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-B0051
    Carbazeran
    		Inhibitor
    Carbazeran, a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran can be used for the research of metabolic disease.
    Carbazeran
  • 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-B0204
    Pimobendan
    		Inhibitor 99.82%
    Pimobendan (UD-CG115) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
    Pimobendan
  • HY-B0004
    Doxofylline
    		Inhibitor 99.40%
    Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.
    Doxofylline
  • HY-124772
    BI-2545
    		Inhibitor 98.85%
    BI-2545, a chemical probe, is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively.
    BI-2545
  • HY-B0549A
    Flavoxate hydrochloride
    		Inhibitor 99.70%
    Flavoxate hydrochloride is a potent and competitive phosphodiesterase (PDE) inhibitor. Flavoxate hydrochloride is an antispasmodic agent and muscarinic mAChR antagonist. Flavoxate hydrochloride shows moderate calcium antagonistic activity and local anesthetic effect. Flavoxate hydrochloride can be used for the research of overactive bladder (OAB) and lower urinary tract infections.
    Flavoxate hydrochloride
  • HY-143256
    Enpp-1-IN-12
    		Inhibitor 99.28%
    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-14930
    Mirodenafil
    		Inhibitor 99.88%
    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-N2443
    Tribuloside
    		Inhibitor 99.26%
    Tribuloside is a flavonoid and PDE4 inhibitor (IC50: 6 μM). Tribuloside exhibits antibacterial and antioxidant activities, capable of scavenging DPPH free radicals. Tribuloside also promotes melanogenesis. Tribuloside can be used in the research of hypopigmentary diseases, sun protection, and inflammatory diseases such as acute lung injury.
    Tribuloside
  • HY-108617
    YM976
    		Inhibitor 99.0%
    YM976 is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.2 nM. YM976 shows the dissociation of anti-inflammatory activities from emetic effects and inhibits the antigen-induced airway responses.
    YM976
  • 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-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 99.71%
    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-104028
    BAY 73-6691
    		Inhibitor 99.84%
    BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
    BAY 73-6691
  • HY-136350
    BRD9500
    		Modulator 99.46%
    BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
    BRD9500
  • HY-119190
    PF-06445974
    		Inhibitor 98.59%
    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-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
  • 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-153192A
    Nerandomilast dihydrate
    		Inhibitor 99.93%
    Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).
    Nerandomilast dihydrate
  • HY-117960
    Orismilast
    		Inhibitor 99.88%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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