Lipofermata is an inhibitor of fatty acid transport (IC50 = 4.84 μM in Caco-2 cells).1 It inhibits uptake of long- and very long-chain, but not medium-chain, fatty acids in mmC2C12, rnINS-1E, Caco-2, and HepG2 cells (IC50s = 3-6 μM).2 Lipofermata inhibits induction of BiP and CHOP, apoptosis, and lipid droplet accumulation, as well as reduces production of reactive oxygen species (ROS) and reverses decreases in glutathione (GSH) levels induced by palmitate in HepG2 and INS-1E cells. In vivo, lipofermata (500 mg/kg) inhibits absorption of 13C-oleate in mice.
1.Sandoval, A., Chokshi, A., Jesch, E.D., et al.Identification and characterization of small compound inhibitors of human FATP2Biochem. Pharmacol.79(7)990-999(2010) 2.Ahowesso, C., Black, P.N., Saini, N., et al.Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell deathBiochem. Pharmacol.98(1)167-181(2015)