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Phosphodiesterase (PDE) Inhibitor
Gisadenafil is a selective, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM. By inhibiting PDE5, it effectively prevents the degradation of cyclic guanosine monophosphate (cGMP), leading to increased intracellular cGMP levels. This mechanism has potential applications in the treatment of erectile dysfunction and pulmonary hypertension, facilitating improved vasodilation and blood flow. -
PDE9 Inhibitor
(R)-Irsenontrine is a potent inhibitor of phosphodiesterase 9 (PDE9) with an IC50 value of 0.041 μM. This compound plays a significant role in modulating cGMP levels and is particularly relevant for research focused on neurological diseases. Its ability to selectively inhibit PDE9 makes it a valuable tool for investigations into cognitive function and related pathological conditions. -
PDE5 Inhibitor
PDE5-IN-9 is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 11.2 μM. This compound selectively interacts with key amino acid residues, including Gln 817, Tyr 612, and Ala 767, enhancing its efficacy. PDE5-IN-9 is primarily utilized in research focused on cardiovascular diseases, providing a valuable tool for studying related pathophysiological mechanisms. -
Phosphodiesterase (PDE) Inhibitor
PDE5-IN-8 is a selective phosphodiesterase type 5 (PDE5) inhibitor. This compound enhances intracellular levels of cyclic GMP, leading to vasodilation and increased blood flow. PDE5-IN-8 is primarily utilized in research exploring cardiovascular diseases, erectile dysfunction, and related therapeutic areas, highlighting its potential in modulating nitric oxide signaling pathways. -
PDE4B Inhibitor
HY-072808 is a selective inhibitor of phosphodiesterase-4B (PDE4B), which plays a critical role in modulating cyclic nucleotide signaling pathways. This compound demonstrates potential biological activity in reducing inflammation and may be utilized in research to investigate therapeutic approaches for atopic dermatitis. Its targeted inhibition of PDE4B makes it a valuable tool for studying the effects of cyclic nucleotide modulation in various cellular contexts. -
PDE4 Inhibitor
PDE4-IN-29 is a selective phosphodiesterase 4 (PDE4) inhibitor, with sub-nanomolar potency against PDE4D3, exhibiting IC50 values of less than 5 nM. By inhibiting the degradation of cyclic adenosine monophosphate (cAMP), PDE4-IN-29 effectively elevates intracellular cAMP levels, leading to a reduction in inflammatory cytokine release, including TNF-α. This compound is of great interest for investigating inflammatory diseases such as psoriasis, atopic dermatitis, and chronic obstructive pulmonary disease. -
PDE10A Inhibitor
ASP9436 is a potent and orally available inhibitor of phosphodiesterase 10A (PDE10A), exhibiting an IC50 of 8 nM against human PDE10A. This compound effectively reduces locomotor activity in mouse models of hyperactivity and improves visual recognition memory deficits in neonatal mice. ASP9436 is valuable for research focused on understanding and potentially treating schizophrenia. -
PDE4 Inhibitor
Tofimilast is a selective inhibitor of Phosphodiesterase 4 (PDE4) with an IC50 of 0.14 μM. By blocking PDE4 activity, Tofimilast elevates intracellular cyclic adenosine monophosphate (cAMP) levels, contributing to its anti-inflammatory properties. This reagent is valuable for research applications aimed at exploring inflammatory pathways and potential therapeutic interventions in respiratory and autoimmune conditions. -
PDE4D Inhibitor
GEBR-7b is a selective inhibitor of phosphodiesterase 4D (PDE4D), exhibiting an IC50 of 0.67 μM. This compound enhances hippocampal cyclic adenosine monophosphate (cAMP) levels without affecting amyloid-beta (Aβ) concentrations in rodent models. GEBR-7b has demonstrated efficacy in improving spatial memory, making it suitable for investigating cognitive deficits and the underlying mechanisms of neurodegenerative diseases. -
cGMP-PDE Inhibitor
DPN-205-734 is a selective cGMP-PDE inhibitor that exerts positive inotropic effects on cardiac muscle cells. This compound has been shown to reduce blood pressure and overall peripheral resistance in various animal models, indicating its potential for cardiovascular effects. DPN-205-734 is suitable for research applications focused on cardiovascular and cerebrovascular diseases, including heart failure and related conditions. -
PDE4D2 Inhibitor
Norbraylin is a natural prenylated coumarin that serves as an inhibitor of the phosphodiesterase 4D2 (PDE4D2) enzyme, exhibiting an IC50 value of 7.15 µM. This compound is utilized in research to explore the modulation of intracellular signaling pathways mediated by cyclic adenosine monophosphate (cAMP). Its activity makes it a valuable tool for studies related to inflammation, neurobiology, and various other fields of biomedical research. -
PDE5 Inhibitor
T-1032 is a selective phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 value of 1.0 nM. This compound demonstrates a relaxant effect on isolated rabbit corpus cavernosum, making it a valuable tool for investigating mechanisms involved in erectile dysfunction. T-1032 is suitable for research applications focused on penile vascular physiology and therapies for erectile dysfunction. -
PDE4 Inhibitor
PDE4-IN-33 is a selective inhibitor of phosphodiesterase 4 (PDE4), an enzyme involved in the degradation of cyclic AMP. This compound effectively reduces uric acid levels, making it a valuable tool for studying conditions associated with hyperuricemia and gout. Its role in modulating inflammatory responses highlights its potential in therapeutic research for these metabolic disorders. -
PDE3/PDE4 Inhibitor
ORG-20241 is a dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4). This compound exhibits a significant bronchodilator effect and effectively prevents allergen-induced airway hyperresponsiveness. Additionally, ORG-20241 significantly inhibits eosinophil infiltration at elevated concentrations. It serves as a valuable tool for research focused on asthma and related respiratory conditions. -
PDE10A Inhibitor
PDE10A-IN-1 is a potent inhibitor of phosphodiesterase 10A (PDE10A), exhibiting an IC50 of 250 nM. This compound effectively crosses the blood-brain barrier, making it valuable for studies related to neurological disorders, particularly schizophrenia. Research applications include investigating the role of PDE10A in neuropsychiatric conditions and exploring therapeutic avenues for treatment. -
PDE3/PDE4 Inhibitor
ICI-63197 is a dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), exhibiting Ki values of 9 µM and 10 µM, respectively. This compound demonstrates selectivity against PDE1 and PDE2, allowing for targeted modulation of cyclic nucleotide levels. ICI-63197 is noted for its antidepressant effects, making it a valuable tool for research into mood disorders and the underlying mechanisms of antidepressant action. -
PDE-III Inhibitor
EMD 57439 is a selective inhibitor of phosphodiesterase III (PDE-III), which plays a critical role in regulating intracellular signaling pathways. This compound is characterized by its ability to modulate cAMP levels without significantly increasing their concentration, and it exhibits minimal impact on calcium signaling (Ca(50)). EMD 57439 is valuable for research applications focused on cardiovascular function, cell signaling, and the pharmacological exploration of PDE inhibitors. -
Phosphodiesterase (PDE)
D-4418 is a selective phosphodiesterase 4 (PDE4) inhibitor, demonstrating significant anti-inflammatory activity. It is primarily being investigated for its potential therapeutic effects in treating asthma and chronic obstructive pulmonary disease (COPD). This compound offers valuable insights into the modulation of inflammatory pathways, making it a useful tool for research in respiratory diseases. -
PDE10A Inhibitor
SCH-1518291 is a potent, orally active inhibitor of phosphodiesterase type 10A (PDE10A). This compound demonstrates antipsychotic effects in animal models of attention-deficit/hyperactivity disorder (ADHD). SCH-1518291 is valuable for investigating neurological disorders, particularly those related to psychosis and cognitive dysfunction. -
Phosphodiesterase (PDE) Inhibitor
Tolafentrine is a dual-selective phosphodiesterase 3 and 4 (PDE3/4) inhibitor that exhibits significant therapeutic potential in managing pulmonary hypertension. In studies utilizing a unilateral diacetamide-induced rat model, Tolafentrine demonstrated the ability to alleviate hemodynamic and gas exchange abnormalities associated with the condition. Additionally, long-term administration was shown to reduce right ventricular hypertrophy and normalize pulmonary vascular remodeling, highlighting its relevance in cardiovascular research and potential therapeutic applications. -
PDE1C Inhibitor
PDE1-IN-5 is a selective inhibitor of phosphodiesterase 1C (PDE1C), exhibiting an IC50 value of 15 nM. This compound demonstrates significant anti-inflammatory activity by reducing the expression of key pro-inflammatory cytokines, including iNOS, TNF-α, IL-1α, IL-1β, and IL-6 in response to LPS stimulation. PDE1-IN-5 has been shown to mitigate symptoms associated with inflammatory bowel disease (IBD) in the dextran sodium sulfate (DSS)-induced colitis mouse model, making it a valuable tool for research in IBD mechanisms and therapies. -
Phosphodiesterase (PDE)
Amentoflavone hexaacetate is a selective inhibitor of phosphodiesterase (PDE), demonstrating notable antiplatelet aggregation properties. This compound effectively inhibits ADP- or collagen-induced platelet aggregation and reduces cAMP phosphodiesterase activity in human platelets, resulting in significantly elevated cAMP levels in the presence of prostaglandin E1. Additionally, amentoflavone hexaacetate exhibits anti-angiogenic and anti-metastatic effects, making it a valuable tool for research in cardiovascular and cancer biology. -
PDE4 Inhibitor
PDE4-IN-11 is a selective inhibitor of phosphodiesterase isoenzyme 4 (PDE4). It exhibits potent bronchodilatory and anti-inflammatory activities, making it a valuable tool for investigating obstructive and inflammatory airway diseases. This compound is particularly relevant for research focused on respiratory conditions and the modulation of inflammatory pathways. -
Phosphodiesterase (PDE) Inhibitor
PF-04471141 hydrochloride is a potent inhibitor of phosphodiesterase (PDE), specifically targeting PDE1. By regulating intracellular levels of cAMP and cGMP, this compound influences signaling pathways involved in cell proliferation and vascular smooth muscle function. It serves as a valuable tool for research into cardiovascular biology and related signaling mechanisms. -
PDE Inhibitor
Phosphodiesterase-IN-2 is a selective inhibitor of phosphodiesterase 10A (PDE10A), demonstrating an IC50 value of 11.9 nM. This compound enhances the stability of liver microsomes while demonstrating reduced permeability across the blood-brain barrier. Additionally, Phosphodiesterase-IN-2 exhibits favorable pharmacokinetic properties and has been shown to mitigate isoprenaline-induced cardiac hypertrophy in murine models, making it a valuable tool for cardiac research and drug development. -
PDE2a Inhibitor
DNS-8254 is a potent inhibitor of phosphodiesterase 2A (PDE2a) with an IC50 of 8 nM, demonstrating significant oral bioavailability and the capability to penetrate the blood-brain barrier. This compound is associated with memory-enhancing effects in rodent models, making it a valuable tool for research into cognitive function and related disorders. Its mechanism suggests potential applications in the study of neurodegenerative diseases and cognitive impairments. -
PDE4 Inhibitor
D159153 is a selective phosphodiesterase 4 (PDE4) inhibitor that plays a crucial role in modulating intracellular cAMP levels. Its primary biological activity includes anti-inflammatory effects, making it relevant for research applications in asthma, chronic obstructive pulmonary disease (COPD), and neuroinflammatory disorders. This compound is valuable for exploring therapeutic pathways in conditions characterized by dysregulated inflammation. -
Phosphodiesterase (PDE)
Drotaverine is a selective phosphodiesterase (PDE) inhibitor with notable antispasmodic properties. It is primarily employed in the management of angina, as well as pain associated with the gastrointestinal and biliary tracts. Additionally, Drotaverine has been implicated in inducing priapism, a side effect characterized by prolonged penile erection, highlighting its diverse biological effects in both vascular and smooth muscle contexts. -
PDE Inhibitor
PDE2A-IN-1 is a highly potent inhibitor of phosphodiesterase 2A (PDE2A) with an IC50 of 1.3 nM. This compound modulates intracellular cyclic nucleotide levels, enhancing signaling pathways associated with cellular regulation and function. PDE2A-IN-1 is utilized in research focusing on neurodegenerative diseases, cardiovascular research, and other conditions where PDE2A activity is implicated. -
PDE4 inhibitor
Arofylline is a phosphodiesterase type 4 (PDE4) inhibitor that plays a significant role in regulating inflammatory processes. It exhibits biological activity by promoting increased levels of cyclic AMP, which can lead to the relaxation of airway smooth muscle and decreased airway inflammation. This compound is primarily used in research related to asthma and other respiratory diseases, offering insights into therapeutic approaches for managing airway hyperresponsiveness and inflammation. -
PDE5/PDEI Inhibitor
Ilexsaponin B2 is a saponin derived from the root of Ilex pubescens Hook. et Arn. It acts as a potent inhibitor of phosphodiesterase 5 (PDE5) and phosphodiesterase I (PDEI), with IC50 values of 48.8 μM and 477.5 μM, respectively. This compound is valuable for research applications focused on vascular biology and therapeutic areas related to erectile dysfunction and cardiovascular diseases. -
PDE2 Inhibitor
EHNA is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2) and adenosine deaminase (ADA). It exhibits significant inhibition of cGMP-stimulated PDE2 activity, with an IC50 of 0.8 μM in human samples and 2 μM in porcine myocardium, while showing lesser effects on unstimulated PDE2. EHNA has been implicated in mediating various pharmacological responses, including antiviral, antitumor, and antiarrhythmic activities, making it a valuable tool for research in these domains. -
PDE4 Inhibitor
PDE4-IN-9 is a potent inhibitor of phosphodiesterase 4 (PDE4) exhibiting an IC50 value of 1.4 μM, which is lower than that of the parent compound rolipram (2.0 μM) in in vitro enzyme assays. This compound demonstrates significant biological activity in vivo, effectively modulating inflammatory responses in animal models of asthma, chronic obstructive pulmonary disease (COPD), and sepsis induced by lipopolysaccharide (LPS). PDE4-IN-9 is a valuable tool for researching therapeutic approaches to managing inflammatory diseases. -
PDE4 Inhibitor
FCPR16 is a selective inhibitor of Phosphodiesterase 4 (PDE4), a crucial enzyme involved in the hydrolysis of cyclic adenosine monophosphate (cAMP). By inhibiting PDE4, FCPR16 effectively increases cAMP levels in SH-SY5Y neuroblastoma cells, facilitating enhanced signaling pathways associated with neuronal functions. This compound is valuable for research investigating the molecular mechanisms underlying Parkinson's disease and other neurodegenerative disorders. -
PDE3/4 Inhibitor
KCA-1490 is a dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), exhibiting IC50 values of 369 nM and 42 nM, respectively. This compound demonstrates significant bronchodilatory and anti-inflammatory effects, effectively suppressing histamine-induced bronchoconstriction in vivo. KCA-1490 is a valuable tool for research into asthma and chronic obstructive pulmonary disease (COPD) pathways and therapeutic strategies. -
PDE Inhibitor
BC8-15 is a phosphodiesterase (PDE) inhibitor, demonstrating IC50 values of 0.28 µM for PDE8A, 0.22 µM for PDE4A, and 6.46 µM for PDE7A. This compound has been shown to enhance steroidogenesis in mouse Leydig cells, making it a valuable tool for research investigating steroid hormone biosynthesis and PDE-related signaling pathways. Its efficacy in selectively inhibiting multiple PDE isoforms positions BC8-15 as a significant reagent for studies in reproductive biology and pharmacology. -
PDE Inhibitor
Isbufylline is a phosphodiesterase (PDE) inhibitor that is available for oral administration. It demonstrates anti-inflammatory and bronchodilatory effects, making it useful for investigating respiratory diseases such as asthma and pneumonia. Its application in research can provide insights into the modulation of inflammatory responses and airway reactivity. -
β₂-adrenergic receptor Agonist/PDE4 Inhibitor
GS-5759 is a dual-action compound functioning as a β₂-adrenergic receptor agonist and a phosphodiesterase 4 (PDE4) inhibitor. By activating the β₂ receptor, GS-5759 elevates intracellular cAMP levels, resulting in bronchial dilation. Additionally, its inhibition of PDE4 activity decreases cAMP degradation, thereby enhancing anti-inflammatory responses. This compound is relevant for research into respiratory disorders, particularly chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilatory and anti-inflammatory effects in preclinical models. -
PDE Inhibitor
Hydroxychlorodenafil is a phosphodiesterase (PDE) inhibitor that modulates intracellular signaling pathways through the inhibition of cyclic nucleotide degradation. This compound demonstrates potential biological activity in cancer research, making it a valuable tool for elucidating the role of PDEs in tumor biology and therapeutic interventions. Hydroxychlorodenafil is suitable for studies exploring the mechanisms of cancer progression and the development of novel treatment strategies. -
PDE1 Inhibitor
PF-04677490 is a potent inhibitor of phosphodiesterase 1 (PDE1), with IC50 values of 21 nM, 83 nM, and 118 nM for PDE1B1, PDE1C, and PDE1A, respectively. This compound effectively inhibits the hydrolytic activity of cAMP and cGMP, making it a valuable tool for investigating signaling pathways mediated by cyclic nucleotides. PF-04677490 is suitable for research applications focused on cardiovascular, neurological, and inflammatory diseases. -
PDE5 Inhibitor
Lunamarine is a potent phosphodiesterase type 5 (PDE5) inhibitor with the ability to cross the blood-brain barrier. This compound demonstrates significant biological activity in the context of pulmonary arterial hypertension (PAH) and erectile dysfunction (ED). It serves as a valuable tool for researchers investigating therapeutic strategies for these conditions. -
PDE4 Inhibitor
Z19153 is a selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 110 nM for PDE4B1 and 1160 nM for PDE4D7. This compound demonstrates significant hepatoprotective effects in the context of hepatic sepsis, making it a valuable tool for studying inflammatory responses in liver disease. Z19153 is suitable for research applications focused on PDE4-related signaling pathways and their implications in various physiological and pathological conditions. -
PDE Inhibitor
SAL-0010042 is a potent inhibitor of Plasmodium phosphodiesterase β (PDEβ), effectively blocking the hydrolysis of cAMP and cGMP with an IC50 of 48.9 nM in gametocytes. This compound activates protein kinase G (PKG) and demonstrates significant inhibitory effects on the growth and development of Plasmodium, with IC50 values of 142 nM and 218 nM for the 3D7 and Dd2 strains, respectively. Additionally, SAL-0010042 also inhibits human phosphodiesterases hPDE5 and hPDE6 with IC50 values of 632 nM and 73 nM, making it valuable for research in malaria and related diseases. -
PDE3A Inhibitor
4'-Methoxyisoagarotetrol is a chromone derivative that primarily targets phosphodiesterase 3A (PDE3A). This compound exhibits moderate inhibitory activity with an IC50 value of 54 μM. It is utilized in research applications focused on PDE3A modulation, contributing to studies in cardiovascular and neurobiology fields. -
PDE Inhibitor
Phosphodiesterase-IN-1 is a phosphodiesterase (PDE) inhibitor recognized for its anti-Plasmodium activity. This compound demonstrates significant antiproliferative effects against Plasmodium falciparum (strain 3D7), exhibiting an IC50 value of 0.64 μM. It is a valuable tool for research into malaria treatment and the role of PDEs in parasitic infections. -
PDE9 Inhibitor
Irsenontrine maleate is a selective inhibitor of phosphodiesterase 9 (PDE9) with oral bioavailability. This compound has demonstrated potential in modulating intracellular signaling pathways, making it a valuable tool for investigating mechanisms underlying neurological diseases. Research applications include studies focused on cognitive function, neuroprotection, and the treatment of neurodegenerative disorders. -
PDE Inhibitor
Torbafylline is a potent phosphodiesterase (PDE) inhibitor that specifically targets the PDE4 pathway. It has been shown to reduce protein degradation in rat skeletal muscle following thermal injuries by activating the cAMP/EPAC/PI3K/Akt signaling pathway. Torbafylline effectively suppresses the heightened ubiquitin-proteasome-dependent protein breakdown associated with conditions such as cancer and sepsis in skeletal muscle, making it a valuable tool for research in muscle wasting and related disorders. -
PDE Inhibitor
Mangostanol is a polyoxygenated xanthone derived from the pericarp of Garcinia mangostana. It functions as a phosphodiesterase (PDE) inhibitor, effectively modulating cAMP levels within cells. This compound exhibits potential anti-inflammatory and antioxidant activities, making it relevant for research in cellular signaling pathways, pharmacology, and therapeutic applications targeting PDE-related diseases. -
PDE10A Inhibitor
JNJ-42314415 is a selective phosphodiesterase 10A (PDE10A) inhibitor, demonstrating Ki values of 35 nM and 64 nM for human recombinant PDE10A and rat PDE10A, respectively. This compound plays a significant role in regulating intracellular signaling pathways through the modulation of cAMP and cGMP levels. JNJ-42314415 is valuable in research applications related to neurological disorders and potential therapeutic strategies for conditions such as schizophrenia and Parkinson's disease. -
PDE5/Na+/H+ Exchanger Inhibitor
1,3,5-Trihydroxy-4-prenylxanthone is an inhibitor of phosphodiesterase type 5 (PDE5) and the Na+/H+ exchanger, with an IC50 value of 3.0 μM and a minimum inhibitory concentration of 10 μg/mL. It effectively inhibits lipopolysaccharide (LPS)-induced nitric oxide production in RAW264.7 macrophages, showcasing its potential anti-inflammatory properties. This compound is valuable for research applications focused on inflammatory pathways and cellular signaling involving nitric oxide.

