2244129-23-3

2244129-23-3 structure
2244129-23-3 structure
  • Name: PCSK9-IN-13
  • Chemical Name: PCSK9-IN-13
  • CAS Number: 2244129-23-3
  • Molecular Formula: C30H33N5O2
  • Molecular Weight: 495.62
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
  • Create Date: 2023-04-20 14:28:05
  • Modify Date: 2025-09-21 06:11:37
  • 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].

Name PCSK9-IN-13
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

Molecular Formula C30H33N5O2
Molecular Weight 495.62
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