Catalog No.
Product Name
Application
Product Information
Citations
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PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride is a potent inhibitor of phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4), and phosphodiesterase 5 (PDE5), with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. Additionally, it acts as an antagonist of the H1-histamine receptor, contributing to its anti-inflammatory properties. Fenspiride is primarily utilized in research related to respiratory diseases, offering insights into mechanisms of action and potential therapeutic applications. -
PDE1C/PDE4B Inhibitor
Sudachitin is a potent inhibitor of phosphodiesterase 1C (PDE1C) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 5.0 μM and 15.0 μM, respectively. It enhances the expression of Sirt1 and PGC-1α in skeletal muscle, thereby influencing energy metabolism and promoting mitochondrial biogenesis. Sudachitin demonstrates beneficial effects on lipid metabolism, improves glucose tolerance and insulin sensitivity, and stimulates energy expenditure and fatty acid β-oxidation. Additionally, it activates the p38MAPK signaling pathway, influences apoptosis, and exhibits significant anti-inflammatory properties by reducing TNF-α, NO, and iNOS expression in macrophages. This compound is suitable for research in metabolic syndrome, type 2 diabetes, and psoriasis. -
PDE6D/CK1α Degrader
TMX-4113 is a degrader targeting phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). This compound exhibits significant biological activity in the degradation of these proteins, making it a valuable tool for investigating their roles in cancer research. TMX-4113 can facilitate studies aimed at elucidating the molecular mechanisms underlying tumor progression and treatment responses. -
PDE4 Inhibitor
Etazolate is a selective phosphodiesterase 4 (PDE4) inhibitor that exhibits anti-inflammatory properties by reducing interleukin-1 beta (IL-1β) levels. This compound demonstrates a dose-dependent effect on inflammation and edema, while also contributing to enhanced memory performance. Additionally, Etazolate's modulation of GABAA receptors suggests potential applications in research related to mood disorders, particularly in studying antidepressant-like effects. -
PDE4 Inhibitor
PDE4-IN-8 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.93 nM specifically for the PDE4B2 isoform. This compound exhibits selective inhibition, with minimal effects on cytokines such as IL-13 (IC50 = 4.04 nM), IL-4 (IC50 = 36.33 nM), and IFN-γ (IC50 = 2394 nM). PDE4-IN-8 is suitable for research applications focused on inflammation and other PDE4-related pathways in various biological contexts. -
PDE3A/PDE4B Inhibitor
PDE3/4-IN-4 is a potent and selective inhibitor of phosphodiesterase 3A (PDE3A) and phosphodiesterase 4B (PDE4B), exhibiting IC50 values of 10 nM and 9.4 nM, respectively. This compound modulates the cAMP/PKA/CREB signaling pathway, effectively inhibiting the pro-inflammatory cytokine IL-6 and reducing expression of inflammatory markers in liver tissue. PDE3/4-IN-4 demonstrates potential in mitigating liver fibrosis and limiting liver damage in models of cholestatic and sepsis-induced liver diseases. This reagent is suitable for research focused on liver injury and cholestatic liver disorders. -
PDEδ Autophagic Degrader
PDEδ autophagic degrader 1 is a targeted autophagic degrader of PDEδ, functioning through an autophagosome-tethering mechanism. This compound effectively reduces the levels of PDEδ protein via lysosome-mediated autophagy, while leaving PDEδ mRNA expression unchanged. Its ability to suppress growth in KRAS mutant pancreatic cancer cells highlights its potential applications in cancer research and therapeutic development. -
PDE4B Inhibitor
Nerandomilast is a potent inhibitor of phosphodiesterase 4B (PDE4B) with an IC50 value of 7.2 nM. Its oral bioavailability and favorable safety profile make it a valuable tool in the research of inflammatory conditions, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD). This compound may facilitate the development of novel therapeutic strategies targeting PDE4B-mediated pathways. -
PDE2A Inhibitor
PDM-631 is a selective inhibitor of phosphodiesterase type 2A (PDE2A) that is both orally active and capable of penetrating the blood-brain barrier. This compound demonstrates potent inhibitory effects, with IC50 values of 1.5 nM against human recombinant PDE2A and 4.2 nM against rat recombinant PDE2A. PDM-631 reliably elevates cGMP levels in the rat cerebral cortex and is valuable for investigating schizophrenia and various neurodegenerative disorders. -
PDE4/PDE IV Inhibitor
Ro 20-1724 is a selective inhibitor of cAMP-specific phosphodiesterase 4 (PDE4). With a Ki value of 1930 nM, it effectively enhances cAMP levels, contributing to its neuroprotective properties. This compound is primarily utilized in research applications focused on neurobiology and the modulation of inflammatory responses. -
PDE3/PDE4 Inhibitor
Ensifentrine 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 elevates the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, leading to bronchodilation and reduced activation and migration of inflammatory cells. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD). -
PDE5 Inhibitor
Zaprinast is a selective inhibitor of cGMP-selective Phosphodiesterase 5 (PDE5), leading to a notable increase in cGMP levels in cardiac myocytes. In addition to its PDE5 inhibition, Zaprinast acts as an agonist for G protein-coupled receptor 35 (GPR35), demonstrating strong activation in rat models and moderate activation in human models. This compound exhibits antiproliferative and proapoptotic effects, making it valuable for research applications focused on vascular remodeling and related cardiovascular studies. -
PDE4 Activator
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), specifically targeting PDE4A4, PDE4B1, PDE4C3, and PDE4D5 variants. This compound effectively inhibits PGE2-induced cyst formation in MDCK cells, exhibiting an EC50 of 1.2 μM. MR-L2 serves as a valuable tool for studying PDE4-related signaling pathways and exploring potential therapeutic applications in conditions involving dysregulated PDE4 activity. -
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.
