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CP671305 is a potent and selective, orally active inhibitor of phosphodiesterase-4-D with high activities. CP-671305 displays high affinity (Km=12 μM) for rat hepatic Oatp1a4. CP-671305 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.
| Molecular Weight | 454.40 |
| Formula | C23H19FN2O7 |
| CAS Number | 445295-04-5 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDE Products |
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GSK256066 is a selective phosphodiesterase 4 (PDE4)inhibitor with an IC50 of 3.2 pM. *The compound is unstable in solutions, freshly prepared is recommended |
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| Roflumilast
Roflumilast (APTA-2217; BYK 20869; B9302-107) is a novel and selective, long-acting inhibitor of phosphodiesterase 4 (PDE-4). |
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