating caspase-3/7^[1].

In Vivo: Single oral administration of FAA1 agonist-1 (compound 20) robustly reduces the plasma glucose excursion and enhances insulin secretion during an oral glucose tolerance test (OGTT) in a dose-dependent manner from 1 to 10 mg/kg when FAA1 agonist-1 is dosed 60 min prior to the oral glucose challenge. The area under the curve of blood glucose (AUC_0-120min) and blood insulin (AUC_0-120min) reveal that the minimum effective dose of FAA1 agonist-1 is 3 mg/kg. The hyperglycemia state is also markedly improved in FAA1 agonist-1 (20 mg/kg) treated group^[1].