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-W050000
    OR-1855
    Inhibitor ≥98.0%
    OR-1855, an active metabolite of Levosimendan, has effect on human myometrial contractility. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.
    OR-1855
  • 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
  • HY-90009
    Nortadalafil
    Inhibitor 99.71%
    Nortadalafil (Demethyl Tadalafil), a tadalafil (HY-90009A) analogue detected in health foods, is a highly selective PDE5 inhibitor. Nortadalafil is used in the research of erectile dysfunction (ED). Nortadalafil can be formed by closing the diketopiperazine ring in high yield. Nortadalafil is promising for research of pulmonary arterial hypertension.
    Nortadalafil
  • HY-117605
    N-Desmethyl Sildenafil
    Inhibitor 99.53%
    N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.
    N-Desmethyl Sildenafil
  • HY-15178
    Oglemilast
    Inhibitor 98.00%
    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-N2168
    Pinoresinol 4-O-β-D-glucopyranoside
    Inhibitor 99.89%
    Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor, with an IC50 of 48.13 μg/mL. Pinoresinol 4-O-β-D-glucopyranoside binds to estrogen receptors. Pinoresinol 4-O-β-D-glucopyranoside inhibits phosphodiesterase. Pinoresinol 4-O-β-D-glucopyranoside exhibits various activities such as antioxidant, anti-inflammatory, anti-hyperglycemic, hepatoprotective and anti-epileptic effects.
    Pinoresinol 4-O-β-D-glucopyranoside
  • 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-100326
    PDE7-IN-3
    Inhibitor 99.94%
    Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain.
    PDE7-IN-3
  • HY-70069
    GSK256066 Trifluoroacetate
    Inhibitor 99.54%
    GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.
    GSK256066 Trifluoroacetate
  • HY-B1209
    Etofylline
    Inhibitor 99.72%
    Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos.
    Etofylline
  • 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-162730
    OPB-171775
    Inhibitor 99.80%
    OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor.
    OPB-171775
  • HY-145583
    Mufemilast
    Inhibitor 99.67%
    Mufemilast is a phosphodiesterase 4 (PDE4) inhibitor.
    Mufemilast
  • HY-106003
    GSK356278
    Inhibitor 99.82%
    GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.
    GSK356278
  • HY-100933
    MY-5445
    Inhibitor 99.86%
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
    MY-5445
  • HY-126137
    PDE9-IN-1
    Inhibitor 99.70%
    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
    PDE9-IN-1
  • HY-U00186
    K134
    Inhibitor 99.84%
    K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively.
    K134
  • HY-W177546
    CD00509
    Inhibitor ≥98.0%
    CD00509 is a Tdp1 inhibitor, with an IC50 value of 0.71 μM. CD00509 can sensitize breast cancer cells to Camptothecin (HY-16560). CD00509 has anti-tumor activity.
    CD00509
  • HY-119611A
    Thioquinapiperifil dihydrochloride
    Inhibitor 99.22%
    Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.
    Thioquinapiperifil dihydrochloride
  • 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
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