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SBC-115337

Names

[ CAS No. ]:
423148-46-3

[ Name ]:
SBC-115337

Biological Activity

[Description]:

SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease
Research Areas >> Cancer

[Target]

IC50: 0.5 μM (PCSK9)[1]


[In Vitro]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H19N3O4

[ Molecular Weight ]:
473.48


Related Compounds