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PDE

A phosphodiesterase (PDE) is an enzyme that breaks a phosphodiester bond. Usually, phosphodiesterase refers 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 (which all break the phosphodiester backbone of DNA or RNA), 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 of signal transduction mediated by these second messenger molecules.

Bucladesine sodium
T141816980-89-5
Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.
  • $31
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TargetMol | Inhibitor Hot
IBMX
T171328822-58-4
IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5 26.3 31.7 μM). IBMX enhances the intracellular cAMP level.
  • $33
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TargetMol | Inhibitor Hot
TPN171
T131931229018-87-4In house
TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.
  • $133
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TargetMol | Inhibitor Hot
MR-L2
T121032374703-19-0
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).
  • $148
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Luteolin
T1027491-70-3
Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.
  • $39
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Mirodenafil
T16079862189-95-5
Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.
  • $30
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BI 1015550
T720311423719-30-5
Nerandomilast (BI 1015550) is an orally active PDE4B inhibitor with IC50 of 7.2 nM. BI 1015550 has potential applications in inflammation, allergic diseases, pulmonary fibrosis and chronic obstructive pulmonary disease (COPD) with a good safety profile.
  • $59
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Mirodenafil dihydrochloride
TQ0126862189-96-6
Mirodenafil dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.
  • $30
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Ensifentrine
T253761884461-72-6
Ensifentrine (Ensifentrinum) is a PDE3 4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.
  • $30
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Gisadenafil
T15381334826-98-1In house
Gisadenafil (UK-369003), a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM, prevents the degradation of cGMP.
  • $195
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Difamilast
T27172937782-05-3
Difamilast is an inhibitor of phosphodiesterase IV.
  • $63
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Mopidamol
T2582913665-88-8In house
Mopidamol (RA 233) is a phosphodiesterase inhibitor, a dipyridamole derivative, with anticancer activity that prevents retinal vascular defects in experimental diabetes.
  • $380
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MK-8189
T734621424371-93-6
MK-8189 is a potent and selective pyrimidine PDE10A inhibitor, Ki = 0.029nM, with excellent PDE (phosphodiesterase) selectivity for the treatment of schizophrenia.
  • $123
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Roflumilast
T1024162401-32-3
Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.
  • $50
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pf-04822163
T283671798334-07-2In house
PF-04822163 is a potent inhibitor of PDE1 with IC50 value of 0.0024 μM.
  • $350
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CM-675
T108411872466-47-1In house
CM-675 is a dual inhibitor of phosphodiesterase 5 (PDE5) and class I histone deacetylases (IC50s: 114 nM and 673 nM for PDE5 and HDAC1) with the potential to treat Alzheimer's disease.
  • $58
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Tanimilast
T386251239278-59-1In house
Tanimilast (CHF-6001) is a novel, potent, and selective phosphodiesterase 4 inhibitor with an IC50 value of 0.026 ± 0.006 nM. It exhibits potent anti-inflammatory activity and is indicated for topical use in the lungs. Tanimilast was studied for its effects on obstructive lung disease.
  • $233
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Levosimendan
T2530141505-33-1
Levosimendan (OR1259) is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner.
  • $31
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Isoprenaline hydrochloride
T105651-30-9
Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
  • $33
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Roflumilast N-oxide
T4462292135-78-5
Roflumilast N-oxide is an inhibitor of PDE type 4.
  • $30
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Fulvic Acid
T38108479-66-3
Fulvic Acid is a natural product of humus produced by microorganisms in soil, sediment or aquatic environments. Fulvic acid is a phenolic acid and fungal metabolite isolated from Penicillium for the first time. Fulvic Acid inhibits the dimerization of amyloid b (17-42) (AB17-42), destroys the pre-formed trimer of AB17-42, and binds to the catalytic site of phosphodiesterase 5A (PDE5A), which can regulate the body's immune system, affect the oxidation state of cells, and improve gastrointestinal function. Fulvic Acid can be used as an oxidant or reducing agent and has the potential to study chronic inflammatory diseases such as diabetes.
  • $88
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Icariin
T2855489-32-7
Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432 73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.
  • $33
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ITI-214
T116891642303-38-5
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
  • $68
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Butein
T6427487-52-5
Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.
  • $36
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