Biological Activity
SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM[1][2].
The potent compound (SBC-115,337) shows an IC50 of 0.6 μM measured in an in vitro ELISA assay to monitor the effect of PCSK9 binding to the recombinant LDLR. SBC-115,337 at 1.2 μM induces more than tenfold upregulation of LDLR in HepG2 cells with respect to the control, increases uptake of fluorescently labeled DiI-LDL and loweres LDL-c levels in mice fed a high-fat diet[2].
References
[1]. Xu S, et al. Small molecules as inhibitors of PCSK9: Current status and future challenges. Eur J Med Chem. 2019;162:212-233. [2]. Lavecchia A, et al. Recent advances in developing PCSK9 inhibitors for lipid-lowering therapy. Future Med Chem. 2019;11(5):423-441.
