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-102050R
    PF-05085727 (Standard)
    		Inhibitor
    PF-05085727 (Standard) is the analytical standard of PF-05085727 (HY-102050). This product is intended for research and analytical applications. PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.
    PF-05085727 (Standard)
  • HY-172297
    Pyrazole N-Desmethyl sildenafil
    		Inhibitor
    Pyrazole N-Desmethyl sildenafil (Compound 10) is an analog of Sildenafil (HY-15025). Pyrazole N-Desmethyl sildenafil shows 16% inhibition on Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) with 100 µM.
    Pyrazole N-Desmethyl sildenafil
  • HY-50098R
    Mardepodect (Standard)
    		Inhibitor
    Mardepodect (Standard) is the analytical standard of Mardepodect. This product is intended for research and analytical applications. Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.
    Mardepodect (Standard)
  • HY-106996
    AWD 12-281
    		Inhibitor 98.07%
    AWD 12-281 is an orally active and highly selective phosphodiesterase 4 (PDE4) inhibitor (IC50 = 9.7 nM). AWD 12-281 is used in the study of allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis.
    AWD 12-281
  • HY-105092R
    Tetomilast (Standard)
    		Inhibitor
    Tetomilast (Standard) is the analytical standard of Tetomilast (HY-105092). This product is intended for research and analytical applications. Tetomilast (OPC-6535) is a PDE4 inhibitor with potential for the research of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).
    Tetomilast (Standard)
  • HY-101803R
    CP671305 (Standard)
    		Inhibitor
    CP671305 (Standard) is the analytical standard of CP671305 (HY-101803). This product is intended for research and analytical applications. CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
    CP671305 (Standard)
  • HY-B0204S2
    Pimobendan-d4
    		Inhibitor
    Pimobendan-d4 (UD-CG115-d4) is deuterium labeled Pimobendan (HY-B0204). Pimobendan (UD-CG115) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
    Pimobendan-d<sub>4</sub>
  • HY-106830
    Pelrinone
    		Inhibitor
    Pelrinone is an orally active cardiotonic agent and PDE III inhibitor with an IC50 of 36 μM. Pelrinone elevates intracellular cAMP levels. The action of Pelrinone is independent of β-adrenergic receptors, and it does not inhibit Na+/K+-ATPase. Pelrinone exerts positive inotropic and vasodilatory effects. Pelrinone inhibits platelet aggregation, reduces thrombus formation, and exerts weak anticoagulant activity without altering hematocrit or circulating platelet counts. Pelrinone can be used in research related to congestive heart failure and coronary thrombosis.
    Pelrinone
  • HY-103024R
    ICI-63197 (Standard)
    		Inhibitor
    ICI-63197 (Standard) is the analytical standard of ICI-63197 (HY-103024). This product is intended for research and analytical applications. ICI-63197 is a phosphodiesterase 3 (PDE3) and PDE4 inhibitor with Ki values of 9 µM and 10 µM, respectively. ICI-63197 is selectivity against PDE1 and PDE2. ICI-63197 has antidepressant effects.
    ICI-63197 (Standard)
  • HY-129474
    MP 518
    		Inhibitor
    MP 518 is a PDE inhibitor with antihypertensive properties. MP 518 can inhibit cAMP degradation, causing an increase in ICa, and can also antagonize β-adrenergic stimulation, exerting vasodilation.
    MP 518
  • HY-29268
    β-Carboline-1-carboxylic acid
    		Inhibitor
    β-Carboline 1-carboxylic acid is a β-carboline alkaloid with anti-inflammatory, antifibrotic, antitumor and antibacterial activities. β-Carboline 1-carboxylic acid is the cAMP phosphodiesterase (IC50: 96 µM) and indoleamine 2, 3-dioxygenase (IDO) inhibitor. β-Carboline 1-carboxylic acid is cytotoxic to tumor cells. β-Carboline 1-carboxylic acid inhibits inflammation through the NF-κb/p65 pathway and can reverse epithelial-mesenchymal transition (EMT). In addition, β-Carboline 1-carboxylic acid has strong inhibitory activity against S. aureus (IC50: 47.70 μg/mL) and E. coli (IC50: 19.17 μg/mL).
    β-Carboline-1-carboxylic acid
  • HY-13344AR
    PF-8380 hydrochloride (Standard)
    		Inhibitor
    PF-8380 (hydrochloride) (Standard) is the analytical standard of PF-8380 (hydrochloride). This product is intended for research and analytical applications. PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
    PF-8380 hydrochloride (Standard)
  • HY-17464R
    Cilostazol (Standard)
    		Inhibitor
    Cilostazol (Standard) is the analytical standard of Cilostazol. This product is intended for research and analytical applications. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM.
    Cilostazol (Standard)
  • HY-B0204A
    Pimobendan hydrochloride
    		Inhibitor
    Pimobendan hydrochloride (UD-CG115 hydrochloride) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
    Pimobendan hydrochloride
  • HY-70069R
    GSK256066 Trifluoroacetate (Standard)
    		Inhibitor
    GSK256066 (Trifluoroacetate) (Standard) is the analytical standard of GSK256066 (Trifluoroacetate). This product is intended for research and analytical applications. GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.
    GSK256066 Trifluoroacetate (Standard)
  • HY-B0531R
    Triflusal (Standard)
    		Inhibitor
    Triflusal (Standard) is the analytical standard of Triflusal (HY-B0531). This product is intended for research and analytical applications. Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
    Triflusal (Standard)
  • HY-B1505R
    Acefylline (Standard)
    		Inhibitor
    Acefylline (Theophyllineacetic acid) (Standard) is the analytical standard of Acefylline (HY-B1505). This product is intended for research and analytical applications. Acefylline (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.
    Acefylline (Standard)
  • HY-14930AR
    Mirodenafil dihydrochloride (Standard)
    		Inhibitor
    Mirodenafil (dihydrochloride) (Standard) is the analytical standard of Mirodenafil (dihydrochloride). This product is intended for research and analytical applications. Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil dihydrochloride (Standard)
  • HY-W740060
    Dipyridamole Mono-O-β-D-glucuronide
    		Inhibitor
    Dipyridamole Mono-O-β-D-glucuronide (compound M4) is a derivative of the phosphodiesterase (PDE) and BCRP inhibitor Dipyridamole (HY-B0312) and is an O-glucuronide.
    Dipyridamole Mono-O-β-D-glucuronide
  • HY-19026R
    Siguazodan (Standard)
    		Inhibitor
    Siguazodan (Standard) is the analytical standard of Siguazodan. This product is intended for research and analytical applications. Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
    Siguazodan (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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