PF-06815345_product_DataBase

Bioactivity	PF-06815345 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 significantly decreases the PCSK9 level in vivo in mouse[1][2].
Target	IC50: >20 μM (cell based), 13.4 (cell free) for Proprotein convertase subtilisin/kexin type 9 (PCSK9)
Invitro	PF-06815345（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（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]。
Name	PF-06815345
CAS	1900686-46-5
Formula	C27H29ClFN9O4
Molar Mass	598.03
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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