Esterases (Phosphodi-)

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].

[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
1229 (R)-(-)-Rolipram PDE4 inhibitor €110.00
1432 (S)-(+)-Rolipram PDE4 inhibitor €115.00
1957 Apremilast PDE4 inhibitor €60.00
1178 BAY 19-8004 PDE4 inhibitor €130.00
3148 BPN14770 Potent, selective, allosteric inhibitor of PDE4D €120.00
3574 Carbazeran Potent phosphodiesterase inhibitor and an aldehyde oxidase (AO) substrate €90.00
3169 Crisaborole Potent PDE4 inhibitor; Anti-inflammatory agent €60.00
3772 DPTIP hydrochloride Potent selective, metabolically stable, and brain-penetrant nSMase2 inhibitor €120.00
4042 ENPP1 inhibitor compound 43 Potent, selective and orally bioavailable ENPP1 inhibitor €220.00
2281 FIPI hydrochloride Phospholipase D (PLD) inhibitor that blocks phosphatidic acid (PA) production in vivo €100.00
2218 Gisadenafil besylate Potent and selective inhibitor of PDE5 €120.00
3094 GLPG1690 First-in-class, potent ATX inhibitor €110.00
3289 GW4869 trifluoroacetate Noncompetitive, neutral, magnesium-dependent SMase inhibitor €65.00
4136 HA130 Autotaxin (ATX) inhibitor Inquire
1127 L 454560 PDE4 inhibitor Inquire
3202 LEI-401 First-in-class, potent, selective and CNS-active NAPE-PLD inhibitor €160.00
3401 MBCQ Potent and selective inhibitor of PDE5 €60.00
3314 Milrinone PDE3 inhibitor €80.00
1168 Olprinone hydrochloride PDE3 inhibitor €119.00
1482 Parogrelil PDE3 inhibitor €120.00
1709 PDE5 inhibitor 42 PDE5 inhibitor €125.00
2825 PDE9A inhibitor C33(S) Potent and selective PDE9A inhibitor €135.00
3179 Pentoxifylline Non-specific inhibitor of cAMP phosphodiesterases €50.00
2148 PF 04447943 Selective, brain penetrant PDE9A inhibitor €70.00
3442 PF-8380 Potent, orally bioavailable ATX inhibitor €60.00
4013 Piclamilast Potent and selective PDE4 inhibitor €130.00
1911 RAD51 inhibitor B02 Inhibitor of RAD51 €95.00
1885 RI-1 Inhibitor of the central recombination protein RAD51 €95.00
2352 Roflumilast First specific PDE4 inhibitor licensed for treatment of COPD €90.00
1212 Rolipram PDE4 inhibitor €65.00

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