BI 01383298

BI 01383298 (CAS No.: 2227549-00-8) is a selective small-molecule chemical probe that functions as a potent inhibitor of the sodium-coupled citrate transporter SLC13A5 (also known as NaCT), a transporter highly expressed in hepatic tissue and implicated in cellular energy metabolism and lipid biosynthesis. By blocking sodium-dependent citrate uptake, BI 01383298 disrupts intracellular citrate homeostasis, thereby modulating metabolic pathways linked to glycolysis, lipogenesis, and tumor cell proliferation. The compound demonstrates strong in vitro activity in the nanomolar range, with reported inhibitory potency in cell-based systems such as HEK and HepG2 cells, and exhibits selective inhibition of citrate transport without affecting the uptake of structurally unrelated substrates, indicating a high degree of target specificity. Mechanistically, its inhibitory effect on SLC13A5 has been associated with reduced metabolic flux through citrate-dependent pathways, making it a valuable tool for investigating metabolic regulation in liver physiology and cancer biology. BI 01383298 is widely applied in biochemical and cellular studies to probe citrate transport function, assess metabolic vulnerabilities, and support drug discovery efforts targeting metabolic disorders and oncology, with experimental concentrations typically optimized according to specific assay conditions and research objectives.