Fezagepras 是一种可口服的GPR40激动剂和GPR84拮抗剂或反向激动剂。它减轻肾、肝和胰腺纤维化，具有抗纤维化、抗炎和抗增殖作用。

Setogepram is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation inhibited by Setogepram (PBI-4050; 500 μM; 24 hours). Setogepram (PBI-4050; 250 or 500 μM; 24hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis [2].

In type 2 diabetes eNOS-/-db/db mice, Setogepram (PBI-4050; 100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improve glucose tolerance [1].

1002101-19-0

C13H18O2

206.28

Setogepram;3-戊基苯乙酸;PBI-4050

DMSO:60 mg/ml (290.87 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years