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: 2024-01-19 19:36:27
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	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

Molecular Formula	C₃₀H₃₃N₅O₂
Molecular Weight	495.62