PF-06446846

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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。

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.