PBI-4050 (sodium salt)

PBI-4050 is an agonist of free fatty acid receptor 1 (FFAR1/GPR40) and an antagonist of G protein-coupled receptor 84 (GPR84).¹ It induces β-arrestin-2 recruitment in a reporter assay using HEK293 cells expressing human FFAR1/GPR40 (EC₅₀ = 275 µM). PBI-4050 inhibits activation of GPR84 induced by decanoic acid (Item No. 20838) or embelin (Item No. 11838) in reporter assays using HEK293 cells expressing the human receptor (IC₅₀s = 398 and 209 µM, respectively). In vivo, PBI-4050 (200 mg/kg) decreases renal histological lesion scores in a mouse model of doxorubicin-induced nephrotoxicity. It also reduces tissue fibrosis in several additional in vivo rodent models, including carbon tetrachloride-induced hepatotoxicity and bleomycin-induced pulmonary fibrosis. PBI-4050 (100 mg/kg) decreases albuminuria, prevents decreases in the glomerular filtration rate (GFR) and podocyte numbers, and reduces blood glucose levels in a model of accelerated type 2 diabetes using eNos^-/- db/db mice.²

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1. Gagnon, L., Leduc, M., J.-F., T., et al. A newly discovered antifibrotic pathway regulated by two fatty acid receptors: GPR40 and GPR84. Am. J. Pathol. 188(5), 1132-1148 (2018).

2. Li, Y., Chung, S., Li, Z., et al. Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control. JCI Insight 3(10), e120365 (2018).