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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2200.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1000.0 |
| 规格： | 5 mg | 产品价格： | ￥2000.0 |
| 规格： | 10 mg | 产品价格： | ￥3000.0 |
| 规格： | 25 mg | 产品价格： | ￥5000.0 |
| 规格： | 50 mg | 产品价格： | ￥9000.0 |
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CP671305
CAS No. : 445295-04-5
MCE 国际站：CP671305
产品活性：CP671305 是一种有效的，可口服的，选择性的 phosphodiesterase-4-D 抑制剂，具有很高的活性。
研究领域：Metabolic Enzyme/Protease
作用靶点：Phosphodiesterase (PDE)
In Vitro: CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1. 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 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.
In Vivo: CP-671,305 pharmacokinetics 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).
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