<Suppliers Price>

PCSK9-IN-10

Names

[ CAS No. ]:
368434-98-4

[ Name ]:
PCSK9-IN-10

Biological Activity

[Description]:

PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 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[1].

[Related Catalog]:

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

[In Vitro]

PCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 µM; 24 h) 以剂量依赖性方式显著降低 PCSK9 蛋白表达并增加 LDL 受体 (LDLR) 的表达[1]。 Cell Cytotoxicity Assay[1] Cell Line: HepG2 cells Concentration: 0-1000 µM Incubation Time: 24 h Result: Showed low cytotoxicity to HepG2 cells. Western Blot Analysis[1] Cell 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 Vivo]

PCSK9-IN-10 (30 mg/kg；口服；每天一次，持续 8 周) 降低 ApoE KO 小鼠的总胆固醇 (TC) 和动脉粥样硬化斑块大小[1]。 Animal Model: Eight weeks old male ApoE KO mice[1] 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.

[References]

[1]. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. Eur J Med Chem. 2022 Dec 26;247:115047.  

Chemical & Physical Properties

[ Molecular Formula ]:
C18H23N5O4

[ Molecular Weight ]:
373.41

Related Compounds