2. Metabolic Enzyme/Protease
  3. PCSK9
  4. PF-06446846

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。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 PF-06446846 hydrochloride。

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PF-06446846 Chemical Structure

PF-06446846 Chemical Structure

CAS No. : 1632250-49-7

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PF-06446846 的其他形式现货产品:

Customer Review

Other Forms of PF-06446846:

PF-06446846 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Bone marrow cell IC50
1.2 μM
Compound: 7f; PF-06446846
Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
[PMID: 29878763]
HeLa IC50
0.5 μM
Compound: 14; PF-06446846
Inhibition of PCSK9 expression in human HeLa cells after overnight incubation by ELISA
Inhibition of PCSK9 expression in human HeLa cells after overnight incubation by ELISA
[PMID: 29519739]
Huh-7 IC50
0.3 μM
Compound: 3; PF-06446846
Binding affinity to 80S ribosome in human HuH7 cells expressing human C-terminal V5/6-His-tagged PCSK9 assessed as inhibition of PCSK9 secretion after 16 to 24 hrs by AlphaLISA method
Binding affinity to 80S ribosome in human HuH7 cells expressing human C-terminal V5/6-His-tagged PCSK9 assessed as inhibition of PCSK9 secretion after 16 to 24 hrs by AlphaLISA method
[PMID: 30448414]
Huh-7 IC50
0.38 μM
Compound: 7f; PF-06446846
Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
[PMID: 29878763]
Huh-7 IC50
0.82 μM
Compound: 7f; PF-06446846
Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA
Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA
[PMID: 29878763]
IEC-6 IC50
> 20 μM
Compound: 7f; PF-06446846
Cytotoxicity against rat IEC-6 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay
Cytotoxicity against rat IEC-6 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo assay
[PMID: 29878763]
体外研究
(In Vitro)

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM[1]. PF-06446846 inhibits PCSK9(1–35)-luciferase expression with an IC50 of 2 μM[1]. PF-06446846 (Compound 7f) shows rat bone marrow and human CD34+ toxicity[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PF-06446846 相关抗体:

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 IC50 values 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

PF-06446846 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-064468461632250-49-7PF06446846PF 06446846PCSK9Proprotein convertase subtilisin/kexin type 9Selective80S ribosomeHuh7Rat bone marrowInhibitorinhibitorinhibit

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