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
In Vitro
PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC 50 of 0.3 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing) Dosage: 5, 15, and 50 mg/kg Administration: Oral gavage; daily for 14 days Result: Lowered plasma PCSK9 in a dose-dependent manner and lowered total cholesterol levels.