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Phosphodiesterase (PDE) Inhibitor
Gisadenafil besylate is a selective phosphodiesterase 5 (PDE5) inhibitor that effectively prevents the degradation of cyclic guanosine monophosphate (cGMP), exhibiting an IC50 of 3.6 nM. This compound is primarily utilized in research related to cardiovascular health and sexual dysfunction, providing insights into the mechanisms regulating vascular smooth muscle relaxation and nitric oxide signaling pathways. Its specificity and oral bioavailability make it a valuable tool for investigating PDE5-related biological processes and therapeutic potential. -
PDE 10 Inhibitor
PDE10-IN-5 is a potent inhibitor of phosphodiesterase 10 (PDE 10), targeting the regulation of intracellular signaling pathways by modulating cyclic nucleotide levels. This compound demonstrates significant biological activity in the central nervous system and is valuable for research on various CNS disorders, including schizophrenia and movement-related diseases. Its specificity for PDE 10 makes it an important tool for elucidating the role of this enzyme in neurodegenerative conditions and potential therapeutic interventions. -
PDE Inhibitor
PF-8380 hydrochloride is a potent phosphodiesterase (PDE) inhibitor, demonstrating an IC50 of 2.8 nM in isolated enzyme assays and 101 nM in human whole blood. This compound is primarily used in research to investigate the role of autotaxin in various biological processes, including inflammation and cancer progression. PF-8380 hydrochloride serves as an important tool for studying the modulation of lysolipid signaling pathways and potential therapeutic interventions targeting autotaxin-related diseases. -
PDE4 Inhibitor
Dovramilast is an orally active phosphodiesterase 4 (PDE4) inhibitor that effectively reduces inflammatory responses. It enhances isoniazid-mediated bacillary clearance from the lungs, making it a valuable adjunct in tuberculosis (TB) research. This compound facilitates studies aimed at understanding and improving therapeutic strategies for TB. -
PDE5 Inhibitor
ent-Tadalafil is the inactive cis-enantiomer of the potent phosphodiesterase type 5 (PDE5) inhibitor (6R,12aS), which exhibits an IC50 of 0.090 μM. While ent-Tadalafil does not demonstrate significant biological activity, its characterization is essential for understanding the structure-activity relationship of PDE5 inhibitors. This compound serves as a reference material in biochemical research and may aid in the evaluation of enantiomeric effects on PDE5 inhibition. -
PDE4 Inhibitor
Tilivapram (AVE8112) is a potent phosphodiesterase 4 (PDE4) inhibitor that demonstrates procognitive effects and enhances processing and psychomotor speeds in vivo. Its oral administration may be associated with dose-related side effects such as nausea and dizziness. However, transdermal delivery offers a controlled elevation of plasma concentrations, minimizing gastrointestinal discomfort and dizziness. Tilivapram is particularly relevant for research into neuropsychiatric disorders and cognitive enhancement. -
PDE9 Inhibitor
(S)-C33 is a highly selective inhibitor of phosphodiesterase-9 (PDE9) with an IC50 value of 11 nM. This compound is primarily utilized in research focused on central nervous system disorders and diabetes. Its significant inhibitory action on PDE9 makes it a valuable tool for investigating the therapeutic potential in these areas. -
PDE5 Inhibitor
Yonkenafil is a potent phosphodiesterase 5 (PDE5) inhibitor that has demonstrated efficacy in reducing cerebral infarction, alleviating neurological deficits, and minimizing edema and neuronal damage in affected areas. Its ability to enhance cognitive function through modulation of neurogenesis indicates potential therapeutic applications in neurodegenerative disorders, including Alzheimer's disease. Researchers may utilize Yonkenafil to investigate its effects on cognitive enhancement and neuroprotection in various experimental models. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a dissociation constant (KD) of 203 pM. This compound effectively disrupts the function of the KRas signaling pathway, making it a valuable tool for investigating tumor biology and related therapeutic strategies. Deltasonamide 1 holds promise for advancing research in cancer treatment and understanding related pathophysiological mechanisms. -
PDE4D Inhibitor
PDE4-IN-24 is a highly potent inhibitor of phosphodiesterase 4D (PDE4D) with an IC50 value of 0.57 nM, demonstrating over 4100-fold selectivity against other phosphodiesterase families. This compound is relevant to research on inflammatory diseases, as it modulates cyclic nucleotide signaling pathways, which are critical for controlling inflammation and immune responses. Its specificity and activity make PDE4-IN-24 a valuable tool for studying the role of PDE4D in various biological contexts. -
PDE5 Inhibitor
MBCQ is a selective phosphodiesterase type 5 (PDE5) inhibitor with a potent IC50 of 19 nM. It demonstrates high specificity for cGMP-specific PDE5, exhibiting minimal activity against other phosphodiesterase isozymes (IC50s > 100 μM). MBCQ facilitates the dilation of coronary arteries, making it a valuable reagent for research focused on vascular biology and cardiovascular therapeutics. -
Phosphodiesterase (PDE) Inhibitor
Prinoxodan is a selective phosphodiesterase (PDE) inhibitor that modulates intracellular cAMP levels. This compound has been shown to enhance biological activity in various cellular models, making it a valuable tool for studying signaling pathways involved in cardiovascular and neurological conditions. Prinoxodan is utilized in research applications focused on the regulation of smooth muscle relaxation and the modulation of neurotransmitter release. -
PDE5 Inhibitor
(6S,12aR)-Tadalafil is a potent phosphodiesterase type 5 (PDE5) inhibitor, exhibiting an IC50 value of 5 nM. This compound is known to lower blood pressure and is utilized in research investigating cardiovascular effects, erectile dysfunction therapies, and other related conditions. Its strong inhibitory action on PDE5 makes it a valuable tool for studying nitric oxide signaling pathways and cGMP levels in various biological systems. -
PDE5 Inhibitor
Carbodenafil is a phosphodiesterase type 5 (PDE5) inhibitor, structurally related to Sildenafil (UK-92480). It effectively inhibits PDE5 with an IC50 of 5.22 nM, leading to increased levels of cyclic GMP and subsequent vasodilation. This compound is primarily utilized in research settings to explore mechanisms associated with erectile dysfunction and pulmonary hypertension. -
PDE Inhibitor
Acetildenafil is a phosphodiesterase type 5 (PDE5) inhibitor that serves as an analogue of Sildenafil. It is primarily used in research to investigate its biological activities related to vasodilation and erectile function. Additionally, Acetildenafil is of interest in studies focusing on its potential therapeutic applications derived from herbal sources. -
PDE5 Inhibitor
Thioquinapiperifil dihydrochloride is a potent and selective non-competitive inhibitor of phosphodiesterase-5 (PDE-5), with an IC50 of 0.074 nM. This compound is primarily utilized in research related to sexual enhancement and erectile function, contributing to studies on the modulation of signaling pathways associated with vasodilation. Its high selectivity and activity make it a valuable reagent for investigating PDE-5's role in various physiological and pathological processes. -
PDE2 Inhibitor
Hcyb1 is a highly selective inhibitor of phosphodiesterase 2 (PDE2), demonstrating an IC50 of 0.57 μM against PDE2A and over 250-fold selectivity towards other members of the phosphodiesterase family. This compound is characterized by its neuroprotective and antidepressant-like effects, which are likely mediated through the cAMP/cGMP-CREB-BDNF signaling pathway. Hcyb1 is a valuable tool for research applications focusing on neurobiology and mood disorders. -
PDE3 Inhibitor
Siguazodan is a selective phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. It effectively increases cyclic adenosine monophosphate (cAMP) levels in intact platelets, demonstrating an EC50 of 18.88 μM. Additionally, Siguazodan inhibits phenylephrine-induced serotonin (5-HT) release with an IC50 of 4.2 μM, making it a valuable tool for research into cardiovascular and platelet function. -
PDE4B Inhibitor
PDE4B-IN-3 is a potent inhibitor of phosphodiesterase 4B (PDE4B), exhibiting an IC50 of 0.94 μM. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for studies aimed at understanding inflammatory pathways and developing novel therapeutic strategies. It is suitable for use in research applications investigating the role of PDE4B in various diseases, including chronic inflammatory conditions. -
PDE Inhibitor
1-Phenyl-3,4-dihydroisoquinoline is a phosphodiesterase (PDE) inhibitor that demonstrates significant activity in modulating cyclic nucleotide levels. This compound has been investigated for its potential applications in various therapeutic areas, including cardiovascular and neurological research. Its ability to inhibit PDE may provide insights into cellular signaling pathways and support the development of novel pharmacological strategies. -
K-Ras-PDEδ Inhibitor
K-Ras-PDEδ-IN-1 is a selective inhibitor of K-Ras-PDEδ, designed for high-affinity binding to the farnesyl binding pocket of PDEδ with a dissociation constant (Kd) of 8 nM. This compound effectively disrupts the interaction between K-Ras and PDEδ, playing a crucial role in modulating K-Ras signaling pathways. It is valuable for research applications focused on cancer biology and therapeutic strategies targeting K-Ras-driven malignancies. -
PDE4 Inhibitor
LEO 39652 is a potent dual-selective inhibitor of phosphodiesterase type 4 (PDE4), exhibiting IC50 values of 1.2 nM for PDE4A and PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM. This compound is primarily utilized in topical research for atopic dermatitis (AD), making it valuable for studies aimed at understanding and developing treatments for this condition. -
PDE4 Inhibitor
Lirimilast is a selective and orally active phosphodiesterase-4 (PDE4) inhibitor, exhibiting an IC50 of 49 nM. This compound demonstrates significant anti-inflammatory activity, making it a valuable candidate for therapeutic applications in asthma and chronic obstructive pulmonary disease (COPD). Research utilizing Lirimilast may provide insights into the modulation of inflammatory responses in respiratory conditions. -
PDE2A Inhibitor
PDE2A-IN-3 is a selective inhibitor of phosphodiesterase 2A (PDE2A), exhibiting an IC50 of 69 nM for PDE2A and 1762 nM for PDE10. This compound is valuable for investigating the role of PDE2A in neurological and psychiatric disorders, providing insights into potential therapeutic interventions. Its specificity for PDE2A makes it an essential tool for researchers studying the modulation of cyclic nucleotide signaling pathways associated with these conditions. -
Phosphodiesterase (PDE) Inhibitor
Theodrenaline hydrochloride is a selective phosphodiesterase (PDE) inhibitor that enhances cardiac contractility and improves hemodynamic performance. It exhibits potent cardiac stimulant properties and serves as an effective anti-hypotensive agent, particularly when used in conjunction with Cafedrine. This reagent is valuable for research applications focused on cardiovascular pharmacology and the mechanisms of blood pressure regulation. -
PDE4 Inhibitor
FCPR03 is a highly selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating IC50 values of 60 nM, 31 nM, and 47 nM against the PDE4 catalytic domain, PDE4B1, and PDE4D7, respectively. With over 2100-fold selectivity against other phosphodiesterases (PDE1-3 and PDE5-11), FCPR03 exhibits significant anti-inflammatory, neuroprotective, and antidepressant-like properties. This compound is pivotal for research applications targeting inflammatory and neurodegenerative diseases, as well as mood disorders. -
Phosphodiesterase (PDE) Inhibitor
Theodrenaline is a phosphodiesterase (PDE) inhibitor that functions primarily as a cardiac stimulant. It enhances cardiac contractility and supports blood pressure regulation, making it valuable in the treatment of hypotension. This compound is utilized in cardiovascular research to investigate heart function and the modulation of vascular tone. -
PDE 4 Inhibitor
RS-25344 hydrochloride is a highly selective inhibitor of phosphodiesterase 4 (PDE 4), exhibiting an IC50 of 0.28 nM in human lymphocytes. The compound demonstrates minimal activity against PDE I, II, and III, with IC50 values exceeding 100 μM. RS-25344 hydrochloride possesses significant anti-inflammatory properties and has been shown to enhance memory and cognitive functions, as well as exhibiting potential antineoplastic effects. This makes it a valuable tool for research in areas related to inflammation, neurobiology, and cancer. -
PDE4 Inhibitor
Atizoram is a selective phosphodiesterase 4 (PDE4) inhibitor that elevates cyclic AMP levels while simultaneously reducing tumor necrosis factor-alpha (TNFα) production in murine models. This compound possesses significant anti-inflammatory properties, making it a valuable tool for investigating inflammatory pathways and potential therapeutic strategies in conditions associated with dysregulated TNFα expression. Atizoram is applicable in research exploring the roles of PDE4 in various biological systems and diseases. -
PDE3 Inhibitor
Motapizone is a selective phosphodiesterase 3 (PDE3) inhibitor. It has been shown to moderately inhibit cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages, highlighting its potential anti-inflammatory properties. Additionally, Motapizone enhances intracellular cyclic AMP levels, thereby preventing human platelet aggregation. This compound is valuable for research in inflammation and platelet physiology. -
PDE4 Inhibitor
PDE4-IN-4 is a selective inhibitor of phosphodiesterase 4 (PDE4) with a pIC50 of 8.8, as well as a dual antagonist of the M3 muscarinic receptor with a pIC50 of 10.2. This compound exhibits significant biological activity in modulating cyclic nucleotide levels, making it valuable for research related to pulmonary diseases. Its dual action allows for exploration of therapeutic pathways in respiratory disorders, providing insights into potential treatment strategies. -
PDE3 Inhibitor
Quazinone is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3), targeting the catalytic activity of this enzyme. It effectively inhibits the phosphorylation of p42/p44 MAP kinase, leading to decreased mitogenic signaling. Quazinone exhibits antimitogenic effects and is useful in studies related to cell proliferation and signal transduction pathways. -
PDE4 Inhibitor
MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor that enhances intracellular cyclic adenosine monophosphate (cAMP) levels by blocking PDE4 activity. This elevation in cAMP activates protein kinase A (PKA), which subsequently inhibits inflammatory cell activity and promotes relaxation of airway smooth muscle. MK-0873 is suitable for research applications related to chronic obstructive pulmonary disease (COPD), providing insights into potential therapeutic strategies for respiratory conditions characterized by inflammation and airway constriction. -
PDE10A Inhibitor
PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A), displaying an IC50 of 4.6 nM and an ED50 of 13 mg/kg. This compound influences patterns of brain glucose metabolism, potentially serving as a translational biomarker in neurological research. PQ-10 is particularly valuable for investigating psychiatric disorders, including schizophrenia, and provides insights into the underlying mechanisms of these conditions. -
PDE4 Inhibitor
MK-0952 is a selective phosphodiesterase 4 (PDE4) inhibitor, characterized by an IC50 value of 0.53 nM. This compound exhibits potential therapeutic effects for disorders associated with PDE4 modulation, particularly in the context of Alzheimer's disease research. MK-0952 provides a valuable tool for studying the role of PDE4 in cognitive function and neurodegenerative diseases. -
PDE4 Inhibitor
(S)-Gebr32a is a selective phosphodiesterase 4 (PDE4) inhibitor, demonstrating IC50 values of 19.5 µM for PDE4 cat and 2.1 µM for PDE4D3. It exhibits significant biological activity by modulating intracellular cyclic AMP levels, making it a valuable tool for investigating inflammatory processes and neurodegenerative diseases. This compound is suitable for research applications focused on the role of PDE4 in various cellular signaling pathways. -
PDE5 Inhibitor
Yonkenafil hydrochloride is a selective phosphodiesterase 5 (PDE5) inhibitor, known for its neuroprotective properties. It effectively reduces cerebral infarction, neurological deficits, edema, and neuronal damage following ischemic events. Additionally, Yonkenafil may enhance cognitive function through modulation of neurogenesis, suggesting its potential therapeutic applications in neurodegenerative conditions such as Alzheimer's disease. -
Phosphodiesterase (PDE) Inhibitor
PDE10-IN-1 is a selective inhibitor of phosphodiesterase 10 (PDE10), which plays a crucial role in regulating cyclic nucleotide levels in the central nervous system. This compound has demonstrated potential in modulating dopaminergic signaling and offers promise for investigating therapeutic strategies for central nervous system and metabolic disorders. Its mechanism of action may provide insights into the treatment of various neuropsychiatric conditions. -
PDE5 Inhibitor
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor that disrupts the hydrolysis of cyclic guanosine monophosphate (cGMP) in a competitive manner, with an IC50 value of 0.23 nM. This compound also demonstrates inhibitory effects on PDE6 (IC50=56 nM) while displaying low potency against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 is valuable for research focusing on the nitric oxide (NO)/cGMP signaling pathway, with potential applications in cardiovascular and erectile dysfunction studies. -
PDE4 Inhibitor
Denbufylline is a potent phosphodiesterase-4 (PDE4) inhibitor that effectively prevents the degradation of intracellular cyclic adenosine monophosphate (cAMP). This inhibition leads to increased levels of cAMP, which plays a crucial role in regulating various cellular functions. Denbufylline is primarily utilized in research related to chronic obstructive pulmonary disease (COPD), asthma, and other inflammatory conditions, making it a valuable tool for understanding these complex diseases. -
PDE-5 Inhibitor
Aildenafil, also known as Methisosildenafil, is a potent inhibitor of phosphodiesterase type 5 (PDE-5), which facilitates vasodilation by elevating nitric oxide (NO) levels. This compound is primarily utilized in research exploring cardiovascular effects and conditions related to erectile dysfunction. Its ability to enhance blood flow through the modulation of cyclic guanosine monophosphate (cGMP) levels makes it a valuable tool for studying vascular physiology and pharmacology. -
PDE4 Inhibitor
PF-07038124 is a potent phosphodiesterase 4 (PDE4) inhibitor, exhibiting an IC50 of 0.5 nM for the PDE4B2 isoform. It demonstrates significant inhibitory activity against pro-inflammatory cytokines, including IL-13 (IC50 = 125 nM), IL-4 (IC50 = 4.1 nM), and IFN-γ (IC50 = 1.06 nM). This compound is valuable for research applications related to atopic dermatitis and plaque psoriasis, offering insights into therapeutic strategies for managing these inflammatory conditions. -
PDE4 Inhibitor
LASSBio-1632 is a selective phosphodiesterase 4 (PDE4) inhibitor, specifically targeting the PDE4A and PDE4D isoenzymes. This compound demonstrates significant anti-asthmatic properties by attenuating airway hyper-reactivity and inhibiting TNF-α production in lung tissue. Additionally, LASSBio-1632 exhibits high permeability across the blood-brain barrier, facilitating its potential use in various research applications related to respiratory conditions. -
PDE1 Inhibitor
PF-04822163 is a selective phosphodiesterase 1 (PDE1) inhibitor that effectively crosses the blood-brain barrier, exhibiting IC50 values of 2 nM for PDE1A, 2.4 nM for PDE1B, and 7 nM for PDE1C. This compound demonstrates significant potential for modulating intracellular signaling pathways, making it valuable in the study of neurological disorders such as attention deficit hyperactivity disorder and Parkinson's disease. Its potency and selectivity support its use in preclinical research efforts aimed at elucidating the role of PDE1 in these conditions. -
PDE5 Inhibitor
Vardenafil dihydrochloride is a selective inhibitor of phosphodiesterase-5 (PDE5), demonstrating a potent inhibitory effect with an IC50 of 0.7 nM. It also exhibits inhibition of PDE1 and PDE6 with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4. By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil dihydrochloride elevates cGMP levels, making it a valuable tool for studying conditions such as erectile dysfunction, hepatitis, and diabetes. -
PDE-5 Inhibitor
Avanafil dibenzenesulfonate is a selective phosphodiesterase-5 (PDE-5) inhibitor with a potent IC50 of 5.2 nM for PDE-5, demonstrating significant selectivity against other PDE isoforms. This compound activates the NO/cGMP/PKG signaling pathway, ultimately leading to reduced bone mineral density loss, alleviation of bone atrophy, and decreased oxidative stress. Avanafil dibenzenesulfonate is suitable for research applications related to erectile dysfunction and osteoporosis, where modulation of cGMP levels is crucial. -
TbrPDEB1 Inhibitor
NPD-1335 is an inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1), demonstrating submicromolar efficacy against T. brucei parasites. This compound enhances intracellular cAMP levels, leading to cell cycle disruption and apoptosis in the target cells. Additionally, NPD-1335 features an alkyne moiety, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, thus expanding its utility in various research applications. -
PDE5 Inhibitor
TPN729MA is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. This compound plays a critical role in regulating erectile function and is suitable for research applications related to erectile dysfunction. Its potent inhibitory effect on PDE5 makes it a valuable tool for studying the underlying mechanisms of this condition. -
PDE5 Inhibitor
TPN729 is a selective inhibitor of phosphodiesterase type 5 (PDE5), exhibiting an IC50 value of 2.28 nM. This compound is primarily involved in modulating erectile function and serves as a valuable tool in the research of erectile dysfunction. Its high potency and specificity make it suitable for investigating PDE5's role in various physiological and pathological processes. -
PDE Inhibitor
Autotaxin-IN-4 is a potent inhibitor of autotaxin, targeting the enzyme responsible for lysophosphatidic acid production. This compound exhibits promising biological activity in the modulation of fibrosis processes, making it a candidate for research in conditions such as idiopathic pulmonary fibrosis. It serves as a valuable tool for studies aimed at understanding the role of autotaxin in fibrotic diseases and exploring therapeutic interventions.

