Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CP671305 是口服具有活力的 phosphodiesterase-4-D 选择性抑制剂,具有很高的活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 683 | 现货 | ||
5 mg | ¥ 1,660 | 现货 | ||
10 mg | ¥ 2,490 | 现货 | ||
25 mg | ¥ 4,160 | 现货 | ||
50 mg | ¥ 5,880 | 现货 | ||
100 mg | ¥ 7,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,680 | 现货 |
产品描述 | CP671305 is an orally active, potent and selective inhibitor of phosphodiesterase-4-D. |
体外活性 | CP-671,305 is a substrate of human OATP2B1 with a high affinity (Km=4 μM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. CP-671,305 displays high affinity (Km=12 μM) for rat hepatic Oatp1a4. CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC50s >?50 μM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305. |
体内活性 | The pharmacokinetics of CP-671,305 are largely unaltered, and compromised biliary clearance of CP-671,305 is compensated by increased urinary clearance. CP-671,305 demonstrates generally favourable pharmacokinetic properties, systemic plasma clearance after intravenous administration is low in Sprague-Dawley rats (9.60?±?1.16?mL/min/kg), beagle dogs (2.90?±?0.81?mL/min/kg) and cynomolgus monkeys (2.94?±?0.87?mL/min/kg) resulting in plasma half-lives >?5?h. Moderate to high bioavailability in rats (43-80%), dogs (45%) and monkeys (26%) is observed after oral dosing. In rats, oral pharmacokinetics are dose dependent over the dose range studied (10 and 25?mg/kg). |
动物实验 | Jugular vein cannulated and bile duct-exteriorized male Sprague-Dawley rats (230-250 g) are used in the assay. All animals are fasted overnight before dosing, whereas access to water is provided ad libitum. Animals are fed following collection of the 2-h blood samples. CP-671,305 (3 mg/kg) in glycerol formal is administered intravenously (i.v.) via the jugular vein to three rats over 30 s, and serial plasma samples are collected before dosing and 0.033, 0.15, 0.5, 1, 2, 4, 6, 8, and 24 h after dosing. All plasma samples are kept frozen until analysis. In addition, an i.v. dose of 3 mg/kg is also given to bile duct-exteriorized rats (n=3), where plasma, bile, and urine samples are collected on ice for up to 24 h and stored at -20°C until analysis. For the DDI studies, cyclosporin A (20 mg/kg in glycerol formal) is administered i.v. 30 min before intravenous administration of CP-671,305. Rifampicin (50 mg/kg) in saline is administered i.v. 5 min before the administration of CP-671,305. Plasma samples from the various pharmacokinetic studies are generated by centrifugation at 3000 rpm for 10 min at 4°C. Samples are stored at -20°C, pending analysis by LC-MS/MS. |
分子量 | 454.4 |
分子式 | C23H19FN2O7 |
CAS No. | 445295-04-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: > 150 mg/mL (330.11 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2007 mL | 11.0035 mL | 22.007 mL | 55.0176 mL |
5 mM | 0.4401 mL | 2.2007 mL | 4.4014 mL | 11.0035 mL | |
10 mM | 0.2201 mL | 1.1004 mL | 2.2007 mL | 5.5018 mL | |
20 mM | 0.11 mL | 0.5502 mL | 1.1004 mL | 2.7509 mL | |
50 mM | 0.044 mL | 0.2201 mL | 0.4401 mL | 1.1004 mL | |
100 mM | 0.022 mL | 0.11 mL | 0.2201 mL | 0.5502 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。
CP671305 445295-04-5 Metabolism PDE Inhibitor CP 671305 Phosphodiesterase (PDE) inhibit CP-671305 inhibitor