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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
PDE5A Inhibitor
PF-03049423 is a potent and highly selective inhibitor of phosphodiesterase-5A (PDE5A), demonstrating an IC50 of approximately 0.2 nM for both rat and human platelet enzymes. This compound is primarily used in research related to acute ischemic stroke, providing valuable insights into the therapeutic potential of PDE5A modulation in cerebrovascular conditions. Its specificity and potency make it a critical tool for exploring the role of phosphodiesterase inhibition in neuroprotection and recovery following ischemic events. -
PDE4/PDE5 Inhibitor
PDE4/5-IN-1 is a selective inhibitor targeting phosphodiesterase 4 and 5 (PDE4/5). This compound effectively inhibits the activity of PDE5, PDE4B2, and PDE4D2, leading to relaxation of isolated rat prostate tissue and enhanced nitric oxide-induced relaxation. Additionally, PDE4/5-IN-1 reduces alpha-1 adrenoceptor-mediated contractile responses and inhibits the proliferation of human hyperplastic prostate cells. It is a valuable tool for research into benign prostatic hyperplasia. -
PDE1 Inhibitor
PDE1-IN-4 is a selective inhibitor of phosphodiesterase-1 (PDE1), demonstrating IC50 values of 10 nM, 145 nM, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. This compound effectively inhibits the TGF-β1-induced differentiation of human lung fibroblasts into myofibroblasts, showcasing its potential in anti-fibrosis research. By modulating the levels of cAMP and cGMP, PDE1-IN-4 serves as a valuable tool for investigating therapeutic strategies in idiopathic pulmonary fibrosis (IPF). -
PDE4 Inhibitor
PDE4-IN-19 is a selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating IC50 values of less than 10 nM for PDE4B1 and between 10-100 nM for PDE4D3. This compound plays a significant role in modulating intracellular levels of cyclic AMP, making it valuable for research on inflammatory diseases and neurological conditions. PDE4-IN-19 is useful in studying the effects of PDE4 inhibition on cellular signaling pathways and may aid in the development of therapeutics targeting these pathways. -
PDE7 Inhibitor
P7-2104 is a potent inhibitor of phosphodiesterase 7 (PDE7), demonstrating an IC50 of 31 nM. This compound is valuable for studies aimed at modulating cyclic nucleotide signaling pathways, particularly in neurological research. Additionally, P7-2104 can be labeled with carbon-11 for use in positron emission tomography (PET) neuroimaging applications, aiding in the exploration of PDE7's role in various neurological disorders. -
PDE3/PDE4 Inhibitor
Ensifentrine tosylate is a potent dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), exhibiting IC50 values of 0.4 nM and 1479 nM, respectively. By inhibiting these enzymes, Ensifentrine tosylate enhances levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, leading to bronchodilation and suppression of inflammatory cell activation and migration. This compound is instrumental in research pertaining to chronic obstructive pulmonary disease (COPD). -
PDE3/PDE4 Inhibitor
Pumafentrine is a potent orally active dual inhibitor of phosphodiesterase type 3 (PDE3) and phosphodiesterase type 4 (PDE4). It has demonstrated the ability to ameliorate clinical symptoms and reduce colonic TNFα production in murine models of Dextran sulphate sodium (DSS)-induced colitis. Pumafentrine is relevant for research in inflammation and gastrointestinal disorders, providing insights into therapeutic strategies targeting these pathways. -
PDE1 Inhibitor
PF-04827736 is a selective phosphodiesterase 1 (PDE1) inhibitor, exhibiting IC50 values of 9.1 nM, 38 nM, and 42 nM for PDE1B, PDE1C, and PDE1A, respectively. This compound demonstrates a high degree of selectivity for human PDE1 compared to other members of the PDE superfamily (PDE2-PDE11). PF-04827736 is primarily utilized in research related to cardiovascular disease, providing valuable insights into the role of PDE1 in cardiovascular pathology and potential therapeutic interventions. -
Phosphodiesterase (PDE)
Hoquizil hydrochloride functions primarily as a phosphodiesterase (PDE) inhibitor, presenting significant bronchodilator activity. It effectively relaxes smooth muscle tissue, making it a valuable tool in the study of airway conditions and potential therapeutic applications for respiratory diseases. Its oral bioactivity enhances its relevance in pharmacological research and drug development. -
PDE5 Inhibitor
PDE5-IN-1 is a potent phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 5.6 nM and notable oral bioavailability. It interacts with the catalytic domain of PDE5 through hydrogen bonds with the Q817 residue and π-π stacking with the F820 residue. PDE5-IN-1 demonstrates significant anti-cardiac hypertrophy and vasodilatory effects, effectively lowering mean pulmonary arterial pressure and right ventricular hypertrophy index. This compound is valuable for research focused on pulmonary arterial hypertension.

