PCSK9-IN-13 (compound 3f) is a potent PCSK9 inhibitor with an IC50 of 537 nM. It antagonizes the binding of the low-density lipoprotein receptor (LDLR) to PCSK9 by interacting with a cryptic binding groove on the PCSK9 protein. Since PCSK9 normally mediates the degradation of LDLR, this inhibitor helps maintain higher levels of LDLR on the hepatocyte surface, thereby promoting the uptake of circulating LDL-C. It is a valuable tool for researching novel cholesterol-lowering therapies and cardiovascular disease prevention.
Molekulargewicht:
495.62
CAS Nummer:
[2244129-23-3]
Formel:
C30H33N5O2
Target-Kategorie:
Others
T73008
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