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  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. Nom du produit Effet Pureté Chemical Structure
  • HY-130786
    Denbufylline
    		Inhibitor 99.92%
    Denbufylline (BRL 30892) is an inhibitor of phosphodiesterase-4 (PDE4). Denbufylline is able to block the degradation of intracellular cAMP (cyclic adenosine phosphate) thereby increasing the level of intracellular cAMP, which helps regulate a variety of cellular functions. Denbufylline can be used in the study of chronic obstructive pulmonary disease (COPD), asthma and other inflammatory diseases.
    Denbufylline
  • HY-12085R
    Apremilast (Standard)
    		Inhibitor
    Apremilast (Standard) is the analytical standard of Apremilast. This product is intended for research and analytical applications. 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 (Standard)
  • HY-12501
    ITI-214 free base
    		Inhibitor 98.0%
    ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
    ITI-214 free base
  • HY-121162
    Mesembrine
    		Inhibitor
    Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM.
    Mesembrine
  • HY-113547
    Nanterinone
    		Inhibitor 99.87%
    Nanterinone (UK 61260) is a positive inotropic and arterial vasodilating agent. Nanterinone is a phosphodiesterase inhibitor.
    Nanterinone
  • HY-119855
    Aildenafil
    		Inhibitor 98.46%
    Aildenafil (Methisosildenafil) is a PDE-5 inhibitor that can induce vasodilation by increasing NO levels.
    Aildenafil
  • HY-101693
    Senazodan
    		Inhibitor
    Senazodan (MCI 154) is a Ca2+ sensitiser, and also shows inhibition effect on PDE III.
    Senazodan
  • HY-19102
    NSP-805
    		Inhibitor 99.28%
    NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
    NSP-805
  • HY-119708S
    Ensifentrine-d6
    		Inhibitor
    Ensifentrine-d6 (RPL-554-d6) is deuterium labeled Ensifentrine. Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research.
    Ensifentrine-d<sub>6</sub>
  • HY-117605R
    N-Desmethyl Sildenafil (Standard)
    		Inhibitor
    N-Desmethyl Sildenafil (Standard) is the analytical standard of N-Desmethyl Sildenafil. This product is intended for research and analytical applications. N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.
    N-Desmethyl Sildenafil (Standard)
  • HY-43934
    Tiropramide hydrochloride
    		Inhibitor
    Tiropramide (CR 605) hydrochloride is a tyrosine derivative with antispastic properties. Tiropramide hydrochloride inhibits phosphodiesterase activity involved in cAMP catabolism in rabbit colon homogenates. Tiropramide hydrochloride relaxes smooth muscle in rabbit isolated colon. Tiropramide hydrochloride can be used for the research of irritable colon and biliary dyskinesia.
    Tiropramide hydrochloride
  • HY-15747A
    Deltarasin hydrochloride
    		Inhibitor 98.07%
    Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.
    Deltarasin hydrochloride
  • HY-16900R
    Rolipram (Standard)
    		Inhibitor
    Rolipram (Standard) is the analytical standard of Rolipram (HY-16900). This product is intended for research and analytical applications. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.
    Rolipram (Standard)
  • HY-102043
    PDM-631
    		Inhibitor
    PDM-631 is a selective and orally active PDE2A inhibitor with blood-brain barrier penetration. PDM-631 exhibits potent inhibitory activity against human and rat recombinant PDE2A with IC50 values of 1.5 nM and 4.2 nM, respectively. PDM-631 increases cGMP levels in the rat cerebral cortex. PDM-631 can be used for the study of schizophrenia and neurodegenerative disorders.
    PDM-631
  • HY-144683
    PF-07038124
    		Inhibitor
    PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1, 1.06 nM, respectively). PF-07038124 can be used for research of atopic dermatitis and plaque psoriasis.
    PF-07038124
  • HY-131340
    LASSBio-1632
    		Inhibitor
    LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.
    LASSBio-1632
  • HY-15455S
    Roflumilast-d4
    		Inhibitor
    Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast 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-d<sub>4</sub>
  • HY-120741
    PF-04822163
    		Inhibitor
    PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC50 values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease.
    PF-04822163
  • HY-107191
    Sildenafil Mesylate
    		Inhibitor
    Sildenafil Mesylate is an orally active and selective phosphodiesterase type 5 (PDE5) inhibitor. Sildenafil Mesylate can be used in studies of erectile dysfunction and cancer.
    Sildenafil Mesylate
  • HY-B0442C
    Vardenafil dihydrochloride
    		Inhibitor
    Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes-.
    Vardenafil dihydrochloride
Cat. No. Nom du produit / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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