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PF-06446846
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-06446846图片
CAS NO:1632250-49-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PF-06446846 是一个具有口服活性的PCSK9抑制剂。PF-06446846通过在密码子区域附近阻滞 80S ribosome,直接和选择性地抑制 PCSK9 的翻译。
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[1].

体外研究
(In Vitro)

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50of 0.3 μM[1].PF-06446846 inhibits PCSK9(1–35)-luciferase expression with an IC50of 2 μM[1].PF-06446846 (Compound 7f) shows rat bone marrow and human CD34+toxicity[2].

Cell Cytotoxicity Assay[2]

Cell Line:Rat bone marrow lineage (–) cell and CD34+cell
Concentration:0-20 μM
Incubation Time:72 h
Result:Showed cytotoxicity with IC50values of 2.9 μM and 2.7 μM against rat Lin(–) and human CD34+, respectively.
体内研究
(In Vivo)

PF-06446846 reduces circulating PCSK9 and total plasma cholesterol levels in vivo without obvious toxicity[1].

Animal Model:Male Sprague-Dawley (Crl:CD [SD] rats, five per group; 6–8 wk old at initiation of dosing)[1]
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.
分子量

433.89

Formula

C22H20ClN7O

CAS 号

1632250-49-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.