Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PDE V Inhibitor
FR-181074 is a selective and orally active phosphodiesterase V (PDE V) inhibitor. By specifically blocking PDE V, it prevents the degradation of cyclic guanosine monophosphate (cGMP), leading to the relaxation of smooth muscle. This compound is valuable for research in cardiovascular diseases and endocrinology, with applications in studying conditions such as hypertension and erectile dysfunction. -
PDE4B/PDE4D Inhibitor
PDE4-IN-32 is a selective inhibitor of phosphodiesterase 4B (PDE4B) and phosphodiesterase 4D (PDE4D) with IC50 values of 13.7 nM and 23.8 nM, respectively. This compound effectively penetrates the blood-brain barrier and has demonstrated the ability to enhance recovery of motor and cognitive function in mouse models of middle cerebral artery occlusion (MCAO). Additionally, PDE4-IN-32 has been shown to reduce cerebral edema and is a valuable tool for research focused on ischemic stroke. -
PDE4 Inhibitor
NVP-ABE171 is a potent, orally active inhibitor of phosphodiesterase 4 (PDE4) that exhibits selective IC50 values of 1.5 nM for PDE4D, 34 nM for PDE4B, 602 nM for PDE4A, and 1230 nM for PDE4C. This compound significantly increases cAMP levels in response to isoproterenol, while also inhibiting eosinophil oxidative bursts and inflammatory cytokine release from T cells and monocytes. NVP-ABE171 demonstrates strong anti-inflammatory effects in preclinical models of asthma and pulmonary inflammation, making it a valuable tool for studying asthma and chronic obstructive pulmonary disease. -
PDE4B Inhibitor
PDE4B-IN-5 is a potent inhibitor of phosphodiesterase 4B (PDE4B), exhibiting an IC50 value of less than 10 nM. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for investigating inflammatory processes. PDE4B-IN-5 is suitable for research applications focused on the modulation of cyclic AMP signaling and its implications in various inflammatory diseases. -
PDE1 Inhibitor
PDE1-IN-12 is a selective phosphodiesterase 1 (PDE1) inhibitor. It effectively inhibits PDE1-mediated suppression of the dopamine D1 receptor signaling pathway, which is crucial for regulating dopaminergic activity. This compound has potential applications in the study of narcolepsy and other neuropsychiatric disorders where dopamine signaling is disrupted. -
Phosphodiesterase (PDE) Inhibitor
ATI22-107 is a dual-pharmacophore inhibitor targeting phosphodiesterase type III (PDE-III) and L-type calcium channels (LTCC). This compound enhances calcium cycling and contractility in cardiac tissues, particularly in cat ventricular myocytes and trabeculae. It is valuable for research focused on cardiac function, calcium signaling, and the pharmacological modulation of heart contractility. -
PDE5 Inhibitor
12-epi-Tadalafil is a potent phosphodiesterase type 5 (PDE5) inhibitor, exhibiting an IC50 value of 0.09 μM. This compound plays a critical role in the modulation of cGMP levels, making it valuable for the study of cardiovascular diseases and related pathophysiological conditions. Its inhibitory effects on PDE5 offer insights into therapeutic approaches for conditions linked to endothelial dysfunction and vasodilatory responses. -
PDE10A Inhibitor
THPP-2 is a selective phosphodiesterase 10A (PDE10A) inhibitor, exhibiting a Ki value of 94 nM. This compound is primarily utilized in the investigation of schizophrenia and offers insights into the mechanisms of this mental disorder. By modulating PDE10A activity, THPP-2 aids in the exploration of potential therapeutic strategies for schizophrenia-related pathophysiology. -
PDE1 Inhibitor
PDE1-IN-7 is a selective inhibitor of bPDE1, demonstrating an IC50 of 10 nM. This compound exhibits notable anti-fibrotic activity, particularly in a bile duct ligation (BDL)-induced liver fibrosis rat model. PDE1-IN-7 is suitable for use in research focused on liver fibrosis and related disorders. -
PDE5 Inhibitor
PDE5-IN-15 is a xanthine derivative functioning as a selective inhibitor of phosphodiesterase type 5 (PDE5). With IC50 values of 0.002 μM against human PDE5, 0.180 μM against bovine PDE6, and 2.85 μM against bovine PDE1, this compound demonstrates potent activity. PDE5-IN-15 exhibits promising oral bioavailability in canines, making it a valuable tool for research on male erectile dysfunction and related therapeutic applications. -
PDE Inhibitor
PDE4-IN-3 is a potent phosphodiesterase 4 (PDE4) inhibitor, exhibiting an inhibitory affinity with an IC50 value of 4.2 nM. This compound effectively modulates intracellular cAMP levels, making it a valuable tool in research focused on inflammatory and neurological disorders. PDE4-IN-3 is primarily utilized to investigate the role of cAMP signaling pathways in various biological processes and potential therapeutic interventions. -
PDE5 Inhibitor
KD-027 is a potent inhibitor of Phosphodiesterase 5 (PDE5), which plays a crucial role in regulating cyclic nucleotide levels in various tissues. This compound demonstrates significant potential in research focused on endothelial dysfunction and hypertension. Its mechanism of action aids in the therapeutic exploration of cardiovascular diseases and related conditions. -
PDE IV Inhibitor
CDP-840 is a selective and orally active phosphodiesterase IV (PDE IV) inhibitor. This compound demonstrates significant inhibition of antigen-induced early and late-phase bronchoconstriction in conscious squirrel monkeys, indicating its potential use in respiratory research. CDP-840 may be useful for investigating therapeutic strategies for asthma and other allergic conditions through modulation of inflammatory pathways. -
PDE4 Inhibitor
HT-0712 is a selective inhibitor of Phosphodiesterase Type 4 (PDE4). This compound has been shown to enhance motor recovery and facilitate cortical reorganization following focal cortical ischemia, making it a valuable tool in neuropharmacology research. Its ability to modulate cAMP levels may provide insights into therapeutic strategies for stroke rehabilitation and related neurological disorders. -
PDE Inhibitor
Autotaxin-IN-5 is a potent inhibitor of autotaxin, primarily targeting phosphodiesterase (PDE) pathways. This compound demonstrates significant biological activity in modulating fibrosis-related processes, making it a valuable candidate for research in idiopathic pulmonary fibrosis. Its application in preclinical studies could provide insights into therapeutic approaches for lung fibrosis and related disorders. -
PDE4B1 Inhibitor
Phosphodiesterase-IN-3 is a potent inhibitor of phosphodiesterase 4B1, exhibiting an IC50 of less than 10 nM, while demonstrating moderate inhibition of PDE4D3 with an IC50 in the range of 10-100 nM. This compound is valuable for research into idiopathic pulmonary fibrosis, providing a tool for investigating PDE4B1-mediated pathways and their therapeutic potential in pulmonary diseases. -
Phosphodiesterase (PDE) Control
(-)-Pimobendan selectively targets phosphodiesterase (PDE), enhancing cyclic nucleotide signaling. This isomer exhibits a pronounced affinity for erythrocytes, leading to a significantly lower clearance rate compared to its counterpart. Notably, (-)-pimobendan demonstrates a 1.5-fold increase in contractile force in detergent-treated myocardial specimens from guinea pigs and dogs. These distinctive pharmacokinetic properties may provide unique advantages for its application in clinical settings, particularly in cardiac research and therapeutics. -
Phosphodiesterase (PDE)
Mardepodect succinate is a potent and selective inhibitor of phosphodiesterase 10A (PDE10A), demonstrating significant potential in the treatment of schizophrenia. This compound has been optimized to enhance its brain penetration and physicochemical properties, making it valuable for schizophrenia-related research applications. Its targeted mechanism may aid in the exploration of PDE10A's role in neuropsychiatric disorders. -
PDE-5 Inhibitor
Acetylvardenafil is a potent phosphodiesterase type 5 (PDE-5) inhibitor, serving as an analog of Vardenafil with an acetyl group replacing the sulfonyl group. This compound exhibits significant biological activity by facilitating the relaxation of smooth muscle tissue and increasing blood flow to the corpus cavernosum, making it a valuable tool in the study of erectile dysfunction (ED). Its mechanism can contribute to research aimed at understanding and developing therapies for erectile dysfunction and related conditions. -
PDE4 Inhibitor
PDE4-IN-5 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 3.1 nM. It demonstrates favorable skin permeability, making it particularly relevant for topical applications. This compound is primarily investigated for its potential anti-psoriasis effects and can be utilized in research focusing on inflammatory skin conditions and associated therapeutic strategies. -
PDE3/4 Inhibitor
(E/Z)-Ensifentrine is a dual inhibitor of phosphodiesterase 3 and 4 (PDE3/4). It exhibits significant bronchodilatory and anti-inflammatory effects, demonstrated in both in vitro and in vivo models. This compound is primarily utilized in research related to respiratory diseases, particularly for studying inflammation and airway obstruction mechanisms. -
PDE10A Inhibitor
JNJ-42396302 is a selective phosphodiesterase 10A (PDE10A) inhibitor that modulates intracellular signaling pathways involving cyclic nucleotides. This compound exhibits significant biological activity in the regulation of dopaminergic and glutamatergic systems, making it a valuable tool for investigating neurobiological processes. Research applications include studies focused on infertility and potential therapeutic interventions in neuropsychiatric disorders. -
Phosphodiesterase (PDE)
PDE5-IN-6c is a selective inhibitor of phosphodiesterase 5A1 (PDE5A1) with significant potential for Alzheimer's disease (AD) research. With an impressive in vitro IC50 of 0.056 nM, it demonstrates strong inhibitory activity. Additionally, PDE5-IN-6c features enhanced water solubility, making it a promising candidate for further drug development and investigation in neurodegenerative disease studies. -
Phosphodiesterase (PDE) Inhibitor
Palmitoylcholine chloride acts as an inhibitor of phosphodiesterase (PDE), particularly affecting the calcium-dependent hydrolysis of phosphatidylinositol. This compound helps to mitigate membrane stress by reducing enzyme activity, thereby influencing cellular signaling pathways. Palmitoylcholine chloride is valuable for research applications involving membrane dynamics and signal transduction. -
PDE3B Inhibitor
GSK4394835A is a reversible covalent inhibitor of phosphodiesterase 3B (PDE3B), exhibiting a pIC50 value of 6.2. This compound demonstrates significant efficacy in modulating cellular signaling pathways associated with cardiovascular diseases. GSK4394835A is a valuable tool for researchers investigating the role of PDE3B in cardiovascular disease mechanisms and potential therapeutic interventions. -
AR/PDE Inhibitor
ADORA2A/PDE4D-IN-1 is a dual inhibitor targeting the adenosine A2a receptor (ADORA2A) and phosphodiesterase 4D (PDE4D). This compound exhibits significant biological activity in modulating adenosine signaling and cyclic nucleotide levels. Its dual inhibitory mechanism makes it valuable for research applications focused on bronchial asthma and related respiratory conditions. -
PDE4 Inhibitor
PDE4-IN-16 is a selective inhibitor of phosphodiesterase 4 (PDE4), displaying an IC50 value of 3.61 μM. This compound is relevant for research in inflammatory diseases and central nervous system (CNS) disorders characterized by elevated cytokine levels. Its ability to modulate inflammatory pathways makes it a valuable tool for exploring therapeutic strategies in related conditions. -
PDE4 Inhibitor
KW-4490 is a selective inhibitor of phosphodiesterase 4 (PDE4), a key enzyme involved in the degradation of cyclic adenosine monophosphate (cAMP). This compound exhibits anti-inflammatory properties and is particularly relevant in studies of asthma and other inflammatory disorders. KW-4490 serves as a valuable tool for researchers investigating the modulation of immune responses and the potential therapeutic avenues in inflammatory diseases. -
PDE5 Inhibitor
(R)-Avanafil is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5), with an IC50 value of 5.2 nM. This compound is utilized in research pertaining to erectile dysfunction, offering insights into its pharmacological effects and potential therapeutic applications. Its specificity for PDE5 makes it a valuable tool for studying the modulation of cyclic nucleotide signaling pathways. -
PDE9 Inhibitor
(Rac)-Tovinontrine, also known as (Rac)-IMR-687, is a selective phosphodiesterase 9 (PDE9) inhibitor that enhances levels of cyclic guanosine monophosphate (cGMP). This compound is particularly relevant in the study of thalassemia, as it may play a role in modulating signaling pathways associated with erythropoiesis and vascular regulation. Its ability to influence cGMP levels makes it a valuable tool in various research applications related to cardiovascular diseases and hematological disorders. -
Phosphodiesterase (PDE) Inhibitor
PDE10A-IN-4 is a selective phosphodiesterase 10A (PDE10A) inhibitor. It primarily modulates intracellular signaling pathways through the inhibition of cyclic nucleotide degradation, which may have implications in the study of neuropsychiatric disorders, particularly schizophrenia. This compound is utilized in research to explore its potential role in cognitive and motor functions associated with PDE10A inhibition. -
PDE5 Inhibitor
PDE5-IN-42 is a potent and orally active phosphodiesterase type 5 (PDE5) inhibitor, demonstrating an IC50 of 0.04 nM. This compound exhibits selectivity over PDE6 and PDE11, making it a valuable tool in research focused on vascular smooth muscle relaxation and erectile dysfunction. Its effectiveness in modulating cGMP levels supports its potential applications in cardiovascular disease studies and related therapeutic explorations. -
PDE Inhibitor
Bemoradan is a selective inhibitor of canine phosphodiesterase (PDE) fraction III, exhibiting potent inotropic and vasodilatory effects. Its long-acting nature makes it a valuable tool in research related to congestive heart failure. Bemoradan facilitates the investigation of cardiac function and therapeutic interventions for heart conditions. -
PDE10A Inhibitor
PDM-042 is a selective inhibitor of phosphodiesterase 10A (PDE10A), demonstrating exceptional potency with IC50 values below 1 nM in both human and rat systems. It exhibits over 1000-fold selectivity against other phosphodiesterases, making it a valuable tool for investigating PDE10A's role in neurobiology. PDM-042 is particularly relevant for research into schizophrenia and related neurological disorders. -
PDE3 Inhibitor
Org-9935 is a selective phosphodiesterase 3 (PDE3) inhibitor with an IC50 of 50 nM. This compound has been shown to inhibit the maturation of oocytes in naturally selected dominant follicles in rhesus macaques. Additionally, Org-9935 enhances glucose-induced insulin secretion in isolated rat islets, with an EC50 of 20 μM, making it a valuable tool for research in reproductive biology and insulin signaling pathways. -
PDE3/PDE4 Inhibitor
PDE3/4-IN-2 is a potent dual inhibitor of phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4), demonstrating IC50 values of 0.13 nM for PDE3A and 50 nM for PDE4B1. This compound is valuable in the investigation of diseases related to phosphodiesterase dysregulation, including asthma, chronic obstructive pulmonary disease, sepsis, and nephritis. Its selective inhibition profile makes it a significant tool for exploring therapeutic strategies in these conditions. -
PDE10A Inhibitor
TC-E 5005 is a highly selective inhibitor of the phosphodiesterase 10A (PDE10A) enzyme, exhibiting IC50 values of 7.28 nM for PDE10A, while demonstrating significantly higher values for PDE2A, 11A, 5A, 7B, and 3A. This compound effectively inhibits adrenergic and neurogenic smooth muscle contractions in human prostate tissues, making it a valuable tool for studying PDE10A's role in smooth muscle physiology and potential therapeutic applications in urological disorders.
