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-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-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)
  • HY-W715511
    N-Desethyl-N-methyl vardenafil
    		Inhibitor
    N-Desethyl-N-methyl vardenafil (Demethyl-vardenafil), an analog of Vardenafil (HY-B0442), is a PDE5 inhibitor with an IC50 value of 0.14 μM.
    N-Desethyl-N-methyl vardenafil
  • HY-108974R
    Drotaverine hydrochloride (Standard)
    		Inhibitor
    Drotaverine (hydrochloride) (Standard) is the analytical standard of Drotaverine (hydrochloride). This product is intended for research and analytical applications. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
    Drotaverine hydrochloride (Standard)
  • HY-B0004S1
    Doxofylline-d4
    		Inhibitor
    Doxofylline-d4 is the deuterium labeled Doxofylline. Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
    Doxofylline-d<sub>4</sub>
  • HY-141555
    5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione
    		Inhibitor
    5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione is a weak inhibitor for snake venom and human recombinant phosphodiesterase 1 with IC50 of 429 and 467 μM. 5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione inhibits mushroom tyrosinase weakly, with Ki of 1.9 μM.
    5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione
  • HY-12085S1
    Apremilast-d8
    		Inhibitor
    Apremilast-d8 (CC-10004-d8) 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>8</sub>
  • HY-136520B
    Xanthoanthrafil
    		Inhibitor
    Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, with an IC50 of 3.95 ng/mL. Xanthoanthrafil can be used for the research of erectile dysfunction.
    Xanthoanthrafil
  • HY-100927R
    Ro 20-1724 (Standard)
    		Inhibitor
    Ro 20-1724 (Standard) is the analytical standard of Ro 20-1724. This product is intended for research and analytical applications. Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect.
    Ro 20-1724 (Standard)
  • HY-131101R
    Nor-Acetildenafil (Standard)
    Nor-Acetildenafil (Standard) is the analytical standard of Nor-Acetildenafil. This product is intended for research and analytical applications. Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
    Nor-Acetildenafil (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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