| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S88345-5mg |
≥98%(HPLC) | ￥492.00 | 4 | - | - | - |
|
S88345-10mg |
≥98%(HPLC) | ￥645.00 | 1 | - | - | - |
|
S88345-25mg |
≥98%(HPLC) | ￥1090.00 | 3 | - | - | - |
|
S88345-50mg |
≥98%(HPLC) | ￥1750.00 | 3 | - | - | - |
|
S88345-100mg |
≥98%(HPLC) | ￥3140.00 | 货期：3-5天 | - | - | - |
|
| 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： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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