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。
产品描述
PF-06446846 hydrochloride suppresses PCSK9 by inducing the ribosome to stall around codon 34. PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9.
体外活性
PF-06446846 suppresses the secretion of PCSK9 by Huh7 cells (IC50: 0.3 μM)[1].
体内活性
PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner. It also decreases total cholesterol levels[1].
Cas No.
1632250-50-0
分子式
C22H20CIN7O.XHCl
分子量
470.36
储存和溶解度
H2O:90.0 mg/mL (191.3 mM),Need ultrasonic
DMSO:225.0 mg/mL (478.4 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years