2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-176708
    ISM5939 Inhibitor 99.79%
    ISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.
    ISM5939
  • 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-136637
    NPD-001 Inhibitor 98.11%
    NPD-001 is a potent Trypanosoma brucei phosphodiesterases 1/2 (TbrPDEB1/2) inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits hPDE4. NPD-001 can increase cAMP levels in parasites, prevent cytokinesis, and cause the parasites to form multinucleated, multi-flagellated cells that eventually lyse. NPD-001 can be used for the research of infection.
    NPD-001
  • HY-136569
    DSR-141562 Inhibitor 99.98%
    DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
    DSR-141562
  • HY-155457
    Enpp-1-IN-19 Inhibitor 99.28%
    Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC50=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence.
    Enpp-1-IN-19
  • 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-B1294
    Amrinone

    アムリノン

    		Inhibitor 99.93%
    Amrinone (Inamrinone) is a positive inotropic-vasodilator agent. Amrinone is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
    Amrinone
  • HY-W044525
    Phyllodulcin Inhibitor 99.75%
    Phyllodulcin is an orally active sweetener found in Hydrangea macrophylla var. thunbergii. Phyllodulcin acts as a non-selective phosphodiesterase inhibitor and exerts anti-allergic effects by suppressing lymphocyte activation. Phyllodulcin can be used to combat obesity by regulating levels of leptin, fat browning-related genes, and hypothalamic BDNF-TrkB signaling.
    Phyllodulcin
  • 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
  • HY-122751
    (R)-DNMDP Inhibitor 99.59%
    (R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line.
    (R)-DNMDP
  • HY-15178
    Oglemilast Inhibitor 99.97%
    Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
    Oglemilast
  • HY-50098A
    Mardepodect hydrochloride Inhibitor 99.94%
    Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
    Mardepodect hydrochloride
  • HY-119372
    TDP1 Inhibitor-1 Inhibitor 98.33%
    TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM. TDP1 Inhibitor-1 shows cytotoxicity against multiple cancer cells. TDP1 Inhibitor-1 can be used for the research of cancer, such as breast cancer.
    TDP1 Inhibitor-1
  • HY-117318
    PDE12-IN-1 Inhibitor 99.11%
    PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity.
    PDE12-IN-1
  • HY-145583
    Mufemilast Inhibitor 99.67%
    Mufemilast (Heymay005) is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor (IC50 = 80-120 nM). Mufemilast modulates cytokines upregulated in Behςet’s syndrome (BS). Mufemilast displays a significant inhibitory effect on TNF-α, which is an important proinflammatory cytokine target in the disease process of psoriasis. Mufemilast can be studied in research for diseases such as rheumatoid arthritis, psoriasis and BS.
    Mufemilast
  • HY-B1639
    Enoximone

    Enoximone

    		Inhibitor 99.91%
    Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
    Enoximone
  • HY-12788
    PF-04449613

    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-144683A
    PF-07038124 hydrochloride Inhibitor 99.26%
    PF-07038124 hydrochloride is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 hydrochloride shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1, 1.06 nM, respectively). PF-07038124 hydrochloride can be used for research of atopic dermatitis and plaque psoriasis.
    PF-07038124 hydrochloride
  • HY-106230A
    Dasantafil Inhibitor 98.35%
    Dasantafil (SCH-446132) is a small molecule phosphodiesterase-5A (PDE5A) inhibitor used to in genitourinary disorders and study erectile dysfunction.
    Dasantafil
  • HY-128879A
    VP3.15 dihydrobromide Inhibitor 98.0%
    VP3.15 dihydrobromide is a highly potent, orally bioavailable, and CNS-penetrant PDE7-GSK3 dual inhibitor, with IC50 values of 1.59 μM and 0.88 μM against PDE7 and GSK3, respectively. VP3.15 dihydrobromide elevates intracellular cAMP levels, suppresses immune responses, enhances remyelination, limits excessive tau phosphorylation, and alleviates neuroinflammation and neuronal loss. VP3.15 dihydrobromide promotes oligodendrocyte precursor cell differentiation, improves in vivo remyelination, inhibits autoimmune encephalomyelitis, and mitigates germinal matrix-intraventricular hemorrhage-related brain injury, cerebral atrophy, ventricular enlargement, and cognitive impairment. VP3.15 dihydrobromide can be used in research related to multiple sclerosis and germinal matrix-intraventricular hemorrhage.
    VP3.15 dihydrobromide
製品番号 製品名 / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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