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-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
  • HY-162954
    SMQ-03-20
    		Inhibitor
    SMQ-03-20 (compund 4g) is an orally bioavailable, brain-penetrant, selective and potent PDE11A4 inhibitor.
    SMQ-03-20
  • HY-176708
    ISM5939
    		Inhibitor
    ISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.
    ISM5939
  • HY-90009AR
    Tadalafil (Standard)
    		Inhibitor
    Tadalafil (Standard) is the analytical standard of Tadalafil. This product is intended for research and analytical applications. Tadalafil (IC-351) is a PDE5 inhibitor with an IC50 value of 1.8 nM.
    Tadalafil (Standard)
  • HY-123008R
    Reproterol hydrochloride (Standard)
    		Inhibitor
    Reproterol (hydrochloride) (Standard) is the analytical standard of Reproterol (hydrochloride). This product is intended for research and analytical applications. Reproterol hydrochloride is a dual-acting beta2-adrenoceptor agonist and phosphodiesterase inhibitor. Reproterol hydrochloride is more potent than albuterol and feterol in stimulating cAMP production in human monocytes, demonstrating its potential in enhancing airway function. Furthermore, Reproterol significantly inhibited the production of LTB4, indicating its anti-inflammatory properties. Reproterol hydrochloride may have inhibitory effects in respiratory diseases such as asthma and COPD.
    Reproterol hydrochloride (Standard)
  • HY-10978S
    Crisaborole-d4
    		Inhibitor 98.8%
    Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
    Crisaborole-d<sub>4</sub>
  • HY-145070
    Enpp-1-IN-9
    		Inhibitor
    Enpp-1-IN-9 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-9 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).
    Enpp-1-IN-9
  • HY-170397
    ADORA2A/PDE4D-IN-1
    		Inhibitor
    ADORA2A/PDE4D-IN-1 (Compound 9) is a dual inhibitor for adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). ADORA2A/PDE4D-IN-1 can be used in research of bronchial asthma.
    ADORA2A/PDE4D-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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