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首页-小分子抑制剂&激动剂-Others-PCSK9-AZD0780
AZD0780

Chemical Structure : AZD0780

CAS No.: 2455427-91-3

AZD0780 (AZD-0780)

货号: PC-24525Not For Human Use, Lab Use Only.

AZD0780 (AZD-0780) is a potent, orally bioavailable inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with Kd of <200 nM, binds to a novel pocket in the PCSK9 C-terminal domain and does not affect the PCSK9-LDL receptor (LDLR) interaction.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD0780 (AZD-0780) is a potent, orally bioavailable inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with Kd of <200 nM, binds to a novel pocket in the PCSK9 C-terminal domain and does not affect the PCSK9-LDL receptor (LDLR) interaction.
AZD0780 inhibits lysosomal trafficking of PSCK9-LDLR complexes and prevents PCSK9-induced LDLR degradation.
AZD0780 demonstrated robust, dose-dependent reductions in LDL-C with a favorable safety and tolerability profile supporting further development of this once daily, oral treatment in clinical investigations.

物理化学性质&存储条件

分子量 414.42
分子式 C20H20F2N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6'-(((1S,3S)-3-((5-(Difluoromethoxy)pyrimidin-2-yl)amino)cyclopentyl)amino)-2H-[1,3'-bipyridin]-2-one

参考文献

1. Koren MJ, et al. J Am Coll Cardiol. 2025 Mar 27:S0735-1097(25)05907-8.

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