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PF-06446846

CAS No. 1632250-49-7

PF-06446846 ( —— )

产品货号. M22373 CAS No. 1632250-49-7

PF-06446846 是一种有效的选择性 PCSK9 抑制剂 PF-06446846 口服给药后可降低大鼠血浆 PCSK9 和总胆固醇水平。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥1077 有现货
5MG ¥1588 有现货
10MG ¥2390 有现货
25MG ¥4398 有现货
50MG ¥6342 有现货
100MG ¥8829 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    PF-06446846
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    PF-06446846 是一种有效的选择性 PCSK9 抑制剂 PF-06446846 口服给药后可降低大鼠血浆 PCSK9 和总胆固醇水平。
  • 产品描述
    PF?06446846 is a potent and selective PCSK9 inhibitor?PF-06446846 reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.?PF-06446846 is highly selective for the inhibition of PCSK9 translation.?The mechanism of action employed by PF-06446846 reveals a previously unexpected tunability of the human ribosome that allows small molecules to specifically block translation of individual transcripts.
  • 体外实验
    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. Cell Cytotoxicity Assay 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.
  • 体内实验
    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.
  • 同义词
    ——
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    PCSK9
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1632250-49-7
  • 分子量
    433.9
  • 分子式
    C22H20ClN7O
  • 纯度
    >98% (HPLC)
  • 溶解度
    ——
  • SMILES
    Clc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.Lintner N G , Mcclure K F , Donna P , et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain[J]. PLoS Biology, 2017, 15(3):e2001882-.
产品手册
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