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-128879A
    VP3.15 dihydrobromide
    Inhibitor 98.01%
    VP3.15 dihydrobromide 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 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
    VP3.15 dihydrobromide
  • HY-123210
    Lodenafil
    Inhibitor 99.94%
    Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
    Lodenafil
  • HY-115383
    Roflupram
    Inhibitor 99.45%
    Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors.
    Roflupram
  • HY-153335
    Enpp-1-IN-16
    Inhibitor 98.46%
    Enpp-1-IN-16 (compound 54) is an ENPP1 inhibitor. Enpp-1-IN-16 has the potential to study cancer, especially in cases of high ENPP1 expression or elevated cytoplasmic DNA levels. Enpp-1-IN-16 can also be used in other diseases mediated by ENPP1, such as bacterial or viral infections, insulin resistance and type II diabetes, chondrocalcinosis and osteoarthritis, calcium pyrophosphate deposition disorder (CPPD), low Phosphatase disease and soft tissue calcification disorders.
    Enpp-1-IN-16
  • HY-N1860
    3-O-Methylquercetin
    Inhibitor 99.98%
    3-O-Methylquercetin is an inhibitor of cAMP and CGMP-phosphodiesterase (PDE) with IC50 at 13.8 μM and 14.3 μM, respectively. 3-O-Methylquercetin is an inhibitor of β-secretase with an IC50 of 6.5 μM. 3-O-Methylquercetin has a neuroprotective effect against neuronal death caused by oxidative damage. 3-O-Methylquercetin has strong antiviral activity against poliovirus, coxsackie virus and human rhinovirus. 3-O-Methylquercetin has anti-inflammatory and trachea-relaxing effects and can be used in the study of inflammatory diseases and asthma.
    3-O-Methylquercetin
  • 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-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone
    Inhibitor 99.86%
    3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma.
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone
  • HY-B0442B
    Vardenafil hydrochloride trihydrate
    Inhibitor 99.67%
    Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
    Vardenafil hydrochloride trihydrate
  • HY-W044525
    Phyllodulcin
    Inhibitor 98.15%
    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-14254A
    Olprinone
    Inhibitor 99.29%
    Olprinone (Loprinone) is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity.
    Olprinone
  • HY-B0327
    Irsogladine
    Inhibitor 99.97%
    Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
    Irsogladine
  • HY-12318G
    IBMX (GMP)
    Inhibitor
    IBMX (3-Isobutyl-1-methylxanthine) (GMP) is IBMX (HY-12318) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor.
    IBMX (GMP)
  • HY-103493
    TAK-915
    Inhibitor 99.57%
    TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment.
    TAK-915
  • HY-107781
    PAT-505
    Inhibitor 99.47%
    PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
    PAT-505
  • HY-153192A
    Nerandomilast dihydrate
    Inhibitor 99.93%
    Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).
    Nerandomilast dihydrate
  • HY-B1505
    Acefylline
    Inhibitor 99.52%
    Acefylline, a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
    Acefylline
  • HY-108974
    Drotaverine hydrochloride
    Inhibitor 99.65%
    Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
    Drotaverine hydrochloride
  • HY-135746
    OR-1896
    Inhibitor 99.04%
    OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
    OR-1896
  • HY-N1465
    Aristolochic acid D
    Inhibitor 99.74%
    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
  • HY-15297
    Vesnarinone
    Inhibitor 98.58%
    Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research.
    Vesnarinone
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