| Description | PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression. |
| In vitro | PF-06446846 suppresses the secretion of PCSK9 by Huh7 cells (IC50: 0.3 μM)[1]. |
| In vivo | 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]. |
| molecular weight | N/A |
| Molecular formula | C22H20CIN7O.XHCl |
| CAS | 1632250-50-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: 90.0 mg/mL (191.3 mM), Sonication is recommended. DMSO: 225.0 mg/mL (478.4 mM), Sonication is recommended. |
| References | 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. |