• 产品描述： PF-05175157是一种广谱有效的ACC抑制剂，对人ACC1，人ACC2，大鼠ACC1和大鼠ACC2的IC50分别为27.0 nM、33.0 nM、23.5 nM和50.4 n

• 靶点： rACC1(Cell-free assay):23.5 nM;hACC1(Cell-free assay):27.0 nM;hACC2(Cell-free assay):33.0 nM;rACC2(Cell-free assay):50.4 nM;Acetyl-CoACarboxylase

• 体内研究：
  In vivo, the plasma clearance of PF-05175157 is low following intravenous (iv) administration (1 mg/kg) to rats, dogs, and monkeys. Oral (po) administration (3 mg/kg) to rats and dogs showed bioavailability of 40% and 54%, respectively, consistent with the low microsomal clearance and good solubility at low pH. The bioavailability following a 50 mg/kg oral dose in rats was 106%, suggesting saturation of clearance. Formation of the direct product of ACC, malonyl-CoA, in the skeletal muscle and liver of lean Sprague Dawley rats is assessed 1 h following an acute oral dose of PF-05175157, showing concentration-dependent reductions in both skeletal muscle and liver malonyl-CoA. At the nadir, quadriceps and liver malonyl-CoA levels are reduced by 76% and 89%, respectively.

• 细胞实验： Cell lines: rat hepatocytes Concentrations: -- Incubation Time: 5 h Method: On the day of the study, media was aspirated and cells are treated with fresh MCM media containing DMSO vehicle or varying concentrations of PF-05175157 as indicated. Compound was initially dissolved in DMSO and subsequently diluted 1:100 in MCM.After 5 h at 37 °C, incubation media is removed and the experiment is terminated by washing the cells with ice cold PBS.

• 动物实验： Animal Models: Male SD rats Dosages: 0.25mg/kg, 0.5mg/kg, 1mg/kg, 2mg/kg, 4mg/kg, 8mg/kg, 15mg/kg, 25mg/kg, 50mg/kg and 100 mg/kg Administration: Oral

• 参考文献：
  1. David A Griffith,et al.J Med Chem.2014;57 (24): 10512-10526.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.466 ml	12.331 ml	24.662 ml
  5 mM	0.493 ml	2.466 ml	4.932 ml
  10 mM	0.247 ml	1.233 ml	2.466 ml
  50 mM	0.049 ml	0.247 ml	0.493 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 *