PCSK9-IN-10 (C09-1164-131)

PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC 50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia.In VitroPCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 µM; 24 h) significantly decreases the PCSK9 protein expression and increases the expression of LDL receptor (LDLR) in a dose dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: HepG2 cells Concentration: 0-1000 µM Incubation Time: 24 h Result: Showed low cytotoxicity to HepG2 cells. Western Blot AnalysisCell Line: HepG2 cells Concentration: 0, 2.5, 5, 12.5, 25 µM Incubation Time: 24 h Result: Significantly decreased PCSK9 protein level in a dose dependent manner.In VivoPCSK9-IN-10 (30 mg/kg; p.o.; once a day for 8 weeks) reduces total cholesterol (TC) and atherosclerotic plaque size in ApoE KO mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Eight weeks old male ApoE KO mice Dosage: 30 mg/kg Administration: P.o.; once a day for 8 weeks Result: Inhibited both hepatic and serum PCSK9 content obviously and reduced reduced atherosclerotic plaque size.Form:Solid. Specification: 0.98 Molecular Formula: C18H23N5O4 Molecular Weight: 373.41