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-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-117954
    CC-3052
    		Inhibitor
    CC-3052 is a phosphodiesterase 4 (PDE4) inhibitor with immunomodulatory activities. CC-3052 reduces neutrophil apoptosis in HIV⁺. CC-3052 is promising for research of HIV-related diseases.
    CC-3052
  • 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)
  • HY-15297R
    Vesnarinone (Standard)
    		Inhibitor
    Vesnarinone (Standard) is the analytical standard of Vesnarinone. This product is intended for research and analytical applications. Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research.
    Vesnarinone (Standard)
  • HY-B1209R
    Etofylline (Standard)
    		Inhibitor
    Etofylline (Standard) is the analytical standard of Etofylline. This product is intended for research and analytical applications. Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.
    Etofylline (Standard)
  • HY-N0579R
    Fraxin (Standard)
    		Inhibitor
    Fraxin (Standard) is the analytical standard of Fraxin. This product is intended for research and analytical applications. Fraxin isolated from Cortex Fraxini, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action, anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme.
    Fraxin (Standard)
  • HY-139096
    4-Pentadecylbenzylphosphonic acid
    		Inhibitor
    4-Pentadecylbenzylphosphonic acid is an Autotaxin (ATX) inhibitor. 4-Pentadecylbenzylphosphonic acid has antitumor activity.
    4-Pentadecylbenzylphosphonic acid
  • HY-119799
    UK-500001
    		Inhibitor
    UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma.
    UK-500001
  • HY-149716
    MEY-003
    MEY-003 is an Autotaxin(ATX) inhibitor with EC50s of 460 nM and 1.09 μM for hATX-β and hATX-ɣ (analysis with LPC18:1). MEY-003 behaves as a non-competitive inhibitor with K iof 432 nM. MEY-003 can be used for targeted ATX-related disease research .
    MEY-003
  • HY-B0715S3
    Pentoxifylline-d3
    		Inhibitor
    Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
    Pentoxifylline-d<sub>3</sub>
  • HY-10790R
    Cilomilast (Standard)
    		Inhibitor
    Cilomilast (Standard) is the analytical standard of Cilomilast. This product is intended for research and analytical applications. Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 μM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).
    Cilomilast (Standard)
  • HY-155165
    Dazonone
    		Inhibitor
    Dazonone is a phosphodiesterase III inhibitor with the IC50 of 1.68 μM.
    Dazonone
  • HY-B0764R
    Bucladesine sodium (Standard)
    		Inhibitor
    Bucladesine (sodium) (Standard) is the analytical standard of Bucladesine (sodium). This product is intended for research and analytical applications. Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
    Bucladesine sodium (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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