PCSK9-IN-13

Names

[ CAS No. ]:
2244129-23-3

[ Name ]:
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]:

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

[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

Related Compounds