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-162911
    Enpp-1-IN-22
    		Inhibitor
    Enpp-1-IN-22 is an orally bioavailable prodrug of the potent ENPP1 inhibitor paraformaldehyde with antitumor activity.
    Enpp-1-IN-22
  • HY-W759997
    Reproterol-d3
    Reproterol-d3 is the deuterium labeled Reproterol (HY-135490). Reproterol is a dual acting β2-adrenoceptor agonist and PDE inhibitor. The theophylline constituent of Reproterol inhibits phosphodiesterase activity induced by adenylyl cyclase. Reproterol has the potential for asthma research.
    Reproterol-d<sub>3</sub>
  • HY-108620
    CDP-840
    		Inhibitor
    CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys.
    CDP-840
  • HY-106245
    HT-0712
    		Inhibitor
    HT-0712 is a Phosphodiesterase Type 4 (PDE4) inhibitor. HT-0712 enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia.
    HT-0712
  • HY-135089
    Autotaxin-IN-5
    		Inhibitor
    Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis.
    Autotaxin-IN-5
  • HY-126754
    Archangelicin
    		Inhibitor
    Archangelicin is an inhibitor for cAMP-phosphodiesterase (cAMP-PDE) with IC50 >400 μM. Archangelicin inhibits nuclear factor of activated T cell (NFAT) with IC50 of 9 μM. Archangelicin exhibits antitumor and anti-inflammatory.
    Archangelicin
  • HY-B0549S
    Flavoxate-d5
    Flavoxate-d5 is deuterium labeled Flavoxate.
    Flavoxate-d<sub>5</sub>
  • HY-172776
    Phosphodiesterase-IN-3
    		Inhibitor
    Phosphodiesterase-IN-3 (Example 20) is a phosphodiesterase 4B inhibitor, with IC50s of <10 nM and 10-100 nM for PDE4B1 and PDE4D3, respectively. Phosphodiesterase-IN-3 has the potential for the research of idiopathic pulmonary fibrosis.
    Phosphodiesterase-IN-3
  • HY-A0027A
    Fenspiride
    		Inhibitor
    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.
    Fenspiride
  • HY-B0204B
    (-)-Pimobendan
    		Control
    (-)-Pimobedan is an isomer of pimobedan. It has the property of stereoselective partitioning or distribution into erythrocytes. The clearance of (-)-pimobedan from erythrocytes is significantly lower than that of (+)-pimobedan, which is entirely due to its stereoselective distribution into erythrocytes. This stereoselective property of (-)-pimobedan may explain the phenomenon previously reported that it produces a 1.5-fold greater contractile force than the (+)-isomer in detergent-treated myocardial specimens of guinea pigs and dogs. These properties suggest that (-)-pimobedan may have unique advantages in terms of in vivo distribution and pharmacological action, which may have important implications for its clinical use.
    (-)-Pimobendan
  • HY-173290
    PDE4D inhibitor 1
    		Inhibitor
    PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.
    PDE4D inhibitor 1
  • HY-10030
    Mardepodect succinate
    Mardepodect succinate (PF-2545920 succinate) is a potent and specific phosphodiesterase 10A (PDE10A) inhibitor with potential activity in the treatment of schizophrenia. Mardepodect succinate has been further optimized to improve brain penetration and compound-like properties for use in schizophrenia research.
    Mardepodect succinate
  • HY-W587881
    Acetylvardenafil
    		Inhibitor
    Acetylvardenafil is a new analog of Vardenafil (HY-B0442). The sulfonyl group in the structure of Acetylvardenafil is replaced by an acetyl group. Acetylvardenafil is a PDE-5 inhibitor that can be used in the study of erectile dysfunction (ED).
    Acetylvardenafil
  • HY-100615A
    R 80123
    		Inhibitor ≥98.0%
    R 80123 is the Z-isomer of R 79595, is also a highly selective phosphodiesterase inhibitor.
    R 80123
  • HY-19586
    Albifylline
    		Inhibitor
    Albifylline (A 81-3138; HWA-138) is a Xanthine (HY-W017389) derivate. Albifylline reduces the shock-induced leukocyte adhesions to the sinusoidal endothelium in the liver after hemorrhagic shock and improves microvascular blood flow in the liver.
    Albifylline
  • HY-144265
    PDE4-IN-5
    		Inhibitor
    PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect.
    PDE4-IN-5
  • HY-111477
    (E/Z)-Ensifentrine
    		Inhibitor
    (E/Z)-Ensifentrine is a dual inhibitor of PDE3/4. (E/Z)-Ensifentrine reduces the inflammatory cells into the airways. (E/Z)-Ensifentrine has bronchodilatory and anti-inflammatory activities in vitro and in vivo model.
    (E/Z)-Ensifentrine
  • HY-13295S
    Vinpocetine-d5
    		Inhibitor
    Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (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.
    Vinpocetine-d<sub>5</sub>
  • HY-124310
    PDE5-IN-6c
    PDE5-IN-6c is a potent and selective phosphodiesterase 5A1 (PDE5A1) inhibitor with the potential to inhibit Alzheimer's disease (AD). PDE5-IN-6c exhibits an excellent in vitro IC50 (0.056 nM), demonstrating its potent inhibitory activity. PDE5-IN-6c has improved water solubility, making it a more attractive drug candidate.
    PDE5-IN-6c
  • HY-139041
    Palmitoylcholine chloride
    		Inhibitor
    Palmitoylcholine chloride reduces membrane stress and reduces enzyme activity by Ca(2+)-dependent phosphatidylinositol phosphodiesterase (EC 3.1.4.10) hydrolysis of phosphatidylinositol monolayers.
    Palmitoylcholine chloride
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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