PCSK9-IN-30

PCSK9-IN-30 (Compound 3f), a PCSK9 inhibitor, effectively targets a cryptic binding groove on PCSK9, thereby preventing PCSK9 from associating with the low-density lipoprotein receptor (LDLR) (IC 50 = 537 nM) . This inhibition aids in the restoration of low-density lipoprotein (LDL) uptake by liver cells and significantly reduces plasma cholesterol levels. Demonstrating good bioavailability in mice, PCSK9-IN-30 holds potential for research within cardiovascular disease contexts.