BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain[1].
BI-0115 efficiently reduces oxLDL internalization in the cellular context. The IC50 values of the cellular assay (5.4 µM) are in good agreement with the determined Kd values in SPR (4.3 µM) and ITC (6.99 µM)[1].
[1]. Schnapp, G., et al. A small-molecule inhibitor of lectin-like oxidized LDL receptor-1 acts by stabilizing an inactive receptor tetramer state. Commun Chem 3, 75 (2020).