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
(60)
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PDE2
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PDE3
(93)
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PDE4
(198)
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PDE5
(97)
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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
(13)
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PDE12
(2)
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PDE8
(11)
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Autotaxin
(36)
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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 (1009)
Related Products (1009)
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Antibodies (4)
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Phosphodiesterase (PDE) Isoform Comparison
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DSR-141562
0 ImagesDSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
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TDP1 Inhibitor-1
0 ImagesTDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM. TDP1 Inhibitor-1 shows cytotoxicity against multiple cancer cells. TDP1 Inhibitor-1 can be used for the research of cancer, such as breast cancer.
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Amrinone
0 ImagesSynonyms: InamrinoneAmrinone (Inamrinone) is a positive inotropic-vasodilator agent. Amrinone is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
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Zardaverine
0 ImagesZardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma.
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Mufemilast
0 ImagesSynonyms: Hemay005Mufemilast (Heymay005) is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor (IC50 = 80-120 nM). Mufemilast modulates cytokines upregulated in Behςet’s syndrome (BS). Mufemilast displays a significant inhibitory effect on TNF-α, which is an important proinflammatory cytokine target in the disease process of psoriasis. Mufemilast can be studied in research for diseases such as rheumatoid arthritis, psoriasis and BS.
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STF-1084
0 ImagesSTF-1084 is a specific, cell-impermeable, competitive inhibitor of ENPP1 (Ki = 33 nM). STF-1084 increases extracellular cGAMP concentrations by preventing its degradation by ENPP1, thereby enhancing immune infiltration. STF-1084 acts synergistically with ionizing radiation (IR) and cGAMP to delay tumor progression. STF-1084 can be used to study cancers with low immunogenicity.
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Ethaverine hydrochloride
0 ImagesEthaverine hydrochloride is a Papaverine derivative and vasodilator. Ethaverine hydrochloride inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrochloride blocks L-type Ca2+ channels, reduces intracellular Ca2+ levels, inhibits platelet adhesion and aggregation, regulates cardiac conduction and heart rate, and increases peripheral and cerebral blood flow. Ethaverine hydrochloride alters cochlear microcirculation, intracochlear Po2, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrochloride is used in the research of peripheral vascular diseases.
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Mirodenafil
0 ImagesSynonyms: SK3530Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
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Sp-cAMPS sodium salt
0 ImagesSp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
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Phyllodulcin
0 ImagesPhyllodulcin is an orally active sweetener found in Hydrangea macrophylla var. thunbergii. Phyllodulcin acts as a non-selective phosphodiesterase inhibitor and exerts anti-allergic effects by suppressing lymphocyte activation. Phyllodulcin can be used to combat obesity by regulating levels of leptin, fat browning-related genes, and hypothalamic BDNF-TrkB signaling.
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Acefylline
0 ImagesSynonyms: Theophyllineacetic acid; Theophylline-7-acetic acidAcefylline (Theophyllineacetic acid), a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
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Enpp-1-IN-19
0 ImagesEnpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC50=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence.
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Enoximone
0 ImagesEnoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
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PF-04449613
0 ImagesPF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM[1]. PF-04449613 improved motor learning ability in a mouse model[2].
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3-Methylxanthine
0 Images3-Methylxanthine is a blood-brain barrier-permeable cyclic GMP phosphodiesterase inhibitor, with an IC50 of 920 μM against guinea pig cyclic GMP phosphodiesterase. 3-Methylxanthine relaxes the spontaneous tension of isolated guinea pig tracheal smooth muscle preparations. Through a DRD1-dependent pathway, 3-Methylxanthine upregulates the expression of γH2AX and activated caspase-3, downregulates the expression of Bcl-2, and enhances Cisplatin-induced apoptosis (apoptosis) in ovarian cancer cells both in vitro and in vivo. 3-Methylxanthine induces clonic convulsions in the central nervous system. 3-Methylxanthine is the major metabolite of Theophylline (HY-B0809). 3-Methylxanthine can be used in studies related to ovarian cancer and neurotoxic convulsions.
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5,7-Dichloropyrazolo[1,5-a]pyrimidine
![5,7-Dichloropyrazolo[1,5-a]pyrimidine](https://file.medchemexpress.com/product_pic/hy-w003486.gif "Click to View 5,7-Dichloropyrazolo[1,5-a]pyrimidine Product Detail")
0 Images5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a Ki of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia.
