Lipofermata

Lipofermata (CAS No.: 297180-15-5) is a small-molecule inhibitor of fatty acid transport protein 2 (FATP2), widely used as a chemical probe to investigate lipid uptake and metabolic regulation in mammalian systems. It effectively suppresses cellular uptake of long- and very long-chain fatty acids across multiple cell types, including Caco-2, HepG2, INS-1E, and myoblast-derived models, with inhibitory activity in the low micromolar range and a reported IC50 of approximately 4.84 μM in Caco-2 cells. Mechanistically, Lipofermata modulates lipid metabolism-associated stress responses, attenuating palmitate-induced endoplasmic reticulum stress markers such as BiP and CHOP, reducing reactive oxygen species production, preventing glutathione depletion, and limiting lipid droplet accumulation and apoptosis. In vivo studies further demonstrate its capacity to inhibit dietary fatty acid absorption, supporting its relevance in metabolic research. In addition to its role in lipid transport inhibition, Lipofermata, as a spiro-indoline-thiadiazole derivative, exhibits zinc-dependent antibacterial activity by disrupting zinc homeostasis in Escherichia coli, with a minimum inhibitory concentration in the micromolar range around 16 μM. These combined properties make Lipofermata a versatile tool for studying fatty acid metabolism, oxidative stress, and host–microbe interactions, with experimental concentrations or dosing regimens typically adjusted according to specific cellular or animal model requirements.