Phosphodiesterase (PDE)
Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules.
Phosphodiesterase (PDE) Isoform Specific Products
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Phosphodiesterase (PDE)
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PDE1
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PDE2
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PDE3
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PDE4
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PDE5
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PDE6
(22)
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PDE7
(28)
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PDE9
(19)
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PDE10
(53)
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PDE11
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PDE12
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PDE8
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Autotaxin
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All Product Categories
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Phosphodiesterase (PDE) Inhibitors
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Phosphodiesterase (PDE) Agonists
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Phosphodiesterase (PDE) Antagonists
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Phosphodiesterase (PDE) Activators
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Phosphodiesterase (PDE) Modulators
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Phosphodiesterase (PDE) Degraders
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Phosphodiesterase (PDE) Controls
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Phosphodiesterase (PDE) Substrates
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Phosphodiesterase (PDE) Ligand
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Phosphodiesterase (PDE) Related Products (1000)
Related Products (1000)
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Antibodies (4)
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Phosphodiesterase (PDE) Isoform Comparison
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Crisaborole
0 ImagesSynonyms: AN-2728; PF-06930164
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ITI-214
0 ImagesITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
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Zatolmilast
0 ImagesSynonyms: BPN14770Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
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Zaprinast
0 ImagesSynonyms: M&B 22948Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
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EHNA hydrochloride
0 ImagesEHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects.
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Butein
0 ImagesButein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
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Ensifentrine
0 ImagesSynonyms: RPL-554Ensifentrine (RPL-554) is an inhaled dual inhibitor of PDE3 and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine blocks PDE3 and PDE4 enzymes, thereby increasing the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, dilating the bronchi, and inhibiting the activation and migration of inflammatory cells. Ensifentrine can be used in the research of chronic obstructive pulmonary disease (COPD).
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Vinpocetine
0 ImagesSynonyms: Ethyl apovincaminateVinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
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8-CPT-Cyclic AMP sodium
0 ImagesSynonyms: 8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.
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Ibudilast
0 ImagesSynonyms: KC-404; AV-411; MN-166Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
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Anagrelide hydrochloride
0 ImagesSynonyms: BL4162AAnagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action.
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Mardepodect
0 ImagesSynonyms: PF-2545920Mardepodect is a potent, selective orally active, and brain-penetrant PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs.
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Sappanone A
0 ImagesSappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular .
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Levosimendan
0 ImagesSynonyms: Simsndan; OR-1259; (4R)-SimendanLevosimendan (Simsndan; OR-1259) is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.
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Vardenafil
0 ImagesVardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
