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-114303
    CM-675
    		Inhibitor 99.53%
    CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease.
    CM-675
  • HY-B0809R
    Theophylline (Standard)
    		Inhibitor 99.99%
    Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline (Standard)
  • HY-B1742
    Proxyphylline
    		99.93%
    Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline
  • HY-W050000
    OR-1855
    		Inhibitor 98.31%
    OR-1855, an active metabolite of Levosimendan, has effect on human myometrial contractility. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.
    OR-1855
  • HY-90009
    Nortadalafil
    		Inhibitor 99.71%
    Nortadalafil (Demethyl Tadalafil), a tadalafil (HY-90009A) analogue detected in health foods, is a highly selective PDE5 inhibitor. Nortadalafil is used in the research of erectile dysfunction (ED). Nortadalafil can be formed by closing the diketopiperazine ring in high yield. Nortadalafil is promising for research of pulmonary arterial hypertension.
    Nortadalafil
  • HY-117605
    N-Desmethyl Sildenafil
    		Inhibitor 99.53%
    N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.
    N-Desmethyl Sildenafil
  • HY-15178
    Oglemilast
    		Inhibitor 98.00%
    Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
    Oglemilast
  • HY-N2168
    Pinoresinol 4-O-β-D-glucopyranoside
    		Inhibitor 99.89%
    Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects.
    Pinoresinol 4-O-β-D-glucopyranoside
  • HY-B0442B
    Vardenafil hydrochloride trihydrate
    		Inhibitor 99.67%
    Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
    Vardenafil hydrochloride trihydrate
  • HY-100326
    PDE7-IN-3
    		Inhibitor 99.94%
    Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain.
    PDE7-IN-3
  • HY-70069
    GSK256066 Trifluoroacetate
    		Inhibitor 99.54%
    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
  • HY-W044525
    Phyllodulcin
    		Inhibitor 98.15%
    Phyllodulcin is an orally active sweetener found in Hydrangea macrophylla var. thunbergii. Phyllodulcin acts as a non-selective phosphodiesterase inhibitor and exerts anti-allergic effects by suppressing lymphocyte activation. Phyllodulcin can be used to combat obesity by regulating levels of leptin, fat browning-related genes, and hypothalamic BDNF-TrkB signaling.
    Phyllodulcin
  • HY-B1209
    Etofylline
    		Inhibitor 99.72%
    Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos.
    Etofylline
  • HY-145561
    Cudetaxestat
    		Inhibitor 98.04%
    Cudetaxestat (BLD-0409) is a potent and orally active autotaxin (ATX) inhibitor.
    Cudetaxestat
  • HY-106003
    GSK356278
    		Inhibitor 99.82%
    GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.
    GSK356278
  • HY-100933
    MY-5445
    		Inhibitor 99.86%
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
    MY-5445
  • HY-145583
    Mufemilast
    		Inhibitor 99.67%
    Mufemilast (Heymay005) is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor (IC50 = 80-120 nM). Mufemilast modulates cytokines upregulated in Behςet’s syndrome (BS). Mufemilast displays a significant inhibitory effect on TNF-α, which is an important proinflammatory cytokine target in the disease process of psoriasis. Mufemilast can be studied in research for diseases such as rheumatoid arthritis, psoriasis and BS.
    Mufemilast
  • HY-126137
    PDE9-IN-1
    		Inhibitor 99.70%
    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
    PDE9-IN-1
  • HY-U00186
    K134
    		Inhibitor 99.84%
    K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
    K134
  • HY-100246
    CI-1044
    		Inhibitor 98.02%
    CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
    CI-1044
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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