Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,950 | 5日内发货 | ||
5 mg | ¥ 2,890 | 5日内发货 | ||
25 mg | ¥ 10,500 | 8-10周 | ||
50 mg | ¥ 13,700 | 8-10周 | ||
100 mg | ¥ 18,700 | 8-10周 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,180 | 5日内发货 |
产品描述 | CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3). |
靶点活性 | PDE4C2:0.56 μM, PDE4A5:0.29 μM, PDE4B2:0.08 μM, PDE4D3:0.09 μM |
体外活性 | CI-1044 selectively inhibits PDE4 crude extract from U937 cells (IC50: 0.27 μM). It being threefold more potent than rolipram (IC50=0.91 μM) and tenfold less potent than cilomilast (IC50=0.026 μM) in the same assay. For CI-1044, cilomilast and rolipram, the production of TNF-α is dose-dependently decreased with mean IC50 values from three separate experiments of 0.31±0.05, 0.26±0.05 and 0.11±0.01 μM, respectively, in the presence of PDE4 inhibitors. |
体内活性 | CI-1044 dose-dependently inhibits the accumulation of eosinophils in Bronchoalveolar lavages (BAL) fluids (ID50: 3.25 mg/kg). CI-1044 (p.o.) plasma levels increase proportionally with doses ranging between 0.1 and 40 mg/kg. Following repeated administration with CI-1044( p.o.), the ID50 value represents 0.5 mg/kg. TNF-α production is dose-dependently inhibited by CI-1044, rolipram, and cilomilast (ID50s: 0.4, 1.4, and 1.6 mg/kg) following single oral administration. A single dose treatment with CI-1044 (10 mg/kg, p.o.) 24, 8, 3, or 1 h before the antigen challenge induces 6, 56, 48, and 79% inhibition in the number of eosinophils in BAL. |
别名 | PD-189659 |
分子量 | 397.43 |
分子式 | C23H19N5O2 |
CAS No. | 197894-84-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (314.52 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5162 mL | 12.5808 mL | 25.1617 mL | 62.9042 mL |
5 mM | 0.5032 mL | 2.5162 mL | 5.0323 mL | 12.5808 mL | |
10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL | 6.2904 mL | |
20 mM | 0.1258 mL | 0.629 mL | 1.2581 mL | 3.1452 mL | |
50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2581 mL | |
100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.629 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CI-1044 197894-84-1 Metabolism PDE PD 189659 CI 1044 PD189659 PD-189659 CI1044 Inhibitor inhibitor inhibit