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-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
  • HY-18252A
    Avanafil dibenzenesulfonate
    		Inhibitor
    Avanafil (TA-1790) dibenzenesulfonate 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 dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil dibenzenesulfonate
  • HY-B0204S1
    Pimobendan-d3
    		Inhibitor
    Pimobendan-d3 (UD-CG115-d3) is deuterium labeled Pimobendan (HY-B0204). Pimobendan (UD-CG115) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
    Pimobendan-d<sub>3</sub>
  • HY-126250
    NPD-1335
    		Inhibitor 98.10%
    NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death. NPD-1335 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    NPD-1335
  • HY-116808B
    TPN729MA
    		Inhibitor 99.45%
    TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction.
    TPN729MA
  • HY-116808
    TPN729
    		Inhibitor
    TPN729 is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. TPN729 affects erectile function and it can be used for the research of erectile dysfunction.
    TPN729
  • HY-135088
    Autotaxin-IN-4
    		Inhibitor
    Autotaxin-IN-4 (compound 51), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat idiopathic pulmonary fibrosis.
    Autotaxin-IN-4
  • HY-112704
    PDE5-IN-2
    		Inhibitor
    PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.
    PDE5-IN-2
  • HY-128879
    VP3.15
    		Inhibitor
    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
    VP3.15
  • HY-B0809A
    Theophylline monohydrate
    Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline monohydrate
  • HY-106358A
    Andolast
    		Inhibitor
    Andolast (CR 2039) is an anti-allergic agent. Andolast can inhibit cAMP-phosphodiesterase with an IC50 value of 50 μM. Andolast can be used for the research of asthma.
    Andolast
  • HY-130262
    PDE1-IN-3
    		Inhibitor
    PDE1-IN-3, compound 4 (WO2019156861), is a selective human phosphodiesterase 1 (PDE1) inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB with IC50 values of 23.99 μM and 10 μM, respectively.
    PDE1-IN-3
  • HY-128349
    MT-3014
    		Inhibitor
    MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively.
    MT-3014
  • HY-17464S
    Cilostazol-d11
    		Inhibitor
    Cilostazol-d11 is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
    Cilostazol-d<sub>11</sub>
  • HY-15455S1
    Roflumilast-d4 N-Oxide
    		Inhibitor 98.13%
    Roflumilast-d4 N-Oxide 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[1][2].
    Roflumilast-d<sub>4</sub> N-Oxide
  • HY-15025S1
    Sildenafil-d8
    		Inhibitor
    Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM[1][2].
    Sildenafil-d<sub>8</sub>
  • HY-18253S
    Udenafil-d7
    		Inhibitor
    Udenafil-d7 is the deuterium labeled Udenafil. 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[1][2].
    Udenafil-d<sub>7</sub>
  • HY-173640
    ID11916
    		Inhibitor
    ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3.
    ID11916
  • HY-110005
    Sp-cAMPS triethylamine
    		Inhibitor
    Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM.
    Sp-cAMPS triethylamine
  • HY-162912
    Enpp-1-IN-23
    		Inhibitor
    Enpp-1-IN-23 (compound 27) is an Enpp-1 inhibitor, with IC50 of 1.2 nM. Enpp-1-IN-23 can be used in cancer research.
    Enpp-1-IN-23
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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