| Name | PF-06446846 hydrochloride |
|---|---|
| Synonyms |
Benzamide, N-(3-chloro-2-pyridinyl)-N-[(3R)-3-piperidinyl]-4-(3H-1,2,3-triazolo[4,5-b]pyridin-3-yl)-
N-(3-Chloro-2-pyridinyl)-N-[(3R)-3-piperidinyl]-4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzamide |
| Description | 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[1] |
| In Vitro | 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: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)[1] 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. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 655.5±65.0 °C at 760 mmHg |
| Molecular Formula | C22H20ClN7O |
| Molecular Weight | 433.893 |
| Flash Point | 350.2±34.3 °C |
| Exact Mass | 433.141785 |
| LogP | 1.86 |
| Appearance | powder,white to beige |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Index of Refraction | 1.745 |
| Storage condition | room temp |