PF-06815345 hydrochloride

Names

[ CAS No. ]:
2334434-49-8

[ Name ]:
PF-06815345 hydrochloride

Biological Activity

[Description]:

PF-06815345 hydrochloride is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 hydrochloride significantly decreases the PCSK9 level in vivo in mouse[1][2].

[Related Catalog]:

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

[In Vitro]

PF-06815345 hydrochloride（实施例 7）（1-30 μM；5-1440 分钟）在人肠细胞和肝细胞中的 CLint 值分别为 <82.9 μL/min/mg 和 97.6 μL/min/mg[2].

[In Vivo]

PF-06815345 hydrochloride（实施例 7）（100-500 mg/kg；口服；单剂量）降低人源化 PCSK9 小鼠模型中的 PCSK9 水平。处理 4 小时后，以 500 mg/kg 的剂量将血浆 PCSK9 降低了 72%[2]。

[References]

[1]. Akin A, et al. Overcoming the Challenges of Making a Single Enantiomer N-1 Substituted Tetrazole Prodrug Using a Tin-Mediated Alkylation and Enzymatic Resolution[J]. Organic Process Research & Development, 2019, 23(6): 1167-1177.

[2]. Darout E, et al. Preparation of substituted amide compounds as PCSK9 inhibitors: Canada, CA2907071 A1 2016-04-08.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H30Cl2FN9O4

[ Molecular Weight ]:
634.49

Related Compounds