CP 80633

CAS# 135637-46-6

CP 80633

Catalog No. BCC7463----Order now to get a substantial discount!

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Chemical structure

CP 80633

3D structure

Chemical Properties of CP 80633

Cas No. 135637-46-6 SDF Download SDF
PubChem ID 60833 Appearance Powder
Formula C18H24N2O3 M.Wt 316.39
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name 5-[3-[[(3S)-3-bicyclo[2.2.1]heptanyl]oxy]-4-methoxyphenyl]-1,3-diazinan-2-one
SMILES COC1=C(C=C(C=C1)C2CNC(=O)NC2)OC3CC4CCC3C4
Standard InChIKey LITNEAPWQHVPOK-TZDAIYRESA-N
Standard InChI InChI=1S/C18H24N2O3/c1-22-15-5-4-12(14-9-19-18(21)20-10-14)8-17(15)23-16-7-11-2-3-13(16)6-11/h4-5,8,11,13-14,16H,2-3,6-7,9-10H2,1H3,(H2,19,20,21)/t11?,13?,16-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CP 80633

DescriptionSelective inhibitor of phosphodiesterase type 4 (IC50 values are 1.9, > 100, > 100, > 100 and > 100 μM for human lung PDE4, lung PDE1, lung PDE2, heart PDE3 and platelet PDE-V respectively) that displays no significant PDE4 isozyme selectivity. Inhibits hydrolysis of cAMP in isolated human peripheral blood monocytes, eosinophils and T cells. Displays anti-inflammatory and bronchodilatory effects in vivo.

CP 80633 Dilution Calculator

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CP 80633 Molarity Calculator

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Preparing Stock Solutions of CP 80633

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1607 mL 15.8033 mL 31.6066 mL 63.2131 mL 79.0164 mL
5 mM 0.6321 mL 3.1607 mL 6.3213 mL 12.6426 mL 15.8033 mL
10 mM 0.3161 mL 1.5803 mL 3.1607 mL 6.3213 mL 7.9016 mL
50 mM 0.0632 mL 0.3161 mL 0.6321 mL 1.2643 mL 1.5803 mL
100 mM 0.0316 mL 0.158 mL 0.3161 mL 0.6321 mL 0.7902 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on CP 80633

The phosphodiesterase type 4 (PDE4) inhibitor CP-80,633 elevates plasma cyclic AMP levels and decreases tumor necrosis factor-alpha (TNFalpha) production in mice: effect of adrenalectomy.[Pubmed:9023272]

J Pharmacol Exp Ther. 1997 Feb;280(2):621-6.

Rolipram was previously reported to elevate plasma cyclic adenosine 3',5'-monophosphate (cAMP) and inhibit serum tumor necrosis factor-alpha (TNF-alpha) production in mice. CP-80,633, a new cyclic nucleotide phosphodiesterase (PDE4) inhibitor, has been shown to augment intracellular cAMP levels and to inhibit TNFalpha release from human monocytes in vitro. This study was undertaken to determine the effect of p.o. CP-80,633 on plasma cAMP levels and lipopolysaccharide-induced TNFalpha production in mice with and without adrenal glands. CP-80,633 dose-dependently (3-32 mg/kg p.o.) elevated plasma cAMP levels and decreased systemic TNFalpha production in response to i.p. injection of lipopolysaccharide. Elevated plasma cAMP levels can be detected for up to 4 hr. CP-80,633 (10 mg/kg p.o.) caused a 6-fold increase in the plasma cAMP level, a 2-fold increase in the plasma epinephrine level and a greater than 95% reduction in TNFalpha production. Unlike CP-80,633, neither vinpocetine, dipyridamole, SKB-94,120 nor zaprinast, at 100 mg/kg p.o., modified the cAMP response, which suggests that this response is mediated by inhibition of PDE4. Adrenalectomy reduced the cAMP response and completely blocked the epinephrine response; however, the levels of plasma cAMP in the CP-80,633-treated mice (10 mg/kg p.o.) remained elevated (vehicle: 47.3 +/- 6.8 vs. CP-80,633: 98.4 +/- 10.3 pmol/ml, n = 7, P < .05). This effect is mimicked by treatment of control mice with propranolol, which demonstrates that beta adrenoreceptors contribute to the cAMP response. Removal of adrenal glands significantly increased the LPS-induced elevation of serum TNFalpha. The ability of CP-80,633 to block the TNFalpha response was only slightly affected by adrenalectomy (ED50 = 1.2 mg/kg in controls vs. 3.9 mg/kg in adrenalectomized mice). Taken together, these results show that CP-80,633, when given p.o. to mice, is capable of elevating plasma cAMP and inhibiting TNFalpha production and that adrenal catecholamines contribute significantly to the effect of CP-80,633 on the cAMP response but only slightly to its effect on the systemic TNFalpha response.

Differential in vivo and in vitro bronchorelaxant activities of CP-80,633, a selective phosphodiesterase 4 inhibitor.[Pubmed:9360015]

Can J Physiol Pharmacol. 1997 Aug;75(8):1001-8.

CP-80,633, a selective phosphodiesterase (PDE) 4 inhibitor, potently reverses histamine bronchoconstriction in anesthetized guinea pigs (ED50 10 micrograms/kg) but only weakly relaxes histamine-constricted guinea pig trachea (EC50 137 microM). Using CP-80,633 as a prototype PDE4 inhibitor, we evaluated the hypothesis that bronchodilation induced by PDE4 inhibitors is not mediated by direct relaxation of airway smooth muscle. In anesthetized guinea pigs, a bronchodilatory dose of CP-80,633 did not increase plasma catecholamines, nor did propranolol pretreatment significantly alter the ability of CP-80,633 to reverse histamine bronchoconstriction. In an isolated organ system, the activity of bronchorelaxants may be attenuated by the lack of endogenous activators of adenylyl cyclase or by decreased levels of intracellular cyclic nucleotides. Pretreatment with the beta-adrenoceptor agonist, salbutamol, or the PDE3 inhibitor imazodan did not potentiate the bronchorelaxant ability of CP-80,633. Milrinone pretreatment increased the potency of CP-80,633 to relax carbachol-constricted tracheal rings, but only at concentrations where nonspecific effects have been reported. By comparing the bronchorelaxant abilities of PDE inhibitors in tracheal rings with or without epithelium, we determined that the epithelium did not serve as a barrier to drug penetration. In conclusion, CP-80,633 is a potent bronchodilator in vivo, whose activity is neither mediated by direct airway smooth muscle relaxation nor dependent upon endogenous catecholamines.

In vitro pharmacology of the novel phosphodiesterase type 4 inhibitor, CP-80633.[Pubmed:8819523]

J Pharmacol Exp Ther. 1996 Sep;278(3):1356-61.

We present the in vitro pharmacology of a novel adenosine 3'-5' -cyclic monophosphate-specific phosphodiesterase (PDE) type 4 inhibitor, CP-80633 ((2'S)5-[3-(2' -exobicyclo[2.2.1]-heptyloxy)4-methoxyphenyl] tetrahydro-2(1H)-primidone), which has shown efficacy in phase II clinical trials for atopic dermatitis. CP-80633 inhibits PDE4 isozymes (human lung IC50 = 1.27 microM) in the absence of effects on PDE1, PDE2, PDE3 and PDE5 isozymes (IC50 > 100 microM). It exhibits no significant selectivity for any single cloned PDE4A, B, C or D isoform. CP-80633 inhibits adenosine 3'-5'-cyclic monophosphate hydrolysis in partially purified human peripheral blood monocyte cytosol (IC50 = 3.52 microM), eosinophil membrane (IC50 = 1.10 microM) and T cell membrane (IC50 = 2.28 microM) preparations. Inhibition of eosinophil PDE4 adenosine 3'-5'-cyclic mono-phosphate hydrolysis by CP-80,633 occurs in a noncompetitive manner. Unlike theophylline, CP-80,633 is inactive against ratrain adenosine (A1,A2) receptors. Consistent with its action as a PDE4 inhibitor in whole cells, CP-80633 potentiates PGE1 dependent increases in adenosine 3'-5'-cyclic monophosphate levels in human U937 cells, and in human eosinophils, monocytes and T cells (EC200 approximately 1.0 microM). Consequently, CP-80633 inhibits many inflammatory cell functions including 1) human eosinophil superoxide anion production (IC50 < 0.6 microM), 2 C5a-(IC50 = 0.40 microM) and LTB4-(IC50 = 0.20 microM) mediated guinea pig peritoneal eosinophil chemotaxis and 3) lipopolysac-charide-induced tumor necrosis factor-alpha release from human monocytes (IC50 = 0.219 microM). These data clearly demonstrate that CP-80633 is a selective inhibitor of PDE4 isozymes, and support its potential use as a therapeutic agent for a number of inflammatory and immune disorders.

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