2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

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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:

Phosphodiesterase (PDE) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-90009AS
    Tadalafil-13C2,d3
    		Inhibitor
    Tadalafil-13C2,d3 is 13C and deuterated labeled Tadalafil (HY-90009A). Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
    Tadalafil-<sup>13</sup>C<sub>2</sub>,d<sub>3</sub>
  • HY-167715
    Traxanox
    		Inhibitor
    Traxanox is an orally available diuretic that enhances phagocytosis of yeast granules by mouse peritoneal macrophages and rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox inhibits IgE-mediated histamine release and cyclic AMP phosphodiesterase activity.Traxanox exhibits anti-inflammatory activity, as it inhibits the anaphylactoid reaction and reduces pleural fluid accumulation in experimental models of inflammation. Traxanox also demonstrates a synergistic effect when combined with hydrocortisone or indomethacin in suppressing adjuvant arthritis in rats.
    Traxanox
  • HY-W186242
    PDE4-IN-16
    		Inhibitor 98.84%
    PDE4-IN-16 (compound 27) is a PDE4 inhibitor with an IC50 value of 3.61 μM. PDE4-IN-16 can be used for the research of inflammatory diseases and central nervous system (CNS) disorders involving elevated levels of cytokines.
    PDE4-IN-16
  • HY-175971
    PDE1-IN-10
    		Inhibitor
    PDE1-IN-10 is a potent and sekective Phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 5 nM. PDE1-IN-10 can suppress TGF-β/Smad-MAPK signaling and exhibit antifibrotic effects. PDE1-IN-10 can be used for the research of idiopathic pulmonary fibrosis.
    PDE1-IN-10
  • HY-174267S
    ATX-IN-2
    		Inhibitor
    ATX-IN-2 (Compound 25) is an orally active and potent ATX inhibitor with an IC50 value of 3.27 nM. ATX-IN-2 reduces lysophosphatidic acid (LPA) secretion. ATX-IN-2 is promising for research of ATX-mediated diseases, such as inflammation, pulmonary fibrosis.
    ATX-IN-2
  • HY-19390
    KW-4490
    		Inhibitor
    KW-4490 is a selective phosphodiesterase 4 (PDE4) inhibitor. KW-4490 can be used for the researches of inflammation and immunology, such as asthma.
    KW-4490
  • HY-18252B
    (R)-Avanafil
    		Inhibitor
    (R)-Avanafil ((R)-TA1790) is a selective PDE5 inhibitor (IC50: 5.2 nM). (R)-Avanafil can be used for research of erectile dysfunction.
    (R)-Avanafil
  • HY-172528
    Enpp-1/3-IN-1
    		Inhibitor
    Enpp-1/3-IN-1 (Compound 5j) is an ENPP1/ENPP3 inhibitor, with IC50s of 0.59 μM (h-ENPP1) and 0.62 μM (h-ENPP3) respectively. Enpp-1/3-IN-1 also inhibits e5′NT (CD73) and TNAP with IC50s of 0.89 μM (h-e5′NT), 5.12 μM (r-e5′NT) and 1.68 μM (h-TNAP), respectively. Enpp-1/3-IN-1 can be used for cancer research.
    Enpp-1/3-IN-1
  • HY-114643
    (Rac)-Tovinontrine
    		Inhibitor
    (Rac)-Tovinontrine ((Rac)-IMR-687) is a phosphodiesterase 9 (PDE9) inhibitor that increases cyclic guanosine monophosphate (cGMP) levels. (Rac)-Tovinontrine is promising for research of thalassemia.
    (Rac)-Tovinontrine
  • HY-115871A
    (Rac)-PDE4-IN-4
    		Inhibitor
    (Rac)-PDE4-IN-4 is the diastereomer mixture of PDE4-IN-4 (HY-115871). PDE4-IN-4 is a dual M3 (pIC50 = 10.2) antagonist-PDE4 (pIC50 = 8.8) inhibitor for the inhaled research of pulmonary diseases.
    (Rac)-PDE4-IN-4
  • HY-B0312S1
    Dipyridamole-d16
    		Inhibitor
    Dipyridamole-d16 is the deuterium labeled Dipyridamole. Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
    Dipyridamole-d<sub>16</sub>
  • HY-N3945R
    Glaucine (Standard)
    		Inhibitor
    Glaucine (Standard) is the analytical standard of Glaucine. This product is intended for research and analytical applications. Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 μM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
    Glaucine (Standard)
  • HY-123154
    PDE10A-IN-4
    		Inhibitor
    PDE10A-IN-4 (compound 38) is a compound used to inhibit schizophrenia. As a PDE10A inhibitor, it is less effective than placebo in inhibiting acute schizophrenia and does not show antipsychotic effect.
    PDE10A-IN-4
  • HY-128060
    PDE5-IN-42
    		Inhibitor
    PDE5-IN-42 (Compound 42) is a potent and orally active PDE5 inhibitor with an IC50 of 0.04 nM. PDE5-IN-42 maintains selectivity over PDE6 and PDE11.
    PDE5-IN-42
  • HY-144684
    PDE4-IN-8
    		Inhibitor
    PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM).
    PDE4-IN-8
  • HY-179550
    Avanafil metabolite M4
    		Inhibitor
    Avanafil metabolite M4 (Compound M-4ii) is a metabolite of Avanafil (HY-18252). Avanafil is a selective Phosphodiesterase-5 (PDE-5) inhibitor with IC50s of 5.2, 630, 5700, 6200, 12000, 27000, 51000 and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cGMP hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil metabolite M4
  • HY-18252S
    Avanafil-13C,d3
    		Inhibitor
    Avanafil-13C,d3 is the 13C- and deuterium labeled Avanafil.
    Avanafil-<sup>13</sup>C,d<sub>3</sub>
  • HY-105482
    BMY 20844
    		Inhibitor
    BMY 20844 is an orally active platelet cAMP phosphodiesterase inhibitor with anti-thrombosis activity. BMY 20844 can elevate cAMP levels and activate protein kinase in platelets. BMY 20844 can be used for the research of cardiovascular disease.
    BMY 20844
  • HY-134954
    Palmitoleoyl 3-carbacyclic phosphatidic acid
    		Inhibitor
    Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) is an intermediately potent inhibitor of autotaxin (ATX) with an IC50 of 620 nM. Palmitoleoyl 3-carbacyclic phosphatidic acid can be used for melanoma research.
    Palmitoleoyl 3-carbacyclic phosphatidic acid
  • HY-182452
    U 84569
    		Inhibitor
    U 84569 is a potent low-Km cAMP-dependent Phosphodiesterase inhibitor, with an IC50 value of 300 nM in platelet cytosol. By inhibiting phosphodiesterase and elevating cAMP levels, U 84569 indirectly blocks receptor-mediated Phospholipase C activation, thereby inhibiting platelet aggregation.
    U 84569
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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