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-117960
    Orismilast
    		Inhibitor 99.37%
    Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants.
    Orismilast
  • HY-A0027
    Fenspiride hydrochloride
    		Inhibitor 99.11%
    Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
    Fenspiride hydrochloride
  • HY-143256
    Enpp-1-IN-12
    		Inhibitor 99.06%
    Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity.
    Enpp-1-IN-12
  • HY-N1938
    D(+)-Raffinose pentahydrate
    		Activator ≥98.0%
    D(+)-Raffinose pentahydrate is an orally active inhibitor of LecA (Kd = 32 μM) and GtfC. D(+)-Raffinose pentahydrate reduces cyclic diguanylate (c-di-GMP) by increased activity of a c-di-GMP specific phosphodiesterase. D(+)-Raffinose pentahydrate interferes with GTF function. D(+)-Raffinose pentahydrate decreases IL-4 and IL-5 mRNA. D(+)-Raffinose pentahydrate exhibits biofilm-inhibitory activity against Pseudomonas aeruginosa and Streptococcus mutans and inhibits allergic airway eosinophilia.
    D(+)-Raffinose pentahydrate
  • HY-102050
    PF-05085727
    		Inhibitor 99.53%
    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
  • HY-145344
    ONO-8430506
    		Inhibitor 99.68%
    ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.
    ONO-8430506
  • HY-15485
    Zardaverine
    		Inhibitor 98.64%
    Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma.
    Zardaverine
  • HY-B0204
    Pimobendan
    		Inhibitor 99.82%
    Pimobendan (UD-CG115) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
    Pimobendan
  • HY-12788
    PF-04449613
    		Inhibitor 99.83%
    PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM[1]. PF-04449613 improved motor learning ability in a mouse model[2].
    PF-04449613
  • HY-14930
    Mirodenafil
    		Inhibitor 99.70%
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil
  • HY-100639
    Roflumilast N-oxide
    		Inhibitor 99.52%
    Roflumilast N-oxide is a PDE type 4 inhibitor.
    Roflumilast N-oxide
  • HY-B0051
    Carbazeran
    		Inhibitor 98.31%
    Carbazeran, a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran can be used for the research of metabolic disease.
    Carbazeran
  • HY-101762
    TyK2-IN-2
    		Inhibitor 98.64%
    TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.
    TyK2-IN-2
  • HY-100530C
    Sp-cAMPS sodium salt
    		Inhibitor 99.45%
    Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
    Sp-cAMPS sodium salt
  • HY-115383
    Roflupram
    		Inhibitor 99.45%
    Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors.
    Roflupram
  • HY-119190
    PF-06445974
    		Inhibitor 98.23%
    PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study.
    PF-06445974
  • HY-P2878
    Phosphodiesterase I
    Phosphodiesterase I (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclic nucleotides, and is often used in biochemical research. Phosphodiesterase I acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclic nucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases.
    Phosphodiesterase I
  • HY-19929
    Tanimilast
    		Inhibitor 99.49%
    Tanimilast (CHF-6001) is an orally active and selective phosphodiesterase 4 inhibitor (IC50=0.026 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration. Tanimilast increases cellular cAMP levels, and inhibits NF-κB signaling pathway. Tanimilast is used for the research of obstructive lung diseases.
    Tanimilast
  • HY-12740
    Lotamilast
    		Inhibitor ≥98.0%
    Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
    Lotamilast
  • HY-18253
    Udenafil
    		Inhibitor 99.67%
    Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research.
    Udenafil
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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