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PDE4 Inhibitor
Difamilast is a selective, nonsteroidal phosphodiesterase-4 (PDE4) inhibitor, with a particular affinity for the PDE4B subtype (IC50 = 11.2 nM). It has demonstrated significant potential in the treatment of mild to moderate atopic dermatitis (AD). This reagent is valuable for studies investigating the modulation of inflammatory pathways and therapeutic approaches in dermatological research. -
PDE4 Inhibitor
Piclamilast is a selective phosphodiesterase 4 (PDE4) inhibitor, exhibiting IC50 values of 16 nM in pig aorta and 2 nM in eosinophil soluble assays. This compound is significant in the investigation of inflammatory disorders and respiratory diseases, facilitating research into potential therapeutic interventions for conditions such as asthma and chronic obstructive pulmonary disease (COPD). Its ability to modulate intracellular cyclic AMP levels makes it a valuable tool for studying PDE4-related signaling pathways. -
PDE10A Inhibitor
Elpipodect (MK-8189) is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A), exhibiting a Ki value of 29 pM. This compound demonstrates significant efficacy in modulating intracellular signaling pathways associated with neuropsychiatric disorders. Elpipodect is primarily utilized in research focused on schizophrenia and related conditions, providing valuable insights into potential therapeutic strategies. -
PDE3A-SLFN12 Complex Inducer
BAY 2666605 is an orally active inhibitor of phosphodiesterase 3A (PDE3A) and phosphodiesterase 3B (PDE3B), exhibiting IC50 values of 87 nM and 50 nM, respectively. This compound functions as a complex inducer of the PDE3A-SLFN12 interaction, making it a valuable tool for research investigating the modulation of these pathways. Its application in pharmacological studies may provide insights into the roles of PDE3A and SLFN12 in various biological processes. -
PDE4B Inhibitor
PDE4B-IN-2 is a selective inhibitor of the phosphodiesterase 4B (PDE4B) enzyme, demonstrating an IC50 of 15 nM. It also exhibits activity against PDE4D with an IC50 of 1.7 μM. PDE4B-IN-2 is recognized for its potent anti-inflammatory properties, making it a valuable tool for research applications focused on inflammation and related pathways in various disease models. -
PDE Inhibitor
Trequinsin hydrochloride is a highly potent inhibitor of platelet cyclic adenosine monophosphate (cAMP) phosphodiesterase (PDE), exhibiting an IC50 value of 0.25 nM. This compound effectively prevents the aggregation of human platelets induced by various agonists, including ADP, collagen, thrombin, and epinephrine. Trequinsin hydrochloride serves as a valuable tool for research applications focused on platelet function and the modulation of vascular responses. -
PDE3A Inhibitor
DNMDP is a selective inhibitor of phosphodiesterase 3A (PDE3A) that exhibits potent cytotoxic effects on cancer cells. By binding to PDE3A, DNMDP facilitates the interaction between PDE3A and Schlafen 12 (SLFN12), thereby enhancing its therapeutic efficacy. This compound demonstrates clear cell-selective cytotoxicity, making it a valuable tool for researchers investigating PDE3A's role in cancer biology and therapeutic strategies. -
PDE3 Inhibitor
BRD9500 is a potent phosphodiesterase 3 (PDE3) inhibitor, exhibiting IC50 values of 10 nM and 27 nM for PDE3A and PDE3B, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic development targeting PDE3 pathways. -
PDE4 Inhibitor
Glaucine, a selective phosphodiesterase 4 (PDE4) inhibitor, is an alkaloid sourced from Glaucium flavum. It demonstrates significant biological activities such as bronchodilation, anti-inflammatory effects, and anticancer properties. With a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes, Glaucine promotes relaxation of isolated human bronchi through calcium channel antagonism. Furthermore, it inhibits NF-κB activation, which downregulates MMP-9 expression, thereby impairing the migration and invasion of breast cancer cells. Glaucine is relevant for research applications in asthma and breast cancer. -
PDE6D Degrader
TMX-4100 is a selective degrader of phosphodiesterase 6D (PDE6D), exhibiting high degradation efficacy with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cell lines. This compound demonstrates potential for targeting PDE6D in research related to multiple myeloma, providing a valuable tool for investigating therapeutic strategies in this area. -
PDE11 Inhibitor
BC11-38 is a selective inhibitor of phosphodiesterase 11 (PDE11) with an IC50 of 0.28 µM, demonstrating over 100-fold selectivity against other PDE isoforms (PDE1-10). This compound effectively elevates cyclic AMP (cAMP) levels, enhancing protein kinase A (PKA)-mediated phosphorylation of ATF-1 and stimulating cortisol production in H295R cells. BC11-38 is valuable for research into the regulatory mechanisms of cAMP signaling and its implications in endocrine function. -
PDE4B PET Radioligand
PF-06445974 is a potent phosphodiesterase 4B (PDE4B) inhibitor with an IC50 of less than 1 nM, demonstrating high specificity compared to PDE4 isoforms A, C, and D, with IC50 values of 36 nM, 17 nM, and 4.7 nM, respectively. This radioligand is designed for positron emission tomography (PET) imaging, exhibiting excellent brain permeability and significant specific binding capabilities. PF-06445974 is a valuable tool for researching PDE4B-related neurobiological processes and diseases. -
PDE Inhibitor
Carbazeran is a potent phosphodiesterase (PDE) inhibitor that serves as a substrate for aldehyde oxidase. This compound is valuable in the study of metabolic diseases, as it may influence cellular signaling pathways regulated by PDEs. Its ability to modulate nucleotide levels positions Carbazeran as a significant tool for research applications focused on metabolic dysregulation. -
PDE4 Inhibitor
YM976 is a potent phosphodiesterase 4 (PDE4) inhibitor, demonstrating an IC50 of 2.2 nM. This compound exhibits significant anti-inflammatory properties while dissociating these effects from emetic responses. YM976 is applicable in research focused on airway hyperresponsiveness and related inflammatory conditions. -
PDE4 Inhibitor
Etazolate hydrochloride is a selective inhibitor of type 4 phosphodiesterase (PDE4) with a reported IC50 of 2 μM. This compound acts as a γ-aminobutyric acid A (GABAA) receptor modulator and promotes the activation of α-secretase, leading to enhanced production of soluble amyloid precursor protein (sAPPα). As a pyrazolopyridine derivative, Etazolate hydrochloride increases intracellular cAMP levels and exhibits anxiolytic, antidepressant, and anti-inflammatory properties. It is a valuable tool for research applications focused on mood disorders, neurodegenerative diseases, and inflammation. -
PDE Inhibitor
3-O-Methylquercetin is a potent inhibitor of phosphodiesterases (PDE), targeting both cAMP and cGMP pathways with IC50 values of 13.8 μM and 14.3 μM, respectively. This compound also inhibits β-secretase with an IC50 of 6.5 μM, showcasing its potential in neuroprotective research against oxidative neuronal damage. Furthermore, 3-O-Methylquercetin exhibits significant antiviral activity against poliovirus, coxsackievirus, and human rhinovirus, along with demonstrated anti-inflammatory and trachea-relaxing properties. Its diverse biological activities make it a valuable tool for studying inflammatory diseases and respiratory conditions such as asthma. -
PDE4 Inhibitor
Orismilast is a selective inhibitor of phosphodiesterase 4 (PDE4) with oral bioavailability, primarily targeting the PDE4B and PDE4D subtype splice variants. It exhibits potent anti-inflammatory activity, making it a valuable tool for the investigation of inflammatory diseases and associated therapeutic pathways. Orismilast's specificity for PDE4 provides insights into its mechanisms in modulating intracellular signaling and inflammatory responses. -
β2-adrenoceptor Agonist/PDE Inhibitor
Reproterol is a dual acting β2-adrenoceptor agonist and phosphodiesterase (PDE) inhibitor. It enhances respiratory function by stimulating β2-adrenoceptors while inhibiting PDE activity, thereby increasing cyclic AMP levels. Reproterol is particularly relevant for research involving asthma and other respiratory conditions, offering insights into therapeutic mechanisms and potential interventions. -
TbrPDEB1/2 Inhibitor
NPD-001 is a potent inhibitor of Trypanosoma brucei phosphodiesterases 1 and 2 (TbrPDEB1/2), demonstrating IC50 values of 4 nM and 3 nM, respectively. This compound effectively raises cAMP levels in parasitic cells, disrupting cytokinesis and leading to the formation of multinucleated, multi-flagellated cells that ultimately undergo lysis. NPD-001 serves as a valuable tool in the study of trypanosomiasis and related infectious diseases. -
PDE Inhibitor
(R)-(-)-Rolipram is a selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating IC50 values of 3 nM, 130 nM, and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. This compound enhances intracellular cAMP levels, making it a valuable tool for studying signal transduction pathways. It is commonly utilized in research related to neuroprotection, inflammation, and other disorders linked to dysregulated cAMP signaling. -
PDE1 Inhibitor
DSR-141562 is a selective inhibitor of phosphodiesterase 1 (PDE1), demonstrating a primary mechanism of action through the inhibition of PDE1B with an IC50 of 43.9 nM. This compound also exhibits lower affinity for PDE1A and PDE1C, with IC50 values of 97.6 nM and 431.8 nM, respectively. DSR-141562 is useful for investigating the positive and negative symptoms, as well as cognitive impairments associated with schizophrenia, making it a valuable tool in psychiatric research. -
PDE4 Inhibitor
Mufemilast is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 80-120 nM. This compound effectively modulates cytokines associated with Behçet's syndrome and exhibits significant inhibition of TNF-α, a key pro-inflammatory cytokine involved in the pathology of psoriasis. Mufemilast is suitable for research applications related to autoimmune conditions, including rheumatoid arthritis, psoriasis, and Behçet’s syndrome. -
PDE3A Inhibitor
(R)-DNMDP is a selective phosphodiesterase 3A (PDE3A) inhibitor, demonstrating significant cytotoxic effects on cancer cells. This compound binds directly to PDE3A, exhibiting a remarkable 500-fold lower EC50 in the HeLa cell line compared to its (S)-enantiomer. Its potent biological activity makes (R)-DNMDP a valuable tool for research related to cancer therapeutics and the modulation of cellular signaling pathways. -
PDE3 Inhibitor
Enoximone is a selective, orally active phosphodiesterase III (PDE3) inhibitor, exhibiting an IC50 of 5.9 μM. By inhibiting cGMP-inhibited PDE, it promotes vasodilation and elevates intracellular cAMP levels. Additionally, Enoximone demonstrates PDE4 inhibitory effects, with an IC50 of 21.1 μM for myocardial PDE4A. This compound is of significant interest for research into congestive heart failure, as well as for its potential bronchodilatory, antiasthma, and anti-inflammatory properties. -
PDE9A Inhibitor
PF-04449613 is a selective inhibitor of phosphodiesterase 9A (PDE9A), exhibiting an IC50 of 22 nM. This compound has demonstrated the ability to enhance motor learning in murine models, making it a valuable tool for investigating cognitive and neuropsychological processes. PF-04449613 is suitable for research applications focused on neurodegenerative diseases and cognitive disorders. -
Phosphodiesterase-5A (PDE5A) Inhibitor
Dasantafil is a selective phosphodiesterase-5A (PDE5A) inhibitor known for its role in modulating cyclic nucleotide levels. It exhibits significant biological activity in enhancing vasodilation and contributes to improved blood flow, making it a valuable tool in the study of genitourinary disorders and erectile dysfunction. This compound is instrumental for research applications focusing on the mechanisms underlying PDE5A inhibition and its therapeutic potential. -
PDE4 Inhibitor
Tetomilast is a selective phosphodiesterase 4 (PDE4) inhibitor that demonstrates the potential to modulate inflammatory responses. It is particularly relevant for research applications concerning inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD). By inhibiting PDE4, Tetomilast may help reduce pro-inflammatory cytokine production, thereby providing insights into therapeutic strategies for these chronic inflammatory conditions. -
PDE10A Inhibitor
Mardepodect hydrochloride is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A), exhibiting an IC50 value of 0.37 nM and demonstrating greater than 1000-fold selectivity over other phosphodiesterases. This compound has the ability to cross the blood-brain barrier, making it a valuable tool in neurological research. Its selective inhibition of PDE10A may provide insights into disorders such as schizophrenia and movement disorders, offering potential pathways for therapeutic development. -
PDE4 Inhibitor
PF-07038124 hydrochloride is a potent phosphodiesterase 4 (PDE4) inhibitor, exhibiting an IC50 of 0.5 nM for the PDE4B2 isoform. This compound displays significant inhibitory effects on pro-inflammatory cytokines, including IL-13, IL-4, and IFNγ, with IC50 values of 125 nM, 4.1 nM, and 1.06 nM, respectively. PF-07038124 hydrochloride serves as a valuable research tool for studying conditions such as atopic dermatitis and plaque psoriasis, aiding in the exploration of therapeutic interventions targeting inflammatory pathways. -
PDE12 Inhibitor
PDE12-IN-1 is a potent and selective inhibitor of phosphodiesterase 12 (PDE12), exhibiting an enzyme inhibition pIC50 value of 9.1. This compound effectively elevates levels of 2′,5′-linked adenylate polymers (2-5A), with a pharmacological effect characterized by a pEC50 value of 7.7. PDE12-IN-1 demonstrates significant antiviral activity, making it a valuable tool in biochemical research related to viral pathogenesis and therapeutic interventions. -
PDE4 Inhibitor
KVA-D-88 is a potent phosphodiesterase 4 (PDE4) inhibitor, specifically targeting PDE4B and PDE4D with IC50 values of 140 nM and 880 nM, respectively. This compound readily crosses the blood-brain barrier and promotes cAMP accumulation, thereby modulating neuroactive substance-driven behaviors such as hyperlocomotion and locomotor sensitization. KVA-D-88 is valuable for research applications focused on drug addiction and related neurobiological processes. -
PDE Inhibitor
Ophiobolin A is a potent inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase (PDE), exhibiting an IC50 value of 9 μM. This fungal metabolite, known for its phytotoxic properties, demonstrates significant antimicrobial and anticancer activities. Ophiobolin A is utilized in research applications exploring PDE inhibition and its effects on various cellular processes. -
PDE4 Inhibitor
SCH 351591 is a selective and potent orally active inhibitor of phosphodiesterase-4 (PDE4), demonstrating an IC50 of 58 nM. It effectively inhibits all four PDE4 subtypes (A, B, C, and D), making it a valuable tool for studying PDE4 biology. This compound has applications in research related to asthma and chronic obstructive pulmonary disease (COPD), offering insights into therapeutic strategies for these conditions. -
PDE2A Inhibitor
TAK-915 is a selective inhibitor of phosphodiesterase 2A (PDE2A) with an IC50 of 0.61 nM, demonstrating over 4100-fold selectivity for PDE2A compared to PDE1A. This brain-penetrant and orally active compound is of particular interest for research focused on neuropsychiatric and neurodegenerative disorders. Its unique mechanism of action positions TAK-915 as a valuable tool in the study of underlying pathways in these conditions. -
PDE9 Inhibitor
Tovinontrine is a selective inhibitor of phosphodiesterase-9 (PDE9) with potent inhibitory activity, displaying IC50 values of 8.19 nM for PDE9A1 and 9.99 nM for PDE9A2. It is primarily researched for its potential therapeutic applications in sickle cell disease due to its ability to modulate intracellular signaling pathways. Studies indicate that Tovinontrine's inhibition of PDE9 may contribute to improved clinical outcomes in this condition. -
PDE4 Inhibitor
GSK356278 is a selective phosphodiesterase 4 (PDE4) inhibitor that demonstrates potent activity with pIC50 values of 8.6, 8.8, and 8.7 against human PDE4A, PDE4B, and PDE4D, respectively. This orally bioavailable compound is characterized by its ability to penetrate the blood-brain barrier, exhibiting anti-inflammatory effects alongside anxiolytic and cognition-enhancing properties. GSK356278 is valuable for research in neurodegenerative diseases and mood disorders, making it a significant tool for understanding PDE4 modulation in therapeutic contexts. -
PDE4 Inhibitor
Drotaverine hydrochloride is a selective phosphodiesterase type 4 (PDE4) inhibitor, which effectively prevents the degradation of 3',5'-cyclic adenosine monophosphate (cAMP). This compound demonstrates notable antispasmodic activity in vivo while avoiding anticholinergic side effects. Due to its mechanism of action, Drotaverine hydrochloride is valuable for research involving smooth muscle relaxation and the modulation of cAMP-related cellular pathways. -
PDE4 Inhibitor
Roflupram is a selective phosphodiesterase 4 (PDE4) inhibitor that demonstrates oral bioavailability and effective central nervous system penetration, with an IC50 of 26.2 nM for human PDE4 core catalytic domains. This compound has been shown to reverse cognitive deficits and decrease the production of pro-inflammatory factors, making it valuable for research applications targeting neurological conditions and inflammation-related pathways. -
Phosphodiesterase (PDE) Inhibitor
K134 is a selective phosphodiesterase 3 (PDE3) inhibitor, demonstrating IC50 values of 0.1 µM for PDE3A and 0.28 µM for PDE3B. Inhibition of PDE3 leads to increased levels of cyclic AMP, which plays a crucial role in various physiological processes. This compound can be used in research applications focused on cardiovascular diseases, as well as in studies investigating the modulation of cellular signaling pathways associated with phosphodiesterase activity. -
PDE5A Inhibitor
Robustine is a furoquinoline alkaloid that acts as a potent inhibitor of human phosphodiesterase 5 (hPDE5A). This compound demonstrates significant inhibitory activity, making it useful for research applications in studying cardiovascular diseases and erectile dysfunction. Its selective targeting of hPDE5A highlights its potential as a therapeutic agent in related fields of investigation. -
PDE7 Inhibitor
PDE7-IN-2 is a selective phosphodiesterase 7 (PDE7) inhibitor with an IC50 value of 2.1 µM. It is primarily utilized in research focused on neurological disorders, particularly Parkinson's disease. By inhibiting PDE7, this compound can elevate intracellular levels of cyclic AMP, potentially influencing neuroprotective pathways and neuroinflammation. -
PDE10A Inhibitor
5,7-Dichloropyrazolo[1,5-a]pyrimidine is a potent inhibitor of phosphodiesterase 10A (PDE10A) with a Ki value of 24 μM. This compound plays a crucial role as an intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives, which are investigated for their potential activity as non-nucleoside reverse transcriptase inhibitors against HIV-1. Additionally, 5,7-Dichloropyrazolo[1,5-a]pyrimidine is utilized in research relating to schizophrenia and related neuropsychiatric disorders. -
PDE5 Inhbitor
PDE5-IN-4 is a selective phosphodiesterase 5 (PDE5) inhibitor that plays a significant role in modulating intracellular signaling pathways. It exhibits potential protective effects in various conditions, including acute myocardial infarction, reperfusion injury, gastrointestinal diseases, diabetes-related complications, and liver failure. This compound is valuable for investigating therapeutic strategies in cardiovascular and metabolic disorders. -
PDE7 Inhibitor
PDE7-IN-3 is an inhibitor of the phosphodiesterase PDE7, exhibiting potential analgesic activity. This compound is valuable for investigating various pain models, including inflammatory, neuropathic, visceral, and nociceptive pain. Researchers can utilize PDE7-IN-3 to explore the effects of PDE7 inhibition on pain mechanisms and develop new therapeutic strategies. -
Phosphodiesterase (PDE) Inhibitor
Cirsimarin is a potent phosphodiesterase (PDE) inhibitor derived from Microtea debilis. This flavonoid demonstrates significant antilipogenic activity, effectively reducing adipose tissue deposition in murine models. Its lipolytic effects are attributed to its antagonistic action on adenosine A1 receptors and its ability to inhibit phosphodiesterase activity, making it a valuable compound for research in metabolic disorders and lipid metabolism. -
PDE Inhibitor
Homo Sildenafil is a phosphodiesterase (PDE) inhibitor that enhances intracellular cyclic nucleotide levels. This compound effectively increases nitric oxide signaling, leading to vasodilation and improved blood flow. Homo Sildenafil may be utilized in various research applications, including studies on cardiovascular function and erectile dysfunction therapies. Its structural similarity to Sildenafil makes it a valuable tool for investigating PDE-related pathways and pharmacological effects. -
PDE5 Inhibitor
PDE5-IN-7 is a selective inhibitor of phosphodiesterase 5 (PDE5), demonstrating an IC50 value of 5 nM, and shows considerably lower activity against PDE1 with an IC50 of 300 nM. This compound exhibits potent biological activity in the modulation of intracellular cGMP levels, making it a valuable reagent for research focused on cardiovascular disorders and erectile dysfunction. Its specificity and efficacy make PDE5-IN-7 an important tool for understanding PDE5-related pathways. -
PDE Inhibitor
Imazodan is a selective phosphodiesterase III (PDE III) inhibitor that enhances myocardial contractility by preventing the degradation of cyclic adenosine monophosphate (cAMP). This mechanism leads to improved contractile function in cardiac tissues. Additionally, Imazodan acts as a peripheral vasodilator, making it valuable for research applications related to cardiovascular physiology and pharmacology. -
PDE10A Inhibitor
N-Methylbenzamide is a potent inhibitor of phosphodiesterase 10A (PDE10A), a key enzyme involved in regulating intracellular signaling pathways. This compound exhibits anti-cancer activity by modulating cAMP and cGMP levels, which can influence tumor cell proliferation and survival. N-Methylbenzamide is suitable for research applications investigating PDE10A's role in cancer biology and therapeutic strategies targeting this pathway. -
PDE3B Inhibitor
PDE3B-IN-1 is a selective inhibitor targeting phosphodiesterase 3B (PDE3B) with a pIC50 of 6.5, indicating significant potency. Its >300-fold selectivity for PDE3B over other isoforms makes it a valuable tool for studying the role of PDE3B in cellular signaling and metabolic processes. This compound is primarily utilized in research applications related to cardiovascular diseases, obesity, and diabetes, where modulation of PDE3B activity may provide therapeutic insights.

