产品
编 号：F196302
分子式：C22H20ClN7O
分子量：433.89
分子式：C22H20ClN7O
分子量：433.89
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CAS No: 1632250-49-7
产品详情
生物活性：
PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region.
体内研究：
PF-06446846 reduces circulating PCSK9 and total plasma cholesterol levels in vivo without obvious toxicity.Animal Model:Male Sprague-Dawley (Crl:CD [SD] rats, five per group; 6–8 wk old at initiation of dosing)
Dosage:5, 15, and 50 mg/kg
Administration:Oral administration, daily, 14 days
Result:Reduced plasma PCSK9, total plasma cholesterol, and LDL-C (low-density lipoprotein cholesterol) in a dose-dependent manner without obvious toxicity.
体外研究：
PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM.PF-06446846 inhibits PCSK9(1–35)-luciferase expression with an IC50 of 2 μM.PF-06446846 (Compound 7f) shows rat bone marrow and human CD34+ toxicity.
PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region.
体内研究：
PF-06446846 reduces circulating PCSK9 and total plasma cholesterol levels in vivo without obvious toxicity.Animal Model:Male Sprague-Dawley (Crl:CD [SD] rats, five per group; 6–8 wk old at initiation of dosing)
Dosage:5, 15, and 50 mg/kg
Administration:Oral administration, daily, 14 days
Result:Reduced plasma PCSK9, total plasma cholesterol, and LDL-C (low-density lipoprotein cholesterol) in a dose-dependent manner without obvious toxicity.
体外研究：
PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM.PF-06446846 inhibits PCSK9(1–35)-luciferase expression with an IC50 of 2 μM.PF-06446846 (Compound 7f) shows rat bone marrow and human CD34+ toxicity.
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