PeptideDB

PF-06446846 hydrochloride

CAS: 1632250-50-0 F: C22H21Cl2N7O W: 470.35

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase sub
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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.