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CP 80633

Cayman Chemical Item Number 13183

(CAS 135637-46-6)

CP 80633 (CAS 135637-46-6)

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Description

Phosphodiesterases (PDE) enzymatically convert the cyclic nucleotide second messengers cAMP and cGMP to 5’-AMP and 5’-GMP, respectively, thus terminating signal transduction. The cAMP-specific PDE4 isoforms may be particularly important in certain respiratory and neurological diseases.1,2 CP 80633 is a selective inhibitor of PDE4 (IC50 = 1.27 μM for PDE4 versus. >100 μM for PDE1, PDE2, PDE3, and PDE5).3 It potentiates PGE1-dependent increases in cAMP levels in eosinophils, monocytes, and T-cells, inhibits eosinophil superoxide production (IC50 < 0.6 μM), and blocks LPS-induced TNF-α release from monocytes (IC50 = 0.22 μM).3 CP 80633 (1 mg/kg) significantly reduces antigen-induced airway inflammation in atopic guinea pigs, monkeys, and mice.4,5

1 Spina, D. PDE4 inhibitors: Current status. Br J Pharmacol 155 308-315 (2008).

2 O'Donnell, J.M., and Zhang, H. Antidepressant effects of inhibitors of cAMP phosphodiesterase (PDE4). Trends Pharmacol Sci 25(3) 158-163 (2004).

3 Cohan, V.L., Showell, H.J., Fisher, D.A., et al. In vitro pharmacology of the novel phosphodiesterase type 4 inhibitor, CP-80633. J Pharmacol Exp Ther 278(3) 1356-1361 (1996).

4 Turner, C.R., Cohan, V.L., Cheng, J.B., et al. The in vivo pharmacology of CP-80, 633, a selective inhibitor of phosphodiesterase 4. J Pharmacol Exp Ther 278(3) 1349-1355 (1996).

5 Cheng, J.B., Watson, J.W., Pazoles, C.J., et al. The phosphodiesterase type 4 (PDE4) inhibitor CP-80,633 elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice: Effect of adrenalectomy. J Pharmacol Exp Ther 280 621-626 (1997).

Formal Name 5-​[3-​[(1S,​2S,​4R)-​bicyclo[2.2.1]hept-​2-​yloxy]-​methoxyphenyl]tetrahydro-​2-​(1H)-​pyrimidinone
CAS Number 135637-46-6
Molecular Formula C18H24N2O3
Formula Weight 316.4
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
O=C(NC1)​NCC1C2=CC(O[C@@H]​3[C@H]​(C4)​CC[C@H]​4C3)​=C(OC)​C=C2

Background Reading

Cohan, V.L., Showell, H.J., Fisher, D.A., et al. In vitro pharmacology of the novel phosphodiesterase type 4 inhibitor, CP-80633. J Pharmacol Exp Ther 278(3) 1356-1361 (1996).

Spina, D. PDE4 inhibitors: Current status. Br J Pharmacol 155 308-315 (2008).

O'Donnell, J.M., and Zhang, H. Antidepressant effects of inhibitors of cAMP phosphodiesterase (PDE4). Trends Pharmacol Sci 25(3) 158-163 (2004).

Cheng, J.B., Watson, J.W., Pazoles, C.J., et al. The phosphodiesterase type 4 (PDE4) inhibitor CP-80,633 elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice: Effect of adrenalectomy. J Pharmacol Exp Ther 280 621-626 (1997).

Turner, C.R., Cohan, V.L., Cheng, J.B., et al. The in vivo pharmacology of CP-80, 633, a selective inhibitor of phosphodiesterase 4. J Pharmacol Exp Ther 278(3) 1349-1355 (1996).

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Size Price Quantity Subtotal
500 µg $21.00 $0.00
1 mg $40.00 $0.00
5 mg $168.00 $0.00
10 mg $294.00 $0.00
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Cart Total $0.00

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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