• 产品描述： PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34

• 靶点： PCSK9

• 体外研究：
  PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM。

• 体内研究：
  PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner. It also decreases total cholesterol levels。 Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing) Dosage: 5, 15, and 50 mg/kg Administration: Oral gavage; daily for 14 days Result: Lowered plasma PCSK9 in a dose-dependent manner and lowered total cholesterol levels.

• 参考文献：
  1. Lintner NG, et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain. PLoS Biol. 2017 Mar 21;15(3):e2001882.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.126 ml	10.63 ml	21.261 ml
  5 mM	0.425 ml	2.126 ml	4.252 ml
  10 mM	0.213 ml	1.063 ml	2.126 ml
  50 mM	0.043 ml	0.213 ml	0.425 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *