Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PDE-10A/A2AR Antagonist
PBF-999 is a dual antagonist of phosphodiesterase 10A (PDE-10A) and adenosine A2A receptors (A2AR). This compound exhibits significant modulation of intracellular signaling pathways, contributing to its potential in neuroscience research, particularly in studying disorders such as schizophrenia and Parkinson's disease. PBF-999 may facilitate insights into the therapeutic effects of PDE-10A and A2A receptor signaling in cognitive and motor function. -
PDE4 Inhibitor
Ronomilast is a potent phosphodiesterase-4 (PDE4) inhibitor, exhibiting an IC50 of 3 nM. This compound is primarily utilized in research focused on inflammation-related diseases. By inhibiting PDE4, Ronomilast increases intracellular cyclic AMP levels, thereby modulating inflammatory responses and offering insights into therapeutic strategies for various inflammatory conditions. -
PDE1A1 Inhibitor
PDE1-IN-11 is a potent and selective inhibitor of phosphodiesterase 1A1 (PDE1A1). This compound enhances intracellular levels of cAMP and cGMP, thereby activating the PKA-CREB and NO-cGMP-PKG signaling pathways, which in turn promotes osteoblast differentiation and supports bone formation while inhibiting osteoclastogenesis and bone resorption. PDE1-IN-11 is a valuable tool for investigating postmenopausal osteoporosis and other disorders related to bone metabolism. -
Phosphodiesterase (PDE) Inhibitor
PDE10-IN-6 is a selective inhibitor of phosphodiesterase-10 (PDE10), which plays a crucial role in the degradation of cyclic AMP (cAMP) and cyclic GMP (cGMP). By inhibiting PDE10, this compound enhances the levels of these important second messengers, thereby affecting various signaling pathways. PDE10-IN-6 is primarily utilized in neurological research, specifically in studies related to cognitive function and neurodegenerative diseases. -
PDE-5 Inhibitor
BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor that elevates cGMP levels in tissues, enhancing the expression of nitric oxide (NO) and facilitating smooth muscle relaxation. This reagent is primarily utilized in research related to inflammation, immunology, and cardiovascular diseases, including conditions such as asthma and hypertension. Its ability to modulate cGMP signaling pathways makes it a valuable tool for investigating therapeutic strategies in these areas. -
PDE5 Inhibitor
UK 343664 is a selective inhibitor of phosphodiesterase 5 (PDE5), demonstrating significant potency and oral bioavailability. This compound has been shown to partially reverse thromboxane-induced pulmonary hypertension, indicating its potential therapeutic applications in treating cardiovascular disorders associated with pulmonary hypertension. -
PDE4 Inhibitor
CP-220629 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.44 μM. This compound is effective in mitigating airway obstruction, as evidenced by an ED50 of 2.0 mg/kg in guinea pig models using aerosolized antigen. CP-220629 is utilized in research aimed at exploring therapeutic strategies for respiratory conditions related to PDE4 activity. -
PDE10A Antagonist
AMG580 is a selective antagonist of phosphodiesterase 10A (PDE10A) with subnanomolar affinity across rat, primate, and human isoforms. This compound demonstrates significant biological activity in modulating intracellular signaling pathways associated with PDE10A inhibition. AMG580 is particularly useful in research applications involving noninvasive radiotracers, aiding in the exploration of brain imaging and neuropharmacology. -
PDE2 Agonist
5,6-DCl-cBIMP is a cyclic adenosine monophosphate (cAMP) analog that functions as an agonist of phosphodiesterase 2 (PDE2). This compound significantly enhances the hydrolytic activity of PDE2 on both cAMP and cGMP, making it a valuable tool for studying signal transduction pathways. Its potency and specificity position it as a useful reagent in research related to cardiovascular, neurological, and metabolic disorders. -
PDE4 Inhibitor
MK-0952 sodium is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, demonstrating an IC50 of 0.53 nM. This compound exhibits potential therapeutic effects in modulating inflammatory responses and cognitive functions, making it a valuable tool in Alzheimer’s disease research. MK-0952 sodium can be utilized to study the role of PDE4 in neurodegenerative disorders. -
PDE4 Inhibitor
UK-500001 is a selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating high potency with IC50 values of 0.28 nM for PDE4D3, 22.8 nM for PDE4B2, 26.1 nM for PDE4A4, and 271 nM for PDE4C2. This compound exhibits significant anti-inflammatory properties by effectively inhibiting the release of TNF-α and IFN-γ in both human and rodent macrophagic cell lines at nanomolar concentrations. UK-500001 holds potential for research applications in chronic obstructive pulmonary disease (COPD) and asthma treatment. -
PDE Inhibitor
Dazonone is a selective phosphodiesterase III (PDE3) inhibitor, exhibiting an IC50 of 1.68 μM. This compound enhances intracellular levels of cyclic AMP, leading to increased vasodilation and improved cardiac function. Dazonone is utilized in research on cardiovascular diseases and for investigating cellular signaling pathways involving cAMP modulation. -
PDE5 Inhibitor
N-Desethyl-N-methyl vardenafil is a potent PDE5 inhibitor, exhibiting an IC50 value of 0.14 μM. This compound is primarily utilized in pharmacological research focused on the modulation of erectile dysfunction and related cardiovascular conditions. Its capacity to inhibit PDE5 facilitates increased levels of cyclic GMP, thus enhancing vascular smooth muscle relaxation and blood flow. -
PDE Inhibitor
5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione is identified as a phosphodiesterase (PDE) inhibitor, specifically targeting both snake venom and human recombinant PDE 1 with IC50 values of 429 μM and 467 μM, respectively. Additionally, it exhibits weak inhibition of mushroom tyrosinase, with a calculated Ki of 1.9 μM. This compound can be utilized in biochemical research related to enzyme inhibition and potential pharmacological applications concerning PDE activity. -
PDE5 Inhibitor
Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 value of 3.95 ng/mL. This compound is primarily utilized in research related to erectile dysfunction, offering valuable insights into its mechanisms and potential therapeutic applications. -
Phosphodiesterase (PDE) Inhibitor
Hedgehog IN-8 is a potent phosphodiesterase (PDE) inhibitor that modulates hedgehog signaling pathways. This compound demonstrates significant biological activity in disrupting aberrant hedgehog signaling, which is often implicated in various cancers and developmental disorders. Hedgehog IN-8 is valuable for research applications aimed at understanding the role of hedgehog signaling in tumorigenesis and developing potential therapeutic interventions. -
PDE1/PDE5 Inhibitor
SCH 51866 is a potent and selective inhibitor of phosphodiesterase 1 (PDE1) and phosphodiesterase 5 (PDE5), with IC50 values of 70 nM and 60 nM, respectively. This compound effectively inhibits collagen-induced aggregation of human washed platelets with an IC50 of 10 μM and demonstrates protective effects against neointimal formation in balloon catheter-injured carotid arteries in spontaneously hypertensive rats. Additionally, SCH 51866 has been shown to reduce blood pressure in this model, making it a valuable tool for research in hypertension and related vascular disorders. -
TbrPDEB1 Inhibitor
Pyrazole N-Desmethyl sildenafil functions as an inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1). It demonstrates approximately 16% inhibition at a concentration of 100 µM. This compound is relevant for research into the pharmacological targeting of TbrPDEB1, which plays a role in the pathogenicity of Trypanosomiasis. -
PDE4 Inhibitor
AWD 12-281 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4), with an IC50 of 9.7 nM. This compound demonstrates significant anti-inflammatory activity and is primarily utilized in research focused on allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis. Its oral bioavailability facilitates in vivo studies of PDE4 modulation in various inflammatory diseases. -
PDE Inhibitor
MP 518 is a phosphodiesterase (PDE) inhibitor that exhibits antihypertensive properties. By inhibiting the degradation of cyclic adenosine monophosphate (cAMP), MP 518 facilitates an increase in intracellular calcium (ICa) levels and antagonizes β-adrenergic stimulation, leading to vasodilation. This compound is valuable for research in cardiovascular biology and the mechanisms underlying hypertension. -
PDE Inhibitor
Pimobendan hydrochloride is a selective phosphodiesterase 3 (PDE3) inhibitor, with an IC50 value of 0.32 μM. It enhances cardiac contractility and promotes vasodilation, making it relevant for research into heart failure and other cardiovascular conditions. This compound can be utilized in studies exploring the modulation of cAMP levels and its effects on cardiac performance. -
Phosphodiesterase (PDE) Inhibitor
Dipyridamole Mono-O-β-D-glucuronide is an O-glucuronide derivative of Dipyridamole, a well-known phosphodiesterase (PDE) inhibitor. This compound exhibits significant inhibitory activity against PDE, which can influence cellular signaling pathways. Dipyridamole Mono-O-β-D-glucuronide is primarily utilized in research exploring drug metabolism and transport mechanisms, as well as in studies assessing the therapeutic potential of PDE inhibition. -
PDE11A Modulator
PDE11A modulator-1 is a selective modulator targeting phosphodiesterase 11A (PDE11A). This compound enhances intracellular cAMP levels, thereby influencing various signaling pathways. It has potential applications in the study of metabolic disorders and neurological conditions linked to cAMP signaling. PDE11A modulator-1 serves as a valuable tool for researchers investigating the role of PDE11A in cellular processes and therapeutic development. -
PDE IV Inhibitor
RS14203 is a potent inhibitor of phosphodiesterase type IV (PDE IV), which plays a crucial role in the regulation of cyclic nucleotide signaling. This compound is known to induce emesis, making it valuable in research focused on gastrointestinal function and the emetic response. Its application extends to investigations of PDE IV's involvement in various physiological processes and the development of therapeutic strategies targeting cyclic nucleotide pathways. -
PDE2 Inhibitor
BML-288 is a potent inhibitor of phosphodiesterase 2 (PDE2) with an IC50 value of 40 nM. This compound demonstrates significant biological activity in modulating cyclic nucleotide levels, making it relevant for research into osteoarthritis pain and related conditions. Its ability to selectively inhibit PDE2 provides valuable insights into cellular signaling pathways and therapeutic targets in inflammatory and pain-related disorders. -
Phosphodiesterase (PDE)
Oxagrelate is a selective inhibitor of cyclic adenosine monophosphate phosphodiesterase (PDE). It demonstrates concentration-dependent inhibition of platelet aggregation induced by collagen and adenosine diphosphate (ADP) in vitro. This compound is valuable for research applications focused on platelet activation, hemostasis, and thrombotic disorders. -
PDE5 Inhibitor
UK-371800 is a highly selective phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 of 4.2 nM. This compound demonstrates favorable permeability characteristics and remains unaffected by P-glycoprotein efflux mechanisms. UK-371800 is primarily utilized in research applications related to erectile dysfunction and pulmonary hypertension, contributing to the understanding of cGMP signaling pathways in cardiovascular health.
