PCSK9-IN-13

Modify Date: 2024-01-19 19:36:27

PCSK9-IN-13 Structure
PCSK9-IN-13 structure
Common Name PCSK9-IN-13
CAS Number 2244129-23-3 Molecular Weight 495.62
Density N/A Boiling Point N/A
Molecular Formula C30H33N5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PCSK9-IN-13


PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM[1].

 Names

Name PCSK9-IN-13

 PCSK9-IN-13 Biological Activity

Description PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM[1].
Related Catalog
In Vitro PCSK9-IN-13(compound 3f) (0.1 or 1 μM) 可剂量依赖性的恢复 HepG2 肝细胞对 LDL 的摄取[1]。
In Vivo PCSK9-IN-13(compound 3f) (3.28 or 16.4 mg/kg/day, s.c., 14 days) 在雄性 C57BL/6 小鼠中,剂量为 3.28 mg/kg 时,小鼠没有表现出总胆固醇降低,然而剂量为 16.4 mg/kg 时显示显著降低了总胆固醇血浆水平约 10%,并表现出优异的生物利用度[1]。
References

[1]. Benny J. Evison, et al. A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.Bioorganic & Medicinal Chemistry

 Chemical & Physical Properties

Molecular Formula C30H33N5O2
Molecular Weight 495.62