FABP4-IN-3 (Compound C3) is a highly selective inhibitor of FABP4, with an inhibition constant (Ki) of 25 ± 3 nM for FABP4 and a Ki of 15.03 μM for FABP3, showcasing a selectivity factor of 601 times over FABP3. It also demonstrates metabolic stability and potent anti-inflammatory activity in cells, making it a promising candidate for research in metabolic disorders, cardiac dysfunction, and inflammation-related diseases.

FABP4-IN-3 exhibits significant metabolic stability in human and mouse microsomes, with half-lives of 165 minutes and 131 minutes, respectively. At a concentration of 100μM for 24 hours, FABP4-IN-3 shows no cytotoxic effects on the viability of THP-1 macrophages. Additionally, at concentrations of 5-20μM for 18 hours, FABP4-IN-3 demonstrates a clear, dose-dependent inhibition of the production of the inflammatory cytokine MCP-1.