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-N1289
    Sequosempervirin B
    		Inhibitor
    Sequosempervirin B, a norlignan isolated from the branches and leaves of Sequoia sempervirens, has antifungal properties. Sequosempervirin B has an inhibitory effect on cyclic AMP phosphodiesterase.
    Sequosempervirin B
  • HY-16256
    Amrinone lactate
    		Inhibitor
    Amrinone lactate is a positive inotropic-vasodilator agent. Amrinone lactate is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone lactate is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
    Amrinone lactate
  • HY-12476
    SAR156497
    		Inhibitor
    SAR156497 (compound 47) is an Aurora inhibitor, with IC50 values ​​of 0.6 nM and 1 nM for Aurora A and Aurora B, respectively. SAR156497 can also inhibit PDE3, with IC50 value of 4 μM. SAR156497 can be used in anticancer research.
    SAR156497
  • HY-120684
    PDE10-IN-6
    		Inhibitor
    PDE10-IN-6 is a phosphodiesterase-10 inhibitor that inhibits the breakdown of cAMP and cGMP, thereby slowing or halting their hydrolysis.
    PDE10-IN-6
  • HY-B0442S1
    Vardenafil-d4
    		Inhibitor
    Vardenafil-d4 is deuterium-labeled Vardenafil (HY-B0442).
    Vardenafil-d<sub>4</sub>
  • HY-108680
    Carbazeran citrate
    		Inhibitor
    Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease.
    Carbazeran citrate
  • HY-149018
    ATX inhibitor 22
    		Inhibitor
    ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) with IC50 of 218 nM but lost its inhibitory activity of LPAR1.
    ATX inhibitor 22
  • HY-157886
    TDP1 Inhibitor-3
    		Inhibitor
    TDP1 Inhibitor-3 (Compound 4E) is a (TDP1) inhibitor with an IC50 value of 0.63 μM.
    TDP1 Inhibitor-3
  • HY-101772R
    Ziritaxestat (Standard)
    		Inhibitor
    Ziritaxestat (Standard) is the analytical standard of Ziritaxestat. This product is intended for research and analytical applications. Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM.
    Ziritaxestat (Standard)
  • HY-15455R
    Roflumilast (Standard)
    		Inhibitor
    Roflumilast (Standard) is the analytical standard of Roflumilast. This product is intended for research and analytical applications. Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
    Roflumilast (Standard)
  • HY-90009BS
    cis-Tadalafil-d3
    cis-Tadalafil-d3 is the deuterium labeled cis-Tadalafil[1].
    cis-Tadalafil-d<sub>3</sub>
  • HY-18252S3
    Avanafil-13C5
    		Inhibitor
    Avanafil-13C5 (TA1790-13C5) is 13C labeled Avanafil. Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM 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 cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil-<sup>13</sup>C<sub>5</sub>
  • HY-B0763R
    Ibudilast (Standard)
    		Inhibitor
    Ibudilast (Standard) is the analytical standard of Ibudilast. This product is intended for research and analytical applications. Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
    Ibudilast (Standard)
  • HY-129785
    CP-220629
    		Inhibitor
    CP-220629 is a potent inhibitor of PDE4, with the IC50 of 0.44 μM. CP-220629 is efficacious in the guinea pig aerosolized antigen induced airway obstruction assay (ED50 2.0 mg/kg).
    CP-220629
  • HY-100640
    Roflumilast Impurity E
    		Inhibitor
    Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a agent which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
    Roflumilast Impurity E
  • HY-100936R
    Etazolate hydrochloride (Standard)
    		Inhibitor
    Etazolate (hydrochloride) (Standard) is the analytical standard of Etazolate (hydrochloride). This product is intended for research and analytical applications. Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
    Etazolate hydrochloride (Standard)
  • HY-124392
    AMG580
    		Antagonist
    AMG580 is a selective PDE10A antagonist with subnanomolar affinity for rat, primate, and human PDE10A. AMG580 can be used for the research of noninvasive radiotracer.
    AMG580
  • HY-131823
    5,6-DCl-cBIMP
    		Agonist
    5,6-DCl-cBIMP, a cyclic adenosine monophosphate analog, can act as an agonist of PDE2 and significantly enhance the cAMP and cGMP hydrolytic activities of PDE2.
    5,6-DCl-cBIMP
  • HY-11071
    MK-0952 sodium
    		Inhibitor
    MK-0952 sodium is a selective and orally active PDE4 inhibitor, with an IC50 of 0.53 nM. MK-0952 sodium has the potential for Alzheimer’s disease study.
    MK-0952 sodium
  • HY-12887R
    Piclamilast (Standard)
    		Inhibitor
    Piclamilast (Standard) is the analytical standard of Piclamilast. This product is intended for research and analytical applications. Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.
    Piclamilast (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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