PCSK9-IN-10

Modify Date: 2024-01-10 20:54:57

PCSK9-IN-10 Structure
PCSK9-IN-10 structure
Common Name PCSK9-IN-10
CAS Number 368434-98-4 Molecular Weight 373.41
Density N/A Boiling Point N/A
Molecular Formula C18H23N5O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PCSK9-IN-10


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].

 Names

Name PCSK9-IN-10

 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
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