CP671305

SKU: orb1222255

Description

CP-671305 is a potent and selective inhibitor of phosphodiesterase 4.

Key Properties

• CAS Number: 445295-04-5
• MW: 454.4
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₉FN₂O₇
• SMILES: O=C(O)[C@@H](C)Oc4ccc(CNC(=O)c3cccnc3Oc1ccc2OCOc2c1)c(F)c4
• Target: PAK
• Solubility: DMSO : ≥ 160 mg/mL; 352.11 mM

Bioactivity

• 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).
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP-671305 | CP 671305 | CP671305 | UNII-9LH034R9R9

Quick Database Links

Gene Symbol

PAK