PF-06446846 hydrochloride |
| カタログ番号GC38028 |
PF-06446846 塩酸塩は、プロタンパク質転換酵素サブチリシン/ケキシン 9 型 (PCSK9) の翻訳の経口活性で選択性の高い阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1632250-50-0
Sample solution is provided at 25 µL, 10mM.
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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].
PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM[1].
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]
[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.
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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