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-123446
    JNJ-42259152
    JNJ-42259152 is a phosphodiesterase 10A (PDE10A) positron emission tomography (PET) tracer that is specific for PDE10A activity. JNJ-42259152 can be dynamically scanned in healthy volunteers to assess its kinetic properties in the brain. The half-life of JNJ-42259152 in the blood is an average of 90 minutes. JNJ-42259152 has demonstrated reliable binding potential (BPND) in different target areas (such as the lentiform nucleus, caudate nucleus, ventral striatum, etc.), providing an important tool for studying neuropsychiatric diseases.
    JNJ-42259152
  • HY-160991
    Menabitan
    		Inhibitor
    Menabitan (SP-204) is an inhibitor for phosphodiesterase 9 (PDE 9), which acts as a non-opioid analgesic agent. Menabitan lowers the intraocular pressure in rabbit model.
    Menabitan
  • HY-B0442BR
    Vardenafil hydrochloride trihydrate (Standard)
    		Inhibitor
    Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. 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-.
    Vardenafil hydrochloride trihydrate (Standard)
  • HY-169258
    PDE4-IN-21
    		Inhibitor
    PDE4-IN-21 (Compound L19) is a poetent PDE4 inhibitor, with an IC50 of 0.48 μM. PDE4-IN-21 exhibits good inhibitory activity and remarkable metabolic stability in rat liver microsomes.
    PDE4-IN-21
  • HY-163606
    PDE4B/D-IN-3
    		Inhibitor
    PDE4B/D-IN-3 (example 22) is a potent inhibitor of PDE4, with IC50s of 0.071 nM and 0.09 nM for PDE4B2 and PDE4D, respectively.
    PDE4B/D-IN-3
  • HY-111219
    Parogrelil hydrochloride
    		Inhibitor
    Parogrelil (hydrochloride) (NM-702) is a phosphodiesterase inhibitor with activity in inhibiting intermittent claudication. Parogrelil (hydrochloride) selectively inhibits PDE3, inhibits human platelet aggregation in vitro and rat aortic contraction, and improves walking distance and plantar surface temperature in the rat femoral artery ligation model, with better effects than cilostazol.
    Parogrelil hydrochloride
  • HY-18037
    AMG-7980
    AMG-7980 exhibits high affinity to phosphodiesterase 10A (PDE10A), with a KD of 0.94 nM. AMG-7980 can be used as a tracer of PDE10A, when labeled with radioactive isotope.
    AMG-7980
  • HY-18252R
    Avanafil (Standard)
    		Inhibitor
    Avanafil (Standard) is the analytical standard of Avanafil. This product is intended for research and analytical applications. Avanafil (TA-1790) 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 activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil (Standard)
  • HY-168212
    PDE4-IN-22
    		Inhibitor
    PDE4-IN-22 (Compound 2e) is a PDE4 inhibitor with an IC50 value of 2.4 nM. PDE4-IN-22 exhibits anti-inflammatory activity and demonstrates significant anti-psoriatic effects in an Imiquimod (HY-B0180)-induced psoriasis mouse model.
    PDE4-IN-22
  • HY-122641D
    Deltasonamide 1 TFA
    		Inhibitor 99.70%
    Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors.
    Deltasonamide 1 TFA
  • HY-143583
    ATX inhibitor 10
    		Inhibitor
    ATX inhibitor 10 is a potent inhibitor of ATX. ATX inhibitor 10 is s nitrogen-containing heterocyclic compound. ATX plays a role in causing pathological conditions including fibrosis, arthritis, neurodegeneration, neuropathic pain, and cancer. ATX inhibitor 10 has the potential for the research of ATX related diseases (extracted from patent WO2021115375A1, compound 35).
    ATX inhibitor 10
  • HY-169981
    PDE4-IN-24
    		Inhibitor
    PDE4-IN-24 (compoud 14h) is a potent inhibitor of PDE4D with the IC50 of 0.57 nM and >4100-fold selectivity over other PDE families. PDE4-IN-24 plays an important role in inflammatory disease.
    PDE4-IN-24
  • HY-10679
    PF-03049423 free base
    		Inhibitor
    PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke.
    PF-03049423 free base
  • HY-146205
    ATX inhibitor 18
    		Inhibitor
    ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis.
    ATX inhibitor 18
  • HY-145065
    Enpp-1-IN-7
    		Inhibitor
    Enpp-1-IN-7 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-7 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51).
    Enpp-1-IN-7
  • HY-151174
    PDE4-IN-12
    		Inhibitor
    PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs).
    PDE4-IN-12
  • HY-136520S
    Xanthoanthrafil-d3
    Xanthoanthrafil-d3 is the deuterium labeled Xanthoanthrafil (HY-136520B). Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, with an IC50 of 3.95 ng/mL. Xanthoanthrafil can be used for the research of erectile dysfunction.
    Xanthoanthrafil-d<sub>3</sub>
  • HY-123008
    Reproterol hydrochloride
    		Inhibitor
    Reproterol hydrochloride is a dual-acting beta2-adrenoceptor agonist and phosphodiesterase inhibitor. Reproterol hydrochloride is more potent than albuterol and feterol in stimulating cAMP production in human monocytes, demonstrating its potential in enhancing airway function. Furthermore, Reproterol significantly inhibited the production of LTB4, indicating its anti-inflammatory properties. Reproterol hydrochloride may have inhibitory effects in respiratory diseases such as asthma and COPD.
    Reproterol hydrochloride
  • HY-107203
    Propentofylline
    		Inhibitor 99.88%
    Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity. Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
    Propentofylline
  • HY-105686
    FR-229934
    		Inhibitor 98.65%
    FR-229934 is a PDE V inhibitor extracted from patent WO2019130052A1. FR-229934 can be used for the research of pulmonary arterial hypertension and erectile dysfunction.
    FR-229934
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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