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-161290
    PDE5-IN-12
    		Inhibitor
    PDE5-IN-12 (compound 4h) is a potent phosphodiesterase-5 (PDE-5) inhibitor with an IC50 of 22 nM. PDE5-IN-12 shows anti-proliferative effects against the aortic cell line.
    PDE5-IN-12
  • HY-153802
    Antitumor agent-100
    Antitumor agent-100 (compound A6) is an orally available apoptosis inducer and molecular gel targeting PDE3A-SLFN12 (IC50: 0.3 μM) with antitumor activity. Antitumor agent-100 binds to the PDE3A enzyme pocket to recruit and stabilize SLFN12, thereby preventing protein translation and leading to apoptosis.
    Antitumor agent-100
  • HY-B0549
    Flavoxate
    		Inhibitor
    Flavoxate is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate can be used for the research of overactive bladder (OAB) and lower urinary tract infections.
    Flavoxate
  • HY-N2958
    Braylin
    		Inhibitor
    Braylin, a coumarin, is a potent phosphodiesterase-4 (PDE4) inhibitor and is involved in anti-inflammatory and immunomodulation, which may serve as a potential target for the study of immunoinflammatory diseases.
    Braylin
  • HY-10679A
    PF-03049423
    		Inhibitor
    PF-03049423 (Compound PF-5) is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 can be used for the research of acute ischaemic stroke.
    PF-03049423
  • HY-B0442AS
    Vardenafil-d5 hydrochloride
    		Inhibitor
    Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
    Vardenafil-d<sub>5</sub> hydrochloride
  • HY-170227
    Autotaxin-IN-7
    		Inhibitor
    Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis.
    Autotaxin-IN-7
  • HY-117181
    UK-1745
    		Inhibitor
    UK-1745 is a cardiotonic agent with vasodilating and antiarrhythmic properties. It increases intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes by inhibiting phosphodiesterase III, thereby enhancing myocardial contractility. Additionally, UK-1745 exhibits β-adrenergic receptor blocking activity, which helps reduce the oxygen consumption of the heart and prevent calcium overload. These characteristics make UK-1745 a promising candidate for research in congestive heart failure.
    UK-1745
  • HY-149661
    PDE5-IN-11
    		Inhibitor
    PDE5-IN-11 is a potent inhibitor of PDE5 with an IC50 of 40 nM. PDE5-IN-11 also inhibits PDE4 and PDE6 with IC50s of 1.78 and 0.09 μM, respectively.
    PDE5-IN-11
  • HY-147946
    PDE1-IN-4
    		Inhibitor
    PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.
    PDE1-IN-4
  • HY-12085S3
    Apremilast-d3
    		Inhibitor
    Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
    Apremilast-d<sub>3</sub>
  • HY-159654
    PDE4-IN-19
    		Inhibitor
    PDE4-IN-19 (compound 1) is a PDE4 inhibitor, with IC50 values of <10 nM and 10-100 nM for PDE4B1 and PDE4D3, respectively.
    PDE4-IN-19
  • HY-147950
    PDE4-IN-10
    		Inhibitor
    PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro.
    PDE4-IN-10
  • HY-N5012R
    Eurycomanone (Standard)
    		Inhibitor
    Eurycomanone (Standard) is the analytical standard of Eurycomanone. This product is intended for research and analytical applications. Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
    Eurycomanone (Standard)
  • HY-169963
    PDE1-IN-8
    		Inhibitor
    PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model.
    PDE1-IN-8
  • HY-114766
    Pumafentrine
    		Inhibitor
    Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting.
    Pumafentrine
  • HY-100239
    ICI 153110
    		Inhibitor
    ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
    ICI 153110
  • HY-15025AR
    Sildenafil (citrate) (Standard)
    		Inhibitor
    Sildenafil (citrate) (Standard) is the analytical standard of Sildenafil (citrate). This product is intended for research and analytical applications. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil (citrate) (Standard)
  • HY-118938
    Hoquizil hydrochloride
    Hoquizil hydrochloride is a novel bronchodilator with oral activity, demonstrating phosphodiesterase inhibitory effects and potential for modulation of smooth muscle contraction.
    Hoquizil hydrochloride
  • HY-14550A
    PDE10-IN-5
    		Inhibitor
    PDE10-IN-5 is a phosphodiesterase 10 (PDE 10) inhibitor, can be used for researching certain central nervous system (CNS) disorders.
    PDE10-IN-5
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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