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CP671305

Cat. No. M9679
CP671305 Structure
Synonym:

CP-671,305

Size Price Availability
10mg USD 198 4-7 Days
25mg USD 328 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 454.40
Formula C23H19FN2O7
CAS Number 445295-04-5
Purity >99%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C
References

Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human
Amit S Kalgutkar, et al. Dτυg Metab Dispos. 2007 Nov;35(11):2111-8. PMID: 17686907.

Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species
A S Kalgutkar, et al. Xenobiotica. 2004 Aug;34(8):755-70. PMID: 15690763.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CP671305, CP-671,305 supplier, PDE, inhibitors

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