Biochem/physiol Actions

Primary TargetPDE I, PDE III, PDE IV, PDE V

General description

Phosphodiesterases (PDEs) play an important role in the regulation of cAMP and cGMP levels in the cell. At least five PDE isozymes have been characterized that are differentially expressed and regulated in different cell types: Ca²⁺-calmodulin-dependent (PDE I); cGMP-stimulated (PDE II); cGMP-inhibited (PDE III); cAMP-specific (PDE IV); cGMP-specific (PDE V). These isozymes exhibit significant homology in their catalytic domain. The cyclic nucleotides are important regulators of many different cellular processes. They are involved in inflammation, asthma, and cardiovascular complications. Hence, specific inhibitors of the PDE isozymes have a potential for use as therapeutic agents. The Phosphodiesterase Inhibitor Set I contains the following inhibitors that are selective for PDE types l, III, IV, and V:r>r>• 8-Methoxymethyl-3-isobutyl-1-methylxanthine(8-Methoxymethyl-IBMX) (Cat. No. 454202), 10 mgr>• 4-{[3′,4′-(Methylenedioxy) benzyl]amino}-6-methoxyquinazoline (Cat. No. 475250), 1 mgr>• Rolipram (Cat. No. 557330), 5 mgr>• Trequinsin, Hydrochloride (Cat. No. 382425), 10 mg

A convenient set of inhibitors that are selective for PDE types I, III, IV, and V. Contains 10 mg of 8-Methoxymethyl-3-isobutyl-1-methylxanthine (Cat. No. 454202), a Ca²⁺/CaM-dependent PDE (PDE I) inhibitor; 1 mg of 4-{[3′,4′-(Methylenedioxy)benzyl]amino}-6-methoxyquinazoline (Cat. No. 475250), a cGMP-specific PDE (PDE V) inhibitor; 5 mg of Rolipram (Cat. No. 557330), a cAMP-specific PDE (PDE IV) inhibitor; and 10 mg of Trequinsin, Hydrochloride (Cat. No. 382425), a cGMP-inhibited PDE (PDE III) inhibitor. Supplied with data sheet.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Takase, Y., et al. 1994. J. Med. Chem.37, 2106.Underwood, D.C., et al. 1994. J. Pharmacol. Exp. Ther.270, 250.Wells, J.N. and Miller, J.R. 1988. Methods Enzymol.159, 489.Ruppert, D. and Weithmann, K.U. 1982. Life Sciences31, 2037.

See properties table for specific solvent and recommended stock concentration.

Packaging

1 set in Glass bottle

Reconstitution

Following reconstitution of each inhibitor, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Multiple Toxicity Values, refer to MSDS (O)