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CDP 840 hydrochloride

Catalog No.
B7539
PDE4 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mg
$322.00
Ship with 5-10 days
50mg
$1,308.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

CDP 840 is a selective phosphodiesterase type IV (PDE4) inhibitor [1] [2] [3] with an IC50 value of 0.007 µM [4].

PDE4 is most abundantly distributed in inflammatory cells such as monocytes and macrophages [3]. PDE4 is a high-affinity cAMP-selective isozyme. It was found that PDE4 was in almost all cell types in asthma pathogenesis [2].

CD P840 showed a potent inhibition against PDE4 with IC50 values ranging from 2-30 nM to different isoenzymes of PDE4. There are four expressed PDE4 isoenzymes in baculovirus cells, i.e. PDE4A, PDE4B, PDE4C and PDE4D. Except for PDE4C2, CDP 840 did not exhibit isoform selectivity of PDE4. CD P840 exhibited a hill number of about 1.0 against all four PDE4 isoenzymes. For all four PDE4 isoenzymes, CDP 840 acted as a simple competitive inhibitor [5].

In vivo, CDP 840 (30 mg/kg) increased cAMP by 145% in the hippocampus and by 112% in the prefrontal cortex of male Sprague-Dawley rats. CDP 840 at doses of 10 and 30 mg/kg increased the phosphorylation of cAMP response element binding protein (pCREB) in the hippocampus (by 36 and 55%, respectively) and in the prefrontal cortex (by 32 and 60%, respectively). But these doses did not affect the expression of the cAMP response element binding protein (CREB). Repeated treatment with CDP 840 at a dose of 30 mg/kg increased the cell proliferation in rat hippocampus, but these cells were not survival [6].

References:
[1].  T.R. Jones, M. McAuliffe, C.S. McFarlane, et al. Effects of a selective phosphodiesterase IV inhibitor (CDP-840) in a leukotriene-dependent non-human primate model of allergic asthma. Can. J. Physiol. Pharmacol., 1998, 76: 210-217.
[2].  Chun Li, Nathalie Chauret, Laird A. Trimble, et al. Investigation of the in vitro metabolism profile of a phosphodiesterase-IV inhibitor, CDP-840: leading to structural optimization. Drug Metabolism and Disposition, 2001, 29:232–241.
[3].  John E. Souness and Sudha Rao. Proposal for Pharmacologically Distinct Conformers of PDE4 Cyclic AMP Phosphodiesterases. Cell. Signal., 1997, 9(3/4):227-236.
[4].  Christopher Hulme, Gregory B. Poli, Fu-Chih Huang, et al. Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles. Bioorganic & Medicinal Chemistry Letters, 1998, 8:175-178.
[5].  M.J. Perry, J. O'Connell, C. Walker, et al. CDP840: a novel inhibitor of PDE-4. Cell Biochem. Biophys., 1998, 29(1-2):113-32.
[6].  Lan Xiao, James P. O’Callaghan and James M. O’Donnell. Effects of Repeated Treatment with Phosphodiesterase-4 Inhibitors on cAMP Signaling, Hippocampal Cell Proliferation, and Behavior in the Forced-Swim Test. J. Pharmacol. Exp. Ther., 2011, 338(2):641-7.

Chemical Properties

Physical AppearanceOff-white solid
StorageDesiccate at RT
M.Wt409.95
Cas No.162542-90-7
FormulaC25H27NO2·HCl
Solubility<40.99mg/ml in DMSO
Chemical Name(R)-4-(2-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-phenylethyl)pyridine hydrochloride
SDFDownload SDF
Canonical SMILESCOC1=C(OC2CCCC2)C=C([[email protected]](C3=CC=CC=C3)([H])CC4=CC=NC=C4)C=C1.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

CDP 840 hydrochloride