Metabolism

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  1. PDE Inhibitor

    Deltasonamide 2 hydrochloride is a potent inhibitor of phosphodiesterase delta (PDEδ), demonstrating competitive binding with a dissociation constant (Kd) of approximately 385 pM. This compound exhibits significant biological activity in modulating intracellular cyclic nucleotide levels, making it a valuable tool for research in signaling pathways related to cancer, cardiovascular diseases, and metabolic disorders. Its ability to selectively target PDEδ allows for potential applications in studies aimed at understanding the roles of cyclic nucleotides in various physiological processes.
  2. PDE9 Inhibitor

    Irsenontrine is a selective inhibitor of phosphodiesterase 9 (PDE9) with oral bioavailability. It has demonstrated potential in modulating intracellular signaling pathways, making it relevant for exploring therapeutic strategies for neurological diseases. This compound is valuable for research aimed at understanding the role of PDE9 in cognitive function and various neurodegenerative conditions.
  3. PDE9A Inhibitor

    BAY-7081 is a potent and selective inhibitor of phosphodiesterase 9A (PDE9A), demonstrating an IC50 value of 15 nM. This cyanopyridone-based compound exhibits robust oral bioavailability and solubility, making it a valuable tool for investigating the role of PDE9A in various biological processes. Its application in research includes studies on neurodegenerative diseases and cognitive function, where modulation of the cyclic GMP signaling pathway may be beneficial.
  4. Phosphodiesterase (PDE) Inhibitor

    Gisadenafil besylate is a selective phosphodiesterase 5 (PDE5) inhibitor that effectively prevents the degradation of cyclic guanosine monophosphate (cGMP), exhibiting an IC50 of 3.6 nM. This compound is primarily utilized in research related to cardiovascular health and sexual dysfunction, providing insights into the mechanisms regulating vascular smooth muscle relaxation and nitric oxide signaling pathways. Its specificity and oral bioavailability make it a valuable tool for investigating PDE5-related biological processes and therapeutic potential.
  5. PDE 10 Inhibitor

    PDE10-IN-5 is a potent inhibitor of phosphodiesterase 10 (PDE 10), targeting the regulation of intracellular signaling pathways by modulating cyclic nucleotide levels. This compound demonstrates significant biological activity in the central nervous system and is valuable for research on various CNS disorders, including schizophrenia and movement-related diseases. Its specificity for PDE 10 makes it an important tool for elucidating the role of this enzyme in neurodegenerative conditions and potential therapeutic interventions.
  6. PDE Inhibitor

    PF-8380 hydrochloride is a potent phosphodiesterase (PDE) inhibitor, demonstrating an IC50 of 2.8 nM in isolated enzyme assays and 101 nM in human whole blood. This compound is primarily used in research to investigate the role of autotaxin in various biological processes, including inflammation and cancer progression. PF-8380 hydrochloride serves as an important tool for studying the modulation of lysolipid signaling pathways and potential therapeutic interventions targeting autotaxin-related diseases.
  7. PDE4 Inhibitor

    Dovramilast is an orally active phosphodiesterase 4 (PDE4) inhibitor that effectively reduces inflammatory responses. It enhances isoniazid-mediated bacillary clearance from the lungs, making it a valuable adjunct in tuberculosis (TB) research. This compound facilitates studies aimed at understanding and improving therapeutic strategies for TB.
  8. PDE5 Inhibitor

    ent-Tadalafil is the inactive cis-enantiomer of the potent phosphodiesterase type 5 (PDE5) inhibitor (6R,12aS), which exhibits an IC50 of 0.090 μM. While ent-Tadalafil does not demonstrate significant biological activity, its characterization is essential for understanding the structure-activity relationship of PDE5 inhibitors. This compound serves as a reference material in biochemical research and may aid in the evaluation of enantiomeric effects on PDE5 inhibition.
  9. PDE4 Inhibitor

    Tilivapram (AVE8112) is a potent phosphodiesterase 4 (PDE4) inhibitor that demonstrates procognitive effects and enhances processing and psychomotor speeds in vivo. Its oral administration may be associated with dose-related side effects such as nausea and dizziness. However, transdermal delivery offers a controlled elevation of plasma concentrations, minimizing gastrointestinal discomfort and dizziness. Tilivapram is particularly relevant for research into neuropsychiatric disorders and cognitive enhancement.
  10. PDE9 Inhibitor

    (S)-C33 is a highly selective inhibitor of phosphodiesterase-9 (PDE9) with an IC50 value of 11 nM. This compound is primarily utilized in research focused on central nervous system disorders and diabetes. Its significant inhibitory action on PDE9 makes it a valuable tool for investigating the therapeutic potential in these areas.
  11. PDE5 Inhibitor

    Yonkenafil is a potent phosphodiesterase 5 (PDE5) inhibitor that has demonstrated efficacy in reducing cerebral infarction, alleviating neurological deficits, and minimizing edema and neuronal damage in affected areas. Its ability to enhance cognitive function through modulation of neurogenesis indicates potential therapeutic applications in neurodegenerative disorders, including Alzheimer's disease. Researchers may utilize Yonkenafil to investigate its effects on cognitive enhancement and neuroprotection in various experimental models.
  12. PDE6δ-KRas Inhibitor

    Deltasonamide 1 is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a dissociation constant (KD) of 203 pM. This compound effectively disrupts the function of the KRas signaling pathway, making it a valuable tool for investigating tumor biology and related therapeutic strategies. Deltasonamide 1 holds promise for advancing research in cancer treatment and understanding related pathophysiological mechanisms.
  13. Phosphodiesterase (PDE)

    PDE8B-IN-1 is a selective inhibitor of phosphodiesterase 8B (PDE8B), functioning to enhance insulin secretion. This compound demonstrates notable efficacy in high-throughput screening and has been optimized for ligand efficiency. With high target selectivity and favorable bioavailability observed in preclinical studies, PDE8B-IN-1 holds promise for further investigation into its inhibitory potential in metabolic research.
  14. PDE4D Inhibitor

    PDE4-IN-24 is a highly potent inhibitor of phosphodiesterase 4D (PDE4D) with an IC50 value of 0.57 nM, demonstrating over 4100-fold selectivity against other phosphodiesterase families. This compound is relevant to research on inflammatory diseases, as it modulates cyclic nucleotide signaling pathways, which are critical for controlling inflammation and immune responses. Its specificity and activity make PDE4-IN-24 a valuable tool for studying the role of PDE4D in various biological contexts.
  15. PDE5 Inhibitor

    MBCQ is a selective phosphodiesterase type 5 (PDE5) inhibitor with a potent IC50 of 19 nM. It demonstrates high specificity for cGMP-specific PDE5, exhibiting minimal activity against other phosphodiesterase isozymes (IC50s > 100 μM). MBCQ facilitates the dilation of coronary arteries, making it a valuable reagent for research focused on vascular biology and cardiovascular therapeutics.
  16. Phosphodiesterase (PDE) Inhibitor

    Prinoxodan is a selective phosphodiesterase (PDE) inhibitor that modulates intracellular cAMP levels. This compound has been shown to enhance biological activity in various cellular models, making it a valuable tool for studying signaling pathways involved in cardiovascular and neurological conditions. Prinoxodan is utilized in research applications focused on the regulation of smooth muscle relaxation and the modulation of neurotransmitter release.
  17. PDE5 Inhibitor

    (6S,12aR)-Tadalafil is a potent phosphodiesterase type 5 (PDE5) inhibitor, exhibiting an IC50 value of 5 nM. This compound is known to lower blood pressure and is utilized in research investigating cardiovascular effects, erectile dysfunction therapies, and other related conditions. Its strong inhibitory action on PDE5 makes it a valuable tool for studying nitric oxide signaling pathways and cGMP levels in various biological systems.
  18. Phosphodiesterase (PDE)

    2',3'-Cyclic NADP disodium serves as a substrate for phosphodiesterase (PDE), particularly 2',3'-cyclic nucleotide 3'-phosphodiesterase (CNP), which is predominantly found in myelin. This compound has been utilized in coupled enzyme assays for the precise quantification of CNP activity. Additionally, 2',3'-Cyclic NADP disodium (at a concentration of 5 μM) has demonstrated the ability to enhance calcium overload-induced calcium release and mitigate calcium-induced swelling in rat brain mitochondria, making it a valuable tool in neurobiological research.
  19. PDE5 Inhibitor

    Carbodenafil is a phosphodiesterase type 5 (PDE5) inhibitor, structurally related to Sildenafil (UK-92480). It effectively inhibits PDE5 with an IC50 of 5.22 nM, leading to increased levels of cyclic GMP and subsequent vasodilation. This compound is primarily utilized in research settings to explore mechanisms associated with erectile dysfunction and pulmonary hypertension.
  20. PDE Inhibitor

    Acetildenafil is a phosphodiesterase type 5 (PDE5) inhibitor that serves as an analogue of Sildenafil. It is primarily used in research to investigate its biological activities related to vasodilation and erectile function. Additionally, Acetildenafil is of interest in studies focusing on its potential therapeutic applications derived from herbal sources.
  21. PDE5 Inhibitor

    Thioquinapiperifil dihydrochloride is a potent and selective non-competitive inhibitor of phosphodiesterase-5 (PDE-5), with an IC50 of 0.074 nM. This compound is primarily utilized in research related to sexual enhancement and erectile function, contributing to studies on the modulation of signaling pathways associated with vasodilation. Its high selectivity and activity make it a valuable reagent for investigating PDE-5's role in various physiological and pathological processes.
  22. PDE2 Inhibitor

    Hcyb1 is a highly selective inhibitor of phosphodiesterase 2 (PDE2), demonstrating an IC50 of 0.57 μM against PDE2A and over 250-fold selectivity towards other members of the phosphodiesterase family. This compound is characterized by its neuroprotective and antidepressant-like effects, which are likely mediated through the cAMP/cGMP-CREB-BDNF signaling pathway. Hcyb1 is a valuable tool for research applications focusing on neurobiology and mood disorders.
  23. PDE3 Inhibitor

    Siguazodan is a selective phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. It effectively increases cyclic adenosine monophosphate (cAMP) levels in intact platelets, demonstrating an EC50 of 18.88 μM. Additionally, Siguazodan inhibits phenylephrine-induced serotonin (5-HT) release with an IC50 of 4.2 μM, making it a valuable tool for research into cardiovascular and platelet function.
  24. PDE4B Inhibitor

    PDE4B-IN-3 is a potent inhibitor of phosphodiesterase 4B (PDE4B), exhibiting an IC50 of 0.94 μM. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for studies aimed at understanding inflammatory pathways and developing novel therapeutic strategies. It is suitable for use in research applications investigating the role of PDE4B in various diseases, including chronic inflammatory conditions.
  25. PDE Inhibitor

    1-Phenyl-3,4-dihydroisoquinoline is a phosphodiesterase (PDE) inhibitor that demonstrates significant activity in modulating cyclic nucleotide levels. This compound has been investigated for its potential applications in various therapeutic areas, including cardiovascular and neurological research. Its ability to inhibit PDE may provide insights into cellular signaling pathways and support the development of novel pharmacological strategies.
  26. K-Ras-PDEδ Inhibitor

    K-Ras-PDEδ-IN-1 is a selective inhibitor of K-Ras-PDEδ, designed for high-affinity binding to the farnesyl binding pocket of PDEδ with a dissociation constant (Kd) of 8 nM. This compound effectively disrupts the interaction between K-Ras and PDEδ, playing a crucial role in modulating K-Ras signaling pathways. It is valuable for research applications focused on cancer biology and therapeutic strategies targeting K-Ras-driven malignancies.
  27. PDE4 Inhibitor

    LEO 39652 is a potent dual-selective inhibitor of phosphodiesterase type 4 (PDE4), exhibiting IC50 values of 1.2 nM for PDE4A and PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM. This compound is primarily utilized in topical research for atopic dermatitis (AD), making it valuable for studies aimed at understanding and developing treatments for this condition.
  28. PDE4 Inhibitor

    Lirimilast is a selective and orally active phosphodiesterase-4 (PDE4) inhibitor, exhibiting an IC50 of 49 nM. This compound demonstrates significant anti-inflammatory activity, making it a valuable candidate for therapeutic applications in asthma and chronic obstructive pulmonary disease (COPD). Research utilizing Lirimilast may provide insights into the modulation of inflammatory responses in respiratory conditions.
  29. PDE2A Inhibitor

    PDE2A-IN-3 is a selective inhibitor of phosphodiesterase 2A (PDE2A), exhibiting an IC50 of 69 nM for PDE2A and 1762 nM for PDE10. This compound is valuable for investigating the role of PDE2A in neurological and psychiatric disorders, providing insights into potential therapeutic interventions. Its specificity for PDE2A makes it an essential tool for researchers studying the modulation of cyclic nucleotide signaling pathways associated with these conditions.
  30. Phosphodiesterase (PDE) Inhibitor

    Theodrenaline hydrochloride is a selective phosphodiesterase (PDE) inhibitor that enhances cardiac contractility and improves hemodynamic performance. It exhibits potent cardiac stimulant properties and serves as an effective anti-hypotensive agent, particularly when used in conjunction with Cafedrine. This reagent is valuable for research applications focused on cardiovascular pharmacology and the mechanisms of blood pressure regulation.
  31. PDE4 Inhibitor

    FCPR03 is a highly selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating IC50 values of 60 nM, 31 nM, and 47 nM against the PDE4 catalytic domain, PDE4B1, and PDE4D7, respectively. With over 2100-fold selectivity against other phosphodiesterases (PDE1-3 and PDE5-11), FCPR03 exhibits significant anti-inflammatory, neuroprotective, and antidepressant-like properties. This compound is pivotal for research applications targeting inflammatory and neurodegenerative diseases, as well as mood disorders.
  32. Phosphodiesterase (PDE) Inhibitor

    Theodrenaline is a phosphodiesterase (PDE) inhibitor that functions primarily as a cardiac stimulant. It enhances cardiac contractility and supports blood pressure regulation, making it valuable in the treatment of hypotension. This compound is utilized in cardiovascular research to investigate heart function and the modulation of vascular tone.
  33. PDE 4 Inhibitor

    RS-25344 hydrochloride is a highly selective inhibitor of phosphodiesterase 4 (PDE 4), exhibiting an IC50 of 0.28 nM in human lymphocytes. The compound demonstrates minimal activity against PDE I, II, and III, with IC50 values exceeding 100 μM. RS-25344 hydrochloride possesses significant anti-inflammatory properties and has been shown to enhance memory and cognitive functions, as well as exhibiting potential antineoplastic effects. This makes it a valuable tool for research in areas related to inflammation, neurobiology, and cancer.
  34. PDE4 Inhibitor

    Atizoram is a selective phosphodiesterase 4 (PDE4) inhibitor that elevates cyclic AMP levels while simultaneously reducing tumor necrosis factor-alpha (TNFα) production in murine models. This compound possesses significant anti-inflammatory properties, making it a valuable tool for investigating inflammatory pathways and potential therapeutic strategies in conditions associated with dysregulated TNFα expression. Atizoram is applicable in research exploring the roles of PDE4 in various biological systems and diseases.
  35. PDE3 Inhibitor

    Motapizone is a selective phosphodiesterase 3 (PDE3) inhibitor. It has been shown to moderately inhibit cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages, highlighting its potential anti-inflammatory properties. Additionally, Motapizone enhances intracellular cyclic AMP levels, thereby preventing human platelet aggregation. This compound is valuable for research in inflammation and platelet physiology.
  36. PDE4 Inhibitor

    PDE4-IN-4 is a selective inhibitor of phosphodiesterase 4 (PDE4) with a pIC50 of 8.8, as well as a dual antagonist of the M3 muscarinic receptor with a pIC50 of 10.2. This compound exhibits significant biological activity in modulating cyclic nucleotide levels, making it valuable for research related to pulmonary diseases. Its dual action allows for exploration of therapeutic pathways in respiratory disorders, providing insights into potential treatment strategies.
  37. PDE3 Inhibitor

    Quazinone is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3), targeting the catalytic activity of this enzyme. It effectively inhibits the phosphorylation of p42/p44 MAP kinase, leading to decreased mitogenic signaling. Quazinone exhibits antimitogenic effects and is useful in studies related to cell proliferation and signal transduction pathways.
  38. PDE4 Inhibitor

    MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor that enhances intracellular cyclic adenosine monophosphate (cAMP) levels by blocking PDE4 activity. This elevation in cAMP activates protein kinase A (PKA), which subsequently inhibits inflammatory cell activity and promotes relaxation of airway smooth muscle. MK-0873 is suitable for research applications related to chronic obstructive pulmonary disease (COPD), providing insights into potential therapeutic strategies for respiratory conditions characterized by inflammation and airway constriction.
  39. PDE10A Inhibitor

    PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A), displaying an IC50 of 4.6 nM and an ED50 of 13 mg/kg. This compound influences patterns of brain glucose metabolism, potentially serving as a translational biomarker in neurological research. PQ-10 is particularly valuable for investigating psychiatric disorders, including schizophrenia, and provides insights into the underlying mechanisms of these conditions.
  40. PDE4 Inhibitor

    MK-0952 is a selective phosphodiesterase 4 (PDE4) inhibitor, characterized by an IC50 value of 0.53 nM. This compound exhibits potential therapeutic effects for disorders associated with PDE4 modulation, particularly in the context of Alzheimer's disease research. MK-0952 provides a valuable tool for studying the role of PDE4 in cognitive function and neurodegenerative diseases.
  41. PDE4 Inhibitor

    (S)-Gebr32a is a selective phosphodiesterase 4 (PDE4) inhibitor, demonstrating IC50 values of 19.5 µM for PDE4 cat and 2.1 µM for PDE4D3. It exhibits significant biological activity by modulating intracellular cyclic AMP levels, making it a valuable tool for investigating inflammatory processes and neurodegenerative diseases. This compound is suitable for research applications focused on the role of PDE4 in various cellular signaling pathways.
  42. PDE5 Inhibitor

    Yonkenafil hydrochloride is a selective phosphodiesterase 5 (PDE5) inhibitor, known for its neuroprotective properties. It effectively reduces cerebral infarction, neurological deficits, edema, and neuronal damage following ischemic events. Additionally, Yonkenafil may enhance cognitive function through modulation of neurogenesis, suggesting its potential therapeutic applications in neurodegenerative conditions such as Alzheimer's disease.
  43. PDE4 Antagonist

    Eggmanone is a selective antagonist of phosphodiesterase 4 (PDE4), with an IC50 of 72 nM for the PDE4D3 isoform. This compound exhibits a remarkable 40- to 50-fold selectivity for PDE4D3 over other phosphodiesterases. By inhibiting PDE4, Eggmanone activates protein kinase A, resulting in the blockade of Hedgehog (Hh) signaling pathways. This biological activity makes Eggmanone a valuable tool for research into cellular signaling and potential therapeutic applications in conditions mediated by Hh pathways.
  44. Phosphodiesterase (PDE)

    PDE7-IN-4 is a selective inhibitor of phosphodiesterase 7 (PDE7), which enhances intracellular levels of cyclic adenosine monophosphate (cAMP). This compound demonstrates significant potential in modulating neurotransmission and exhibits anti-inflammatory effects through the cAMP/cAMP response element binding protein (CREB) signaling pathway. PDE7-IN-4 is a valuable tool for researchers investigating neurodegenerative diseases and inflammation-related conditions, offering insights into therapeutic mechanisms and potential interventions.
  45. Phosphodiesterase (PDE) Inhibitor

    PDE10-IN-1 is a selective inhibitor of phosphodiesterase 10 (PDE10), which plays a crucial role in regulating cyclic nucleotide levels in the central nervous system. This compound has demonstrated potential in modulating dopaminergic signaling and offers promise for investigating therapeutic strategies for central nervous system and metabolic disorders. Its mechanism of action may provide insights into the treatment of various neuropsychiatric conditions.
  46. PDE5 Inhibitor

    T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor that disrupts the hydrolysis of cyclic guanosine monophosphate (cGMP) in a competitive manner, with an IC50 value of 0.23 nM. This compound also demonstrates inhibitory effects on PDE6 (IC50=56 nM) while displaying low potency against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 is valuable for research focusing on the nitric oxide (NO)/cGMP signaling pathway, with potential applications in cardiovascular and erectile dysfunction studies.
  47. PDE III Inhibition

    Senazodan hydrochloride is a selective inhibitor of phosphodiesterase III (PDE III), functioning primarily as a calcium sensitizer. This compound enhances cardiac contractility and has potential applications in researching heart failure and other cardiovascular disorders. Its ability to modulate cAMP levels makes it a valuable tool for investigating the signaling pathways involved in cardiac function and disease.
  48. PDE4 Inhibitor

    Denbufylline is a potent phosphodiesterase-4 (PDE4) inhibitor that effectively prevents the degradation of intracellular cyclic adenosine monophosphate (cAMP). This inhibition leads to increased levels of cAMP, which plays a crucial role in regulating various cellular functions. Denbufylline is primarily utilized in research related to chronic obstructive pulmonary disease (COPD), asthma, and other inflammatory conditions, making it a valuable tool for understanding these complex diseases.
  49. PDE4B Modulator

    PDE4B modulator-1 is a selective modulator of phosphodiesterase 4B (PDE4B), targeting intracellular signaling pathways. It exhibits significant inhibition of PDE4B activity, leading to increased cAMP levels and subsequent regulation of various cellular processes. This compound is valuable for research in neurobiology, inflammation, and respiratory diseases, providing insights into PDE4B's role in mediating inflammatory responses and neuronal signaling.
  50. Phosphodiesterase (PDE)

    (E/Z)-N-Desethylsunitinib hydrochloride is a potent inhibitor of phosphodiesterase (PDE), functioning as a competitive inhibitor of ATP. This compound exhibits significant anti-tumor activity by targeting and inhibiting VEGF-R2 and PDGF-Rβ tyrosine kinases. Its role as the principal active metabolite of sunitinib makes it valuable for research applications focused on tumor angiogenesis and proliferation.

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