| Identification | Back Directory | [Name]
CP671305 | [CAS]
445295-04-5 | [Synonyms]
CS-2886
CP671305
UNII-9LH034R9R9
CP-671305; CP 671305; CP671305; UNII-9LH034R9R9;445295-04-5
Propanoic acid, 2-[4-[[[[2-(1,3-benzodioxol-5-yloxy)-3-pyridinyl]carbonyl]amino]methyl]-3-fluorophenoxy]-, (2R)- | [Molecular Formula]
C23H19FN2O7 | [MDL Number]
MFCD31382154 | [MOL File]
445295-04-5.mol | [Molecular Weight]
454.4 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 50 mg/ml; DMSO: 25 mg/ml; Ethanol: 3 mg/ml; PBS (pH 7.2): 2 mg/ml | [form ]
A crystalline solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
CP 671,305 is a potent inhibitor of phosphodiesterase 4D (PDE4D; IC50 = 3 nM). It is selective for PDE4D over PDE4A, -B, and -C (IC50s = 310, 287, and 3,858 nM, respectively), as well as over PDE1-3 and 5 (IC50s = >5,000 nM for all). CP 671,305 inhibits release of leukotriene E4 (LTE4; ) from eosinophils (IC50 = 52 nM) and LTB4 from neutrophils (IC50 = 106 nM). In vivo, CP 671,305 inhibits antigen-induced pulmonary eosinophil influx in cynomolgus monkeys in a dose-dependent manner. | [Uses]
CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities. | [in vivo]
CP-671,305 pharmacokinetics are largely unaltered, and compromised biliary clearance of CP-671,305 is compensated by increased urinary clearance[1]. 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)[2]. | [References]
[1] Kalgutkar AS, et al. 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. Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8. DOI:10.1124/dmd.107.016162
[2] Kalgutkar AS, et al. Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species. Xenobiotica. 2004 Aug;34(8):755-70. DOI:10.1080/00498250400005682 |
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| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
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