
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)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥1077 | 有现货 |
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5MG | ¥1588 | 有现货 |
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10MG | ¥2390 | 有现货 |
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25MG | ¥4398 | 有现货 |
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50MG | ¥6342 | 有现货 |
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100MG | ¥8829 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称PF-06446846
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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
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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。
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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.
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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.
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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.
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同义词——
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通路Others
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靶点Other Targets
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受体PCSK9
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研究领域——
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适应症——
化学信息
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CAS Number1632250-49-7
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分子量433.9
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分子式C22H20ClN7O
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纯度>98% (HPLC)
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溶解度——
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SMILESClc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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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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