PF-06446846 hydrochloride 是一种具有口服活性，高选择性前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 的翻译抑制剂。PF-06446846 hydrochloride 可通过诱导核糖体停在密码子 34 周围，从而抑制 PCSK9。
货号:ajcx14206
CAS:1632250-50-0
分子式:C22H20ClN7O.xHCl
分子量：N/A
溶解度:DMSO : 250 mg/mL (531.52 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34[1].

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM[1].

PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner and lowers total cholesterol levels[1]. Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)[1]

[1]. Lintner NG, et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain. PLoS Biol. 2017 Mar 21;15(3):e2001882.