PDE

No less than eleven sub-types of the enzyme family of phosphodiesterases (PDE; EC 3.1.4.-) are known to date, many of which exist as splice variants[1]. They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. Roughly, the sub-types can be divided into 3 groups: one group of enzymes specifically degrades cyclic adenosine monophosphate (cAMP; PDE4, 7 and 8), another group specifically targets cyclic guanosine monophosphate (cGMP; PDE5, 6, and 9), whereas the third group of enzymes (including PDE1, 2, 3, 10, and 11) are non specific towards either cAMP or cGMP. PDEs influence a vast array of pharmacological processes, including pro-inflammatory mediator production and action, ion channel function, muscle contraction, learning, differentiation, apoptosis, lipogenesis, glycogenolysis and gluconeogenesis. Recent advances in molecular pharmacology of PDE isoenzymes resulted in identification of new potential applications of PDE inhibitors in various therapeutic areas, including dementia, depression and schizophrenia[2].

Phosphodiesterases listed: PDE, PLC, PLD


[1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. Bolger G. B. Cell. Signal. 1994, 6,  851–859.
[2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. Y. H. Jeon,Y. -S. Heo, C. M. Kim,Y. -L. Hyun, T. G. Lee, S. Ro and J. M. Cho. Cell. Mol. Life Sci. Vol. 2005, 62, 1198.

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Axon ID Name Description From price
2825 PDE9A inhibitor C33(S) Potent and selective PDE9A inhibitor €135.00
3179 Pentoxifylline Non-specific inhibitor of cAMP phosphodiesterases €40.00
2148 PF 04447943 Selective, brain penetrant PDE9A inhibitor €90.00
3442 PF-8380 Potent, orally bioavailable ATX inhibitor  Recently added €60.00
2352 Roflumilast First specific PDE4 inhibitor licensed for treatment of COPD €90.00
1212 Rolipram PDE4 inhibitor €65.00
1592 SB 207499 PDE4 inhibitor €80.00
2046 Sildenafil citrate Inhibitor of cGMP-specific PDE5 €75.00
2399 TAK 063 Highly potent, selective, and orally active PDE10A inhibitor €125.00
3396 Vardenafil dihydrochloride Highly potent, selective and orally bioavailable inhibitor of cGMP-specific PDE5 €60.00
1216 Zardaverine PDE3 and PDE4 inhibitor €75.00

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