| S1512 |
Tadalafil
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Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. This compound is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11
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J Immunother Cancer, 2024, 12(11)e009805
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Cell Mol Life Sci, 2024, 81(1):434
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J Clin Invest, 2021, 131(1)136779
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| S1895 |
Dipyridamole
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Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
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Nature, 2025, 10.1038/s41586-025-09755-9
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Theranostics, 2024, 14(18):6947-6968
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J Immunother Cancer, 2024, 12(11)e009805
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| S7858 |
Dibutyryl cAMP (db cAMP/Bucladesine) sodium
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Bucladesine sodium is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor.
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Cell, 2025, S0092-8674(25)00735-4
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Nat Neurosci, 2025, 28(6):1174-1184
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Nat Commun, 2025, 16(1):6151
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| S1431 |
Sildenafil Citrate
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Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.
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Br J Pharmacol, 2025, 10.1111/bph.70166
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Drug Des Devel Ther, 2025, 19:6487-6504
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J Pharm Pharmacol, 2023, rgad045
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| S4684 |
Sildenafil
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Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
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Adv Sci (Weinh), 2024, 11(40):e2407712
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J Immunother Cancer, 2024, 12(11)e009805
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Brain, 2023, 146(6):2453-2463
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| S2131 |
Roflumilast
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Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
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Redox Biol, 2025, 81:103563
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Invest Ophthalmol Vis Sci, 2024, 65(12):38
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Respir Investig, 2024, 62(3):455-461
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| S1430 |
Rolipram
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The PDE4 selective inhibitor, Rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.
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Elife, 2022, 11e73511
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ProQuest, 2022, 30509631
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Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4
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| S5836 |
IBMX (3-Isobutyl-1-methylxanthine)
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IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) is a nonspecific inhibitor of phosphodiesterase (PDE) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. It may enhance the intracellular cAMP levels and also acts as an adenosine (A1) receptor antagonist.
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J Biomed Sci, 2025, 32(1):31
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J Hematol Oncol, 2023, 16(1):30
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J Hematol Oncol, 2023, 16(1):30
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| S2515 |
Vardenafil HCl Trihydrate
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Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
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Gastroenterology, 2020, 159(3):1068-1084.e2
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Bone, 2020, 10.1016/j.bone.2020.115305
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Pulm Pharmacol Ther, 2020, 66:101985
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| S8034 |
Apremilast
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Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.
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Signal Transduct Target Ther, 2023, 8(1):40
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Acta Pharm Sin B, 2022, 12(1):228-245
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Int J Mol Sci, 2021, 22(23)12878
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