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CP671305

CAS No. : 445295-04-5

MCE 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 (K_m=4 μM) but not a substrate for human OATP1B1 or OATP1B3. CP-671,305 displays high affinity (K_m=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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