产品
编 号:F196303
分子式:C22H21Cl2N7O
分子量:470.35
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
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.

体内研究:
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.Animal Model:Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)
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.

体外研究:
PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM.
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