Metabolism

Items 2601-2650 of 6037

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  1. PDE V Inhibitor

    FR-181074 is a selective and orally active phosphodiesterase V (PDE V) inhibitor. By specifically blocking PDE V, it prevents the degradation of cyclic guanosine monophosphate (cGMP), leading to the relaxation of smooth muscle. This compound is valuable for research in cardiovascular diseases and endocrinology, with applications in studying conditions such as hypertension and erectile dysfunction.
  2. PDE4B/PDE4D Inhibitor

    PDE4-IN-32 is a selective inhibitor of phosphodiesterase 4B (PDE4B) and phosphodiesterase 4D (PDE4D) with IC50 values of 13.7 nM and 23.8 nM, respectively. This compound effectively penetrates the blood-brain barrier and has demonstrated the ability to enhance recovery of motor and cognitive function in mouse models of middle cerebral artery occlusion (MCAO). Additionally, PDE4-IN-32 has been shown to reduce cerebral edema and is a valuable tool for research focused on ischemic stroke.
  3. PDE4 Inhibitor

    NVP-ABE171 is a potent, orally active inhibitor of phosphodiesterase 4 (PDE4) that exhibits selective IC50 values of 1.5 nM for PDE4D, 34 nM for PDE4B, 602 nM for PDE4A, and 1230 nM for PDE4C. This compound significantly increases cAMP levels in response to isoproterenol, while also inhibiting eosinophil oxidative bursts and inflammatory cytokine release from T cells and monocytes. NVP-ABE171 demonstrates strong anti-inflammatory effects in preclinical models of asthma and pulmonary inflammation, making it a valuable tool for studying asthma and chronic obstructive pulmonary disease.
  4. PDE4B Inhibitor

    PDE4B-IN-5 is a potent inhibitor of phosphodiesterase 4B (PDE4B), exhibiting an IC50 value of less than 10 nM. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for investigating inflammatory processes. PDE4B-IN-5 is suitable for research applications focused on the modulation of cyclic AMP signaling and its implications in various inflammatory diseases.
  5. PDE1 Inhibitor

    PDE1-IN-12 is a selective phosphodiesterase 1 (PDE1) inhibitor. It effectively inhibits PDE1-mediated suppression of the dopamine D1 receptor signaling pathway, which is crucial for regulating dopaminergic activity. This compound has potential applications in the study of narcolepsy and other neuropsychiatric disorders where dopamine signaling is disrupted.
  6. Phosphodiesterase (PDE) Inhibitor

    ATI22-107 is a dual-pharmacophore inhibitor targeting phosphodiesterase type III (PDE-III) and L-type calcium channels (LTCC). This compound enhances calcium cycling and contractility in cardiac tissues, particularly in cat ventricular myocytes and trabeculae. It is valuable for research focused on cardiac function, calcium signaling, and the pharmacological modulation of heart contractility.
  7. PDE5 Inhibitor

    12-epi-Tadalafil is a potent phosphodiesterase type 5 (PDE5) inhibitor, exhibiting an IC50 value of 0.09 μM. This compound plays a critical role in the modulation of cGMP levels, making it valuable for the study of cardiovascular diseases and related pathophysiological conditions. Its inhibitory effects on PDE5 offer insights into therapeutic approaches for conditions linked to endothelial dysfunction and vasodilatory responses.
  8. PDE10A Inhibitor

    THPP-2 is a selective phosphodiesterase 10A (PDE10A) inhibitor, exhibiting a Ki value of 94 nM. This compound is primarily utilized in the investigation of schizophrenia and offers insights into the mechanisms of this mental disorder. By modulating PDE10A activity, THPP-2 aids in the exploration of potential therapeutic strategies for schizophrenia-related pathophysiology.
  9. PDE1 Inhibitor

    PDE1-IN-7 is a selective inhibitor of bPDE1, demonstrating an IC50 of 10 nM. This compound exhibits notable anti-fibrotic activity, particularly in a bile duct ligation (BDL)-induced liver fibrosis rat model. PDE1-IN-7 is suitable for use in research focused on liver fibrosis and related disorders.
  10. PDE5 Inhibitor

    PDE5-IN-15 is a xanthine derivative functioning as a selective inhibitor of phosphodiesterase type 5 (PDE5). With IC50 values of 0.002 μM against human PDE5, 0.180 μM against bovine PDE6, and 2.85 μM against bovine PDE1, this compound demonstrates potent activity. PDE5-IN-15 exhibits promising oral bioavailability in canines, making it a valuable tool for research on male erectile dysfunction and related therapeutic applications.
  11. PDE Inhibitor

    PDE4-IN-3 is a potent phosphodiesterase 4 (PDE4) inhibitor, exhibiting an inhibitory affinity with an IC50 value of 4.2 nM. This compound effectively modulates intracellular cAMP levels, making it a valuable tool in research focused on inflammatory and neurological disorders. PDE4-IN-3 is primarily utilized to investigate the role of cAMP signaling pathways in various biological processes and potential therapeutic interventions.
  12. PDE5 Inhibitor

    KD-027 is a potent inhibitor of Phosphodiesterase 5 (PDE5), which plays a crucial role in regulating cyclic nucleotide levels in various tissues. This compound demonstrates significant potential in research focused on endothelial dysfunction and hypertension. Its mechanism of action aids in the therapeutic exploration of cardiovascular diseases and related conditions.
  13. PDE IV Inhibitor

    CDP-840 is a selective and orally active phosphodiesterase IV (PDE IV) inhibitor. This compound demonstrates significant inhibition of antigen-induced early and late-phase bronchoconstriction in conscious squirrel monkeys, indicating its potential use in respiratory research. CDP-840 may be useful for investigating therapeutic strategies for asthma and other allergic conditions through modulation of inflammatory pathways.
  14. PDE4 Inhibitor

    HT-0712 is a selective inhibitor of Phosphodiesterase Type 4 (PDE4). This compound has been shown to enhance motor recovery and facilitate cortical reorganization following focal cortical ischemia, making it a valuable tool in neuropharmacology research. Its ability to modulate cAMP levels may provide insights into therapeutic strategies for stroke rehabilitation and related neurological disorders.
  15. PDE Inhibitor

    Autotaxin-IN-5 is a potent inhibitor of autotaxin, primarily targeting phosphodiesterase (PDE) pathways. This compound demonstrates significant biological activity in modulating fibrosis-related processes, making it a valuable candidate for research in idiopathic pulmonary fibrosis. Its application in preclinical studies could provide insights into therapeutic approaches for lung fibrosis and related disorders.
  16. PDE4B1 Inhibitor

    Phosphodiesterase-IN-3 is a potent inhibitor of phosphodiesterase 4B1, exhibiting an IC50 of less than 10 nM, while demonstrating moderate inhibition of PDE4D3 with an IC50 in the range of 10-100 nM. This compound is valuable for research into idiopathic pulmonary fibrosis, providing a tool for investigating PDE4B1-mediated pathways and their therapeutic potential in pulmonary diseases.
  17. Phosphodiesterase (PDE) Control

    (-)-Pimobendan selectively targets phosphodiesterase (PDE), enhancing cyclic nucleotide signaling. This isomer exhibits a pronounced affinity for erythrocytes, leading to a significantly lower clearance rate compared to its counterpart. Notably, (-)-pimobendan demonstrates a 1.5-fold increase in contractile force in detergent-treated myocardial specimens from guinea pigs and dogs. These distinctive pharmacokinetic properties may provide unique advantages for its application in clinical settings, particularly in cardiac research and therapeutics.
  18. Phosphodiesterase (PDE)

    Mardepodect succinate is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A), demonstrating significant potential in the treatment of schizophrenia. This compound has been optimized to enhance its brain penetration and physicochemical properties, making it valuable for schizophrenia-related research applications. Its targeted mechanism may aid in the exploration of PDE10A's role in neuropsychiatric disorders.
  19. PDE-5 Inhibitor

    Acetylvardenafil is a potent phosphodiesterase type 5 (PDE-5) inhibitor, serving as an analog of Vardenafil with an acetyl group replacing the sulfonyl group. This compound exhibits significant biological activity by facilitating the relaxation of smooth muscle tissue and increasing blood flow to the corpus cavernosum, making it a valuable tool in the study of erectile dysfunction (ED). Its mechanism can contribute to research aimed at understanding and developing therapies for erectile dysfunction and related conditions.
  20. PDE4 Inhibitor

    PDE4-IN-5 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 3.1 nM. It demonstrates favorable skin permeability, making it particularly relevant for topical applications. This compound is primarily investigated for its potential anti-psoriasis effects and can be utilized in research focusing on inflammatory skin conditions and associated therapeutic strategies.
  21. PDE3/4 Inhibitor

    (E/Z)-Ensifentrine is a dual inhibitor of phosphodiesterase 3 and 4 (PDE3/4). It exhibits significant bronchodilatory and anti-inflammatory effects, demonstrated in both in vitro and in vivo models. This compound is primarily utilized in research related to respiratory diseases, particularly for studying inflammation and airway obstruction mechanisms.
  22. PDE10A Inhibitor

    JNJ-42396302 is a selective phosphodiesterase 10A (PDE10A) inhibitor that modulates intracellular signaling pathways involving cyclic nucleotides. This compound exhibits significant biological activity in the regulation of dopaminergic and glutamatergic systems, making it a valuable tool for investigating neurobiological processes. Research applications include studies focused on infertility and potential therapeutic interventions in neuropsychiatric disorders.
  23. Phosphodiesterase (PDE)

    PDE5-IN-6c is a selective inhibitor of phosphodiesterase 5A1 (PDE5A1) with significant potential for Alzheimer's disease (AD) research. With an impressive in vitro IC50 of 0.056 nM, it demonstrates strong inhibitory activity. Additionally, PDE5-IN-6c features enhanced water solubility, making it a promising candidate for further drug development and investigation in neurodegenerative disease studies.
  24. Phosphodiesterase (PDE) Inhibitor

    Palmitoylcholine chloride acts as an inhibitor of phosphodiesterase (PDE), particularly affecting the calcium-dependent hydrolysis of phosphatidylinositol. This compound helps to mitigate membrane stress by reducing enzyme activity, thereby influencing cellular signaling pathways. Palmitoylcholine chloride is valuable for research applications involving membrane dynamics and signal transduction.
  25. PDE3B Inhibitor

    GSK4394835A is a reversible covalent inhibitor of phosphodiesterase 3B (PDE3B), exhibiting a pIC50 value of 6.2. This compound demonstrates significant efficacy in modulating cellular signaling pathways associated with cardiovascular diseases. GSK4394835A is a valuable tool for researchers investigating the role of PDE3B in cardiovascular disease mechanisms and potential therapeutic interventions.
  26. AR/PDE Inhibitor

    ADORA2A/PDE4D-IN-1 is a dual inhibitor targeting the adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). This compound exhibits significant biological activity in modulating adenosine signaling and cyclic nucleotide levels. Its dual inhibitory mechanism makes it valuable for research applications focused on bronchial asthma and related respiratory conditions.
  27. PDE4 Inhibitor

    PDE4-IN-16 is a selective inhibitor of phosphodiesterase 4 (PDE4), displaying an IC50 value of 3.61 μM. This compound is relevant for research in inflammatory diseases and central nervous system (CNS) disorders characterized by elevated cytokine levels. Its ability to modulate inflammatory pathways makes it a valuable tool for exploring therapeutic strategies in related conditions.
  28. PDE4 Inhibitor

    KW-4490 is a selective inhibitor of phosphodiesterase 4 (PDE4), a key enzyme involved in the degradation of cyclic adenosine monophosphate (cAMP). This compound exhibits anti-inflammatory properties and is particularly relevant in studies of asthma and other inflammatory disorders. KW-4490 serves as a valuable tool for researchers investigating the modulation of immune responses and the potential therapeutic avenues in inflammatory diseases.
  29. PDE5 Inhibitor

    (R)-Avanafil is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 5.2 nM. This compound is utilized in research pertaining to erectile dysfunction, offering insights into its pharmacological effects and potential therapeutic applications. Its specificity for PDE5 makes it a valuable tool for studying the modulation of cyclic nucleotide signaling pathways.
  30. PDE9 Inhibitor

    (Rac)-Tovinontrine, also known as (Rac)-IMR-687, is a selective phosphodiesterase 9 (PDE9) inhibitor that enhances levels of cyclic guanosine monophosphate (cGMP). This compound is particularly relevant in the study of thalassemia, as it may play a role in modulating signaling pathways associated with erythropoiesis and vascular regulation. Its ability to influence cGMP levels makes it a valuable tool in various research applications related to cardiovascular diseases and hematological disorders.
  31. Phosphodiesterase (PDE) Inhibitor

    PDE10A-IN-4 is a selective phosphodiesterase 10A (PDE10A) inhibitor. It primarily modulates intracellular signaling pathways through the inhibition of cyclic nucleotide degradation, which may have implications in the study of neuropsychiatric disorders, particularly schizophrenia. This compound is utilized in research to explore its potential role in cognitive and motor functions associated with PDE10A inhibition.
  32. PDE5 Inhibitor

    PDE5-IN-42 is a potent and orally active phosphodiesterase type 5 (PDE5) inhibitor, demonstrating an IC50 of 0.04 nM. This compound exhibits selectivity over PDE6 and PDE11, making it a valuable tool in research focused on vascular smooth muscle relaxation and erectile dysfunction. Its effectiveness in modulating cGMP levels supports its potential applications in cardiovascular disease studies and related therapeutic explorations.
  33. PDE Inhibitor

    Bemoradan is a selective inhibitor of canine phosphodiesterase (PDE) fraction III, exhibiting potent inotropic and vasodilatory effects. Its long-acting nature makes it a valuable tool in research related to congestive heart failure. Bemoradan facilitates the investigation of cardiac function and therapeutic interventions for heart conditions.
  34. PDE10A Inhibitor

    PDM-042 is a selective inhibitor of phosphodiesterase 10A (PDE10A), demonstrating exceptional potency with IC50 values below 1 nM in both human and rat systems. It exhibits over 1000-fold selectivity against other phosphodiesterases, making it a valuable tool for investigating PDE10A's role in neurobiology. PDM-042 is particularly relevant for research into schizophrenia and related neurological disorders.
  35. PDE3 Inhibitor

    Org-9935 is a selective phosphodiesterase 3 (PDE3) inhibitor with an IC50 of 50 nM. This compound has been shown to inhibit the maturation of oocytes in naturally selected dominant follicles in rhesus macaques. Additionally, Org-9935 enhances glucose-induced insulin secretion in isolated rat islets, with an EC50 of 20 μM, making it a valuable tool for research in reproductive biology and insulin signaling pathways.
  36. PDE3/PDE4 Inhibitor

    PDE3/4-IN-2 is a potent dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), demonstrating IC50 values of 0.13 nM for PDE3A and 50 nM for PDE4B1. This compound is valuable in the investigation of diseases related to phosphodiesterase dysregulation, including asthma, chronic obstructive pulmonary disease, sepsis, and nephritis. Its selective inhibition profile makes it a significant tool for exploring therapeutic strategies in these conditions.
  37. PDE10A Inhibitor

    TC-E 5005 is a highly selective inhibitor of the phosphodiesterase 10A (PDE10A) enzyme, exhibiting IC50 values of 7.28 nM for PDE10A, while demonstrating significantly higher values for PDE2A, 11A, 5A, 7B, and 3A. This compound effectively inhibits adrenergic and neurogenic smooth muscle contractions in human prostate tissues, making it a valuable tool for studying PDE10A's role in smooth muscle physiology and potential therapeutic applications in urological disorders.
  38. Phosphodiesterase (PDE)

    PDE4-IN-20 is a selective phosphodiesterase-4 (PDE4) inhibitor that operates at submicromolar concentrations and exhibits anti-TNF-α activity. This compound demonstrates significant biological effects both in vitro and in vivo, making it a valuable tool for research on inflammatory diseases. Molecular modeling studies highlight its binding interactions with PDE4, and conformational analyses confirm its pharmacological profile aligns with established PDE4 inhibitors. PDE4-IN-20 is useful for studies aimed at elucidating the role of PDE4 in cellular processes and therapeutic interventions.
  39. CAMP PDEl Inhibitor

    CK-3197 is a selective inhibitor of cyclic 3',5'-adenosine monophosphate phosphodiesterase (cAMP PDE1), targeting enzyme activity to modulate intracellular signaling. This compound demonstrates hemodynamic and myocardial energetic effects in vivo, potentially offering therapeutic benefits in managing congestive heart failure. As an imidazolone derivative, CK-3197 serves as a positive inotropic agent, making it valuable for research related to cardiovascular function and heart disease studies.
  40. PDE Inhibitor

    Mopidamol is a phosphodiesterase inhibitor primarily used in cancer research. This compound has shown potential biological activity in the context of non-small cell lung cancer (N-SCLC), making it a relevant tool for exploring therapeutic strategies targeting this malignancy. Its mechanism of action involves modulation of cyclic nucleotide levels, contributing to the understanding of tumor biology and potential treatment pathways.
  41. PDE-4B Inhibitor

    PDE4B-IN-7 is a potent inhibitor of phosphodiesterase-4B (PDE-4B) with an IC50 value of 160 nM, demonstrating strong and stable binding at its active site. This compound effectively inhibits acetylcholine-induced bronchospasm in guinea pigs, making it a valuable tool for asthma research. Additionally, PDE4B-IN-7 exhibits antimicrobial activity against both susceptible Gram-positive and Gram-negative bacterial strains, supporting its application in studies related to respiratory diseases and bacterial infections.
  42. PDE6D Inhibitor

    Deltaflexin3 is a selective inhibitor of phosphodiesterase 6D (PDE6D), targeting the modulation of intracellular signaling pathways. This compound effectively diminishes Ras signaling and has demonstrated the ability to selectively inhibit the growth of KRAS mutant and PDE6D-dependent cancer cells. Deltaflexin3 is a valuable tool for researchers investigating the molecular mechanisms of cancer and the therapeutic potential of targeting PDE6D in oncogenic pathways.
  43. PDE Inhibitor

    JNJ-54082730 is a potent phosphodiesterase (PDE) inhibitor targeting PDE2A, PDE3B, and PDE10A2 with IC50 values of 0.95 nM, 6.17 μM, and 87.1 nM, respectively. It enhances AMPA receptor activity, modulating synaptic plasticity and improving learning and memory functions in rodent models. Furthermore, JNJ-54082730 exhibits the ability to cross the blood-brain barrier, making it a valuable tool for neuropharmacological research.
  44. Phosphodiesterase (PDE)

    Parogrelil is a potent phosphodiesterase (PDE) inhibitor, primarily targeting PDE3. It exhibits significant activity in reducing intermittent claudication by inhibiting platelet aggregation and vasoconstriction, leading to an improvement in walking distance and plantar surface temperature in experimental rat models. This compound is valuable for research in vascular biology and cardiology, particularly in studies related to peripheral artery disease and associated therapeutic interventions.
  45. PDE5 Inhibitor

    PDE5-IN-5 is a potent and selective inhibitor of phosphodiesterase 5 (PDE5), exhibiting an IC50 of 2.0 nM. This compound is utilized in research to investigate the modulation of cyclic guanosine monophosphate (cGMP) signaling pathways, which are implicated in various physiological processes such as vasodilation and erectile function. PDE5-IN-5 serves as a valuable tool in studies related to cardiovascular diseases and sexual dysfunction.
  46. PDE-IV Inhibitor

    Filaminast is a selective phosphodiesterase type IV (PDE-IV) inhibitor, exhibiting an IC50 of 0.42 μM against canine trachealis PDE-IV. This compound promotes respiratory muscle relaxation and induces bronchodilation, making it a valuable tool for research in respiratory disorders and inflammation-related studies. Its mechanism of action facilitates the modulation of intracellular signaling pathways associated with airway constriction, contributing to potential therapeutic applications in respiratory diseases.
  47. PDE4D Inhibitor

    Catramilast is a selective inhibitor of phosphodiesterase 4D (PDE4D), which plays a crucial role in the regulation of intracellular signaling pathways. This compound is primarily utilized in research focused on pain modulation and inflammatory responses. Its ability to enhance cyclic AMP levels makes it a valuable tool for studying PDE4-mediated biological processes and therapeutic interventions.
  48. PDE4 Inhibitor

    Z21115 is an orally active inhibitor of phosphodiesterase 4 (PDE4), specifically targeting PDE4D7 with an IC50 of 10.5 nM. This compound effectively inhibits the lipopolysaccharide-induced expression of pro-inflammatory cytokines IL-6, TNF-α, and iNOS. Z21115 demonstrates notable anti-inflammatory activity in dextran sulfate sodium (DSS)-induced mouse colitis models while exhibiting minimal toxicity at doses up to 1 g/kg. This makes Z21115 a valuable reagent for research on inflammatory diseases.
  49. PDE4 Inhibitor

    L-869298 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 value of 0.5 nM for the PDE4A isoform. This compound exhibits minimal activity against the hERG potassium channel, making it a valuable tool for studies focused on inflammation, neurodegeneration, and other PDE4-related pathways. Its specificity and efficacy make it a suitable candidate for research applications in therapeutic development targeting PDE4-mediated signaling.
  50. PDE10 Inhibitor

    PyP-1 is a potent and selective inhibitor of the phosphodiesterase 10A (PDE10A) enzyme, exhibiting a strong inhibitory effect with a Ki value of 0.32 nM. This compound has been shown to enhance cognitive behavior and is widely utilized in research focused on neurological conditions such as schizophrenia and cognitive impairment. Its specificity and efficacy make PyP-1 a valuable tool for investigating PDE10A's role in cognitive function and related disorders.

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