1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-178987
    BJH-86
    Inhibitor
    BJH-86 is a soluble mitochondrial complex 1 inhibitor (oxygen consumption rate inhibition IC50 = 5 μM). BJH-86 exhibits weak inhibitory activity against phosphodiesterase 10A (PDE10A) (IC50 >10 μM). BJH-86 can reduce cellular oxygen consumption and inhibit cancer cell proliferation. BJH-86 can be used for the research of cancer, such as lung cancer.
    BJH-86
  • HY-182271
    GPR61 Inverse agonist 3
    Inhibitor
    GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia.
    GPR61 Inverse agonist 3
  • HY-168558
    PDE4B/D-IN-4
    Inhibitor
    PDE4B/D-IN-4 (compound 4p) is a potent inhibitor of PDE-4B and PDE-4D, with IC50s of 5.50 nM and 6.81 nM, respectively. PDE4B/D-IN-4 shows an increase in the level of intracellular cAMP.
    PDE4B/D-IN-4
  • HY-106044
    Etazolate
    Inhibitor
    Etazolate (SQ 64442) is a α-secretase activator, selective PDE4 inhibitor, selective GABAA receptor modulator. Etazolate reduces IL-1β levels Etazolate exerts a dose-dependent anti-inflammatory and anti-œdematous effect accompanied by lasting memory improvement. Etazolate produces an antidepressant-like effect.
    Etazolate
  • HY-14458
    SCH-1518291
    Inhibitor
    SCH-1518291 (Compound 27) is an orally active PDE10A inhibitor. SCH-1518291 exhibits antipsychotic activity in an ADHD rat model. SCH-1518291 can be used in research on neurological disorders such as psychosis.
    SCH-1518291
  • HY-W700639
    Tolafentrine
    Inhibitor
    Tolafentrine, a dual-selective phosphodiesterase 3/4 (PDE3/4) inhibitor, has been shown to have significant acute and chronic effects in a unilateral diacetamide-induced rat pulmonary hypertension model. Experiments show that long-term administration can significantly alleviate all unilateral bisacetamide-induced hemodynamic and gas exchange abnormalities, reduce right ventricular hypertrophy, and normalize pulmonary vascular remodeling changes.
    Tolafentrine
  • HY-155199
    PDE1-IN-5
    Inhibitor
    PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD.
    PDE1-IN-5
  • HY-105647
    Ambuphylline
    Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases.
    Ambuphylline
  • HY-182638
    CPL500036
    Inhibitor
    CPL500036 is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). CPL500036 acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. CPL500036 alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. CPL500036 induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. CPL500036 can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia.
    CPL500036
  • HY-124371
    Amentoflavone hexaacetate
    Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects.
    Amentoflavone hexaacetate
  • HY-158237
    PDE10A-IN-3
    Inhibitor
    PDE10A-IN-3 (Compound 8a) is an inhibitor of phosphodiesterase 10A (PDE10A). PDE10A-IN-3 can be used in schizophrenia research.
    PDE10A-IN-3
  • HY-111164
    CBS-3595
    Inhibitor
    CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases.
    CBS-3595
  • HY-N1465R
    Aristolochic acid D (Standard)
    Inhibitor
    Aristolochic acid D (Standard) (Aristolochic acid-IVa (Standard)) is the analytical standard of Aristolochic acid D (HY-N1465). This product is intended for research and analytical applications. Aristolochic acid D (Aristolochic acid-IVa) is an orally active PDE2 (IC50: 4.673 μM) and CDK2 (IC50: 25 μM) inhibitor that can be isolated from Aristolochia indica L. Aristolochic acid D exhibits anti-inflammatory activity and is non-carcinogenic and non-nephrotoxic. Aristolochic acid D can be used in the research of inflammation and tumor-related diseases.
    Aristolochic acid D (Standard)
  • HY-150060
    PDE4-IN-11
    Inhibitor
    PDE4-IN-11 is an inhibitor of phosphodiesterase isoenzyme 4 (PDE4). PDE4-IN-11 displays highly effective bronchodilatory and anti-inflammatory properties, can be used for obstructive or inflammatory airway diseases research.
    PDE4-IN-11
  • HY-122622
    PF-04471141 hydrochloride
    Inhibitor
    PF-04471141 (hydrochloride) is a compound that regulates intracellular cAMP and cGMP concentrations. It is a PDE1 inhibitor and has different effects on different PDE enzymes in regulating intracellular signaling molecule concentrations and cell proliferation in vascular smooth muscle cells.
    PF-04471141 hydrochloride
  • HY-201403
    LY2775240
    Inhibitor
    LY2775240 is an orally active phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC50 = 0.09 nM), PDE4B (IC50 = 0.09 nM) and PDE4D (IC50 = 0.14 nM), and exhibits an IC50 of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production upon immune activation. LY2775240 decreases TNFα production in rodent and rhesus monkey models. LY2775240 can be used in the research of psoriasis.
    LY2775240
  • HY-161663
    Phosphodiesterase-IN-2
    Inhibitor
    Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models.
    Phosphodiesterase-IN-2
  • HY-167891
    GPD-1116
    Inhibitor
    GPD-1116 is an orally active Phosphodiesterase (PDE) 4 and PDE1 inhibitor. GPD-1116 can reduce smoke-induced apoptosis of lung cells. GPD-1116 is effective in several disease models in animals, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma and pulmonary hypertension.
    GPD-1116
  • HY-146122
    ATX inhibitor 19
    Inhibitor
    ATX inhibitor 19 (compound 22) is a potent ATX (autotaxin) inhibitor, with an IC50 of 156 nM.
    ATX inhibitor 19
  • HY-120710
    DNS-8254
    Inhibitor
    DNS-8254 is an oral active and brain-penetrating PDE2a inhibitor with the IC50 of 8 nM. DNS-8254 shows memory enhancing effects in a rat model.
    DNS-8254
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