Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions. IC50 & Target: GPR40, GPR84In Vitro: Setogepram (PBI-4050; 500 µM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation. Setogepram (PBI-4050; 250 or 500 µM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis. In Vivo: Setogepram (PBI-4050; 100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS-/-db/db mice.