Tetomilast (OPC-6535) is a PDE4 inhibitor with potential for the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.Target: Phosphodiesterase (PDE)Dipyridamole concentrations of 1 nmol/ml blood caused 90% inhibition of adenosine metabolism. Dipyridamole at therapeutic concentrations causes significant inhibition of adenosine metabolism in whole blood [1]. Dipyridamole has a dose-dependent inhibitory effect on thromboxane synthesis which was independent of aggregation. Dipyridamole also inhibited malonyldialdehyde production in response to both thrombin and arachidonic acid [2]. Dipyridamole enhances platelet inhibition by amplifying the signaling of the NO donor sodium nitroprusside. These data support the concept that enhancement of endothelium-dependent NO/cGMP-mediated signaling may be an important in vivo component of dipyridamole action [3].
BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the research of memory enhancement in CNS disorders.
PDE10-IN-5 is a phosphodiesterase 10 (PDE 10) inhibitor, can be used for researching certain central nervous system (CNS) disorders[1].
Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect[1][2].
(R)-DNMDP (DNMDP R-form) is the R-form of is DNMDP, which is a potent and selective cancer cell cytotoxic agent that binds to PDE3A, promotes an interaction between PDE3A and Schlafen 12 (SLFN12).
Pentoxifylline-d6 (BL-191-d6) is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Senazodan (MCI 154) (hydrochloride), as a Ca2+ sensitiser, shows inhibition effect on PDE III[1][2].
Kuraridine is a prenylated flavonol extract from the roots of Sophora flavescens. Kuraridine an inhibitory effect on cGMP specific phosphodiesterase type 5 (PDE5) and has an IC50 of 0.64 μM[1].
(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine (HY-132821), is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases[1].
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model[1].
Anagrelide hydrochloride monohydrate is a imidazoquinazoline agent. Anagrelide hydrochloride monohydrate decreases the level of platelets in blood, prevents blood clots formation. Anagrelide hydrochloride monohydrate can be used for research of essential thrombocythaemia (ET) and thrombocythaemia associated with polycythaemia vera (PV)[1].
Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE 9) inhibitor. Irsenontrine can be used for the research of neurological diseases[1].
ATX inhibitor 8 is a Autotaxin (ATX) inhibitor extracted from patent WO2018212534A1 compound 96[1].
Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity.
Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM[1][2][3].