PDE

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  1. PDE Inhibitor

    Theophylline L-lysine is a soluble derivative of Theophylline that primarily acts as a phosphodiesterase (PDE) inhibitor. It effectively inhibits PDE3 activity, which leads to relaxation of airway smooth muscle and exhibits anti-inflammatory properties through the enhancement of IL-10 levels and the inhibition of NF-κB nuclear translocation. Additionally, Theophylline L-lysine induces apoptosis, making it a valuable compound for research applications in asthma and chronic obstructive pulmonary disease (COPD).
  2. PDE4 PROTAC Degrader

    PROTAC PDE4 degrader-1 is a selective and orally active degrader targeting phosphodiesterase 4 (PDE4). It exhibits a DC50 of 41.98 μM and effectively inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. This compound demonstrates significant potential in alleviating pulmonary inflammation in LPS-induced acute lung injury models, making it a valuable tool for studying inflammatory diseases and therapeutic interventions.
  3. PDE4 Inhibitor

    AN-2898 is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 0.027 μM, demonstrating significant potency over other phosphodiesterase enzymes, including PDE1A, PDE2A, and PDE3A. It effectively inhibits PDE4 subtypes such as PDE4B1, PDE4A1A, and PDE4D2. AN-2898 significantly reduces the production of pro-inflammatory cytokines including TNF-α, IL-2, IFN-γ, IL-5, and IL-10, making it a valuable reagent for research applications in mild to moderate atopic dermatitis and psoriasis.
  4. PDE4 Inhibitor

    LY2775240 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor, demonstrating significant inhibitory activity against PDE4A, PDE4B, and PDE4D with IC₅₀ values of 0.09 nM and 0.14 nM for the latter two, as well as an IC₅₀ of 2.4 nM for PDE4C. This compound effectively reduces TNFα production during immune activation, making it valuable for studies investigating inflammatory conditions. LY2775240 is particularly relevant for research focused on psoriasis, as evidenced by its efficacy in lowering TNFα levels in rodent and cynomolgus monkey models.
  5. PDE4 Inhibitor

    ASP9831 is an orally active phosphodiesterase type 4 (PDE4) inhibitor. It effectively inhibits lipopolysaccharide (LPS)-induced tumor necrosis factor-alpha (TNF-α) production, demonstrating notable anti-inflammatory properties. This compound is valuable for research applications centered on fatty liver disease and related inflammatory conditions.
  6. PDE4 Inhibitor

    Revamilast is an orally active phosphodiesterase-4 (PDE4) inhibitor with a reported IC50 of 3 nM. This compound effectively inhibits the production of tumor necrosis factor-alpha (TNF-α), making it a valuable tool for research into inflammatory conditions. Applications include studies related to rheumatoid arthritis, plaque psoriasis, asthma, and other related inflammatory diseases.
  7. PDE4 Inhibitor

    PDE4-IN-15 is a selective inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 0.17 μM. This compound demonstrates notable anti-TNF-α activity, exhibiting an EC50 of 0.19 μM, which is significant for inflammatory research. Additionally, PDE4-IN-15 shows good skin permeability, making it suitable for studies involving topical administration and localized therapeutic applications.
  8. PDE Inhibitor

    Theophylline sodium glycinate is a potent phosphodiesterase (PDE) inhibitor with significant effects on airway smooth muscle relaxation. It acts primarily by inhibiting PDE3, which contributes to its anti-inflammatory properties through the upregulation of IL-10 and the inhibition of NF-κB translocation into the nucleus. Additionally, Theophylline sodium glycinate has been shown to induce apoptosis. This reagent is valuable for research applications related to asthma and chronic obstructive pulmonary disease (COPD).
  9. PDE-4 Inhibitor

    Apremilast-d5 is a deuterated analog of Apremilast, a potent inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. This compound effectively reduces TNF-α release in response to lipopolysaccharide (LPS) stimulation, exhibiting an IC50 of 104 nM. Apremilast-d5 is valuable for research applications related to inflammatory diseases and the modulation of immune responses.
  10. Phosphodiesterase (PDE) Inhibitor

    CDC801 is a potent inhibitor of phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α), with IC50 values of 1.1 μM and 2.5 μM, respectively. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into conditions associated with elevated TNF-α levels, such as autoimmune diseases and chronic inflammatory disorders. CDC801 is suitable for exploring the therapeutic potential of PDE4 inhibition and its effects on inflammatory pathways.
  11. PDE Inhibitor

    Theophylline monohydrate is a potent phosphodiesterase (PDE) inhibitor that primarily targets PDE3, promoting relaxation of airway smooth muscle. This compound exhibits anti-inflammatory properties by increasing interleukin-10 (IL-10) levels and inhibiting the nuclear translocation of NF-κB. Additionally, Theophylline monohydrate is known to induce apoptosis in certain cell types. It is widely utilized in research related to asthma and chronic obstructive pulmonary disease (COPD).
  12. HDAC/PDE5 Inhibitor

    CM-414 is a potent dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDACs), exhibiting IC50 values of 60 nM for PDE5 and ranging from 91 nM to 490 nM for various HDAC isoforms, including HDAC6 and HDAC1. This compound effectively reduces levels of amyloid-beta (Aβ) and phosphorylated tau (pTau) in Tg2576 mouse models, making it a valuable tool for Alzheimer's disease research. Its ability to penetrate the blood-brain barrier enhances its potential for studying neurodegenerative disorders and therapeutic interventions.
  13. HDAC/PDE5 Inhibitor

    CM-545 is a dual inhibitor targeting both histone deacetylases (HDACs) and phosphodiesterase 5 (PDE5). With pIC50 values of 7.47 for PDE5, 6.65 for HDAC1, 6.14 for HDAC2, 6.55 for HDAC3, and 6.84 for HDAC6, CM-545 demonstrates potent inhibitory activity. This compound has applications in cancer research and therapeutic interventions related to neurodegenerative diseases and cardiovascular conditions, owing to its modulation of histone acetylation and cyclic nucleotide signaling pathways.
  14. PDE IV Inhibitor/A1AR Antagonist

    Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm.
  15. PDE Inhibitor

    Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches.
  16. PDE5 Inhibitor

    Vardenafil hydrochloride trihydrate is a selective and orally active phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 of 0.7 nM. It also demonstrates inhibitory effects on PDE1 and PDE6 with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4 (IC50s >1000 nM). By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil hydrochloride trihydrate elevates cGMP levels. This compound is primarily utilized in research related to erectile dysfunction as well as conditions such as hepatitis and diabetes.
  17. PDE3/PDE4/PDE5/HRH1 Inhibitor

    Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses.
  18. PDE Inhibitor

    Pentoxifylline is a non-selective phosphodiesterase (PDE) inhibitor with significant haemorheological properties. It exhibits immune modulation, anti-inflammatory, anti-fibrinolytic, and anti-proliferative activities, making it a valuable tool in biomedical research. Pentoxifylline is particularly applicable in studies of peripheral vascular disease, cerebrovascular disease, and other conditions associated with impaired regional microcirculation.
  19. PDE5 Inhibitor

    Vardenafil hydrochloride is a selective phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 of 0.7 nM. This compound demonstrates moderate inhibition of PDE1 and PDE6, with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4. By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil hydrochloride effectively elevates cGMP levels. It serves as a valuable tool in research related to erectile dysfunction, hepatitis, and diabetes.
  20. PDEIII Inhibitor

    Anagrelide hydrochloride is a selective phosphodiesterase type III (PDE3) inhibitor with an IC50 value of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and suppresses megakaryocyte development in the bone marrow. Additionally, Anagrelide hydrochloride has been shown to reduce the proliferation of gastrointestinal stromal tumor (GIST) cells and induce apoptosis in vitro, highlighting its potential as an antineoplastic agent. Its primary application lies in its role as a platelet-lowering agent with antithrombopoietic properties.
  21. PDE 3/4 inhibitor

    Zardaverine is a phosphodiesterase inhibitor, selective for PDE3 and 4 (IC50 values are 0.5 and 0.8 uM respectively).
  22. platelet PDE inhibitor

    Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
  23. PDE5 inhibitor

    Avanafil is a PDE5 Inhibitor for the Treatment of Erectile Dysfunction
  24. PDE-4-D inhibitor

    CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
  25. PDE4 inhibitor?€?

    AN2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines
  26. PDE inhibitor

    Forskolin is a cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties.
  27. PDE9A inhibitor

    BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM.
  28. PDE2A inhibitor

    PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.
  29. PDE9 inhibitor

    PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor that increased indicators of hippocampal synaptic plasticity and improved cognitive function in a variety of cognition models in both rats and mice.
  30. PDE5 inhibitor

    Udenafil is a PDE5 inhibitor used in urology to treat erectile dysfunction.
  31. PDE3 inhibitor

    Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
  32. PDE4 inhibitor

    MK-0359 is a selective and potent oral PDE4 inhibitor, in chronic asthma.
  33. PDE3 inhibitor

    Cilostamide is a selective inhibitor of phosphodiesterase (PDE)3A and PDE3B with IC50 values of 27 and 50 nM, respectively.
  34. PDE9A Inhibitor

    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
  35. PDE-KRAS inhibitor

    Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
  36. PDE7 inhibitor

    BRL-50481 acts as a phosphodiesterase inhibitor selective for the PDE7 subtype.
  37. PDE9 inhibitor

    BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor.
  38. PDE4 inhibitor

    BW-A78U is a PDE4 inhibitor with an IC50 of 3 μM.
  39. PDE4B inhibitor

    Ademetionine, also known as AdoMet; MSI-195; SAMe, S-adenosylmethionine, is a PDE4B inhibitor potentially for treatment of primary biliary cirrhosis and major depressive disorder.
  40. PDE5 inhibitor

    Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
  41. PDE-5 inhibitor

    Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
  42. PDE3 inhibitor

    Fosphenytoin Sodium is the sodium salt form of fosphenytoin, a prodrug that is hydrolyzed to the anticonvulsant phenytoin. It is an PDE3 (phosphodiesterase 3) inhibitor.
  43. PDE5 inhibitor

    TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6.
  44. PDE5 inhibitor

    PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.
  45. autotaxin inhibitor

    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.
  46. PDE inhibitor

    Tibenelast sodium is a phosphodiesterase inhibitor.
  47. PDE4 inhibitor

    ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
  48. Ca2+ sensitiser

    Senazodan is a Ca2+ sensitiser, and also shows inhibition effect on PDE III.
  49. PDE inhibitor

    Win 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.
  50. PDE2A inhibitor

    PF-05085727 is a potent, selective and brain penetrant Phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 2 nM.

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