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-N1289
    Sequosempervirin B
    		Inhibitor
    Sequosempervirin B, a norlignan isolated from the branches and leaves of Sequoia sempervirens, has antifungal properties. Sequosempervirin B has an inhibitory effect on cyclic AMP phosphodiesterase.
    Sequosempervirin B
  • HY-19091
    ICI-170777
    		Inhibitor
    ICI-170777 is an orally active cardiotonic agent and type III Phosphodiesterase inhibitor, with an IC50 of 2.5 μM against cyclic AMP phosphodiesterase type III from canine cardiac fractions. ICI-170777 inhibits Aldrin epoxidase and pentobarbital metabolism. It enhances β-adrenergic receptor-mediated positive inotropic effects without causing chronotropic effects, while also exerting balanced arteriolar/venular vasodilator, platelet aggregation inhibitor and smooth muscle relaxant activities. ICI-170777 restores cardiac function in an acute canine heart failure model, exhibits additive effects when combined with Ouabain (HY-B1457), and shows no significant activity against multiple receptor classes or non-cardiac systems. ICI-170777 can be used in research related to congestive heart failure.
    ICI-170777
  • HY-16256
    Amrinone lactate
    		Inhibitor
    Amrinone lactate is a positive inotropic-vasodilator agent. Amrinone lactate is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone lactate is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
    Amrinone lactate
  • HY-15179
    Ronomilast
    		Inhibitor
    Ronomilast (Elbimilast; ELB353) is an orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 3 nM. Revamilast can be used for research to inflammation related diseases.
    Ronomilast
  • HY-12476
    SAR156497
    		Inhibitor
    SAR156497 (compound 47) is an Aurora inhibitor, with IC50 values ​​of 0.6 nM and 1 nM for Aurora A and Aurora B, respectively. SAR156497 can also inhibit PDE3, with IC50 value of 4 μM. SAR156497 can be used in anticancer research.
    SAR156497
  • HY-178478
    PDE1-IN-11
    		Inhibitor 99.24%
    PDE1-IN-11 (Compound 5cc) is an orally active and highly selective PDE1A1 inhibitor. PDE1-IN-11 increases intracellular cAMP and cGMP levels, activating the PKA-CREB and NO-cGMP-PKG signaling pathways, promoting osteoblast differentiation and bone formation, while suppressing osteoclastogenesis and bone resorption. PDE1-IN-11 is promising for research of postmenopausal osteoporosis (PMO) and other bone metabolism disorders.
    PDE1-IN-11
  • HY-120684
    PDE10-IN-6
    		Inhibitor
    PDE10-IN-6 is a phosphodiesterase-10 inhibitor that inhibits the breakdown of cAMP and cGMP, thereby slowing or halting their hydrolysis.
    PDE10-IN-6
  • HY-B0442S1
    Vardenafil-d4
    		Inhibitor
    Vardenafil-d4 is deuterium-labeled Vardenafil (HY-B0442).
    Vardenafil-d<sub>4</sub>
  • HY-114218
    BL-122
    		Inhibitor
    BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor. BL-122 can increase the level of cGMP in the tissue, promote the expression of nitric oxide (NO), and mediate the relaxation of smooth muscle. BL-122 can be used for the researches of inflammation, immunology and cardiovascular disease, such as asthma and hypertension.
    BL-122
  • HY-105341
    UK 343664
    		Inhibitor
    UK 343664 is a potent, orally active and selective PDE5 inhibitor. UK 343664 partially reverses Thromboxane-induced pulmonary hypertension.
    UK 343664
  • HY-108680
    Carbazeran citrate
    		Inhibitor
    Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease.
    Carbazeran citrate
  • HY-149018
    ATX inhibitor 22
    		Inhibitor
    ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) with IC50 of 218 nM but lost its inhibitory activity of LPAR1.
    ATX inhibitor 22
  • HY-101772R
    Ziritaxestat (Standard)
    		Inhibitor
    Ziritaxestat (Standard) is the analytical standard of Ziritaxestat. This product is intended for research and analytical applications. Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM.
    Ziritaxestat (Standard)
  • HY-15455R
    Roflumilast (Standard)
    		Inhibitor
    Roflumilast (Standard) is the analytical standard of Roflumilast. This product is intended for research and analytical applications. Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
    Roflumilast (Standard)
  • HY-100530CR
    Sp-cAMPS sodium salt (Standard)
    		Inhibitor
    Sp-cAMPS (sodium salt) (Standard) is the analytical standard of Sp-cAMPS (sodium salt) (HY-100530C). This product is intended for research and analytical applications. 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 (Standard)
  • HY-90009BS
    cis-Tadalafil-d3
    cis-Tadalafil-d3 is the deuterium labeled cis-Tadalafil[1].
    cis-Tadalafil-d<sub>3</sub>
  • HY-P2209
    Nummularine B
    		Inhibitor
    Nummularine B (Daechuine S27; N-Demethylamphibine H) is an anti-parasite agent. Nummularine B inhibits calmodulin-dependent phosphodiesterase activity with an IC50 of 16.8 μM. Nummularine B inhibits the growth of Plasmodium and Leishmania donovani in vitro. Nummularine B inhibits the calmodulin-dependent activity of actomyosin Ca2+-ATPase. Nummularine B is applicable to research related to malaria and visceral leishmaniasis.
    Nummularine B
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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