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.
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 | €160.00 | |
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 | |
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 | |
4234 | HA-155 | Potent ATX inhibitor | Recently added | €130.00 |
4136 | HA130 | Autotaxin (ATX) inhibitor | Inquire | |
1127 | L 454560 | PDE4 inhibitor | Inquire | |
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 | |
2352 | Roflumilast | First specific PDE4 inhibitor licensed for treatment of COPD | €90.00 | |
1212 | Rolipram | PDE4 inhibitor | €65.00 | |
4002 | RS 25344 | Selective PDE4 inhibitor | €130.00 | |
1592 | SB 207499 | PDE4 inhibitor | €70.00 | |
2046 | Sildenafil citrate | Inhibitor of cGMP-specific PDE5 | €75.00 |