PCSK9-IN-10 is a potent and orally active inhibitor of PCSK9, (IC50: 6.4 µM).PCSK9-IN-10 increases LDLR protein expression and decreases PCSK9 expression.PCSK9-IN-10 slows the progression of atherosclerosis.PCSK9-IN-10 has the potential to investigate hyperlipidemia.CSK9 -IN-10 significantly decreased protein expression and increased LDLR receptor expression in a dose-dependent manner.PCSK9-IN-10 showed low cytotoxicity against HepG2, inhibited liver and serum PCSK9 levels, and reduced atherosclerotic plaque size.