PF-06815345 hydrochloride

Modify Date: 2024-01-11 16:54:27

PF-06815345 hydrochloride Structure
PF-06815345 hydrochloride structure
Common Name PF-06815345 hydrochloride
CAS Number 2334434-49-8 Molecular Weight 634.49
Density N/A Boiling Point N/A
Molecular Formula C27H30Cl2FN9O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF-06815345 hydrochloride


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].

 Names

Name PF-06815345 hydrochloride

 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
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