| Bioactivity | 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]. |
| Target | PCSK9 |
| Invitro | PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 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 and lowers total cholesterol levels[1]. Animal Model: |
| Name | PF-06446846 hydrochloride |
| CAS | 1632250-50-0 |
| Formula | C22H21Cl2N7O |
| Molar Mass | 470.35 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |