Catalog No.
Product Name
Application
Product Information
Citations
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PDE-4 inhibitor
Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM. -
PDE inhibitor
Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM. -
dual PDE7/GSK-3 inhibitor
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). -
PDE12 inhibitor
PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity. -
TDP1 inhibitor
TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM. -
autotaxin inhibitor
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain. -
ATX inhibitor
Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM. -
PDE5 inhibitor
Lodenafil carbonate, a dimer that acts as a prodrug delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED). -
PDE-4 inhibitor
WAY127093B racemate is the racemate of WAY127093B. WAY127093B is a novel, orallyactive phosphodiesterase IV inhibitor in guinea pigs and rats. -
PDE Inhibitor
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. -
PDE5 inhibitor
Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension. -
PDE3 inhibitor
Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor. -
PDE9 inhibitor
BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor. -
PDE-5 inhibitor
Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction. -
PDE3 inhibitor
Fosphenytoin Sodium is the sodium salt form of fosphenytoin, a prodrug that is hydrolyzed to the anticonvulsant phenytoin. It is an PDE3 (phosphodiesterase 3) inhibitor. -
Calcium Sensitiser
OR-1896 is a potent calcium sensitizer and active metabolite of Levosimendan, primarily targeting phosphodiesterase (PDE) III isoforms. It exhibits significant vasodilatory effects and can activate ATP-sensitive potassium channels, enhancing calcium sensitivity. OR-1896 has been shown to reduce cardiomyocyte apoptosis, alleviate cardiac remodeling, and mitigate myocardial inflammation, making it valuable for research in cardiovascular disease therapies. -
PDEIII Inhibitor
Anagrelide is a potent phosphodiesterase type III (PDE3) inhibitor with an IC50 of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and attenuates megakaryocytopoiesis in the bone marrow. Additionally, Anagrelide demonstrates the capacity to reduce proliferation and promote apoptosis in gastrointestinal stromal tumor (GIST) cells in vitro. Its primary application includes functioning as a platelet-lowering agent with significant antithrombopoietic properties. -
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. -
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. -
PDE4/7 Inhibitor
BC-54 is a selective inhibitor of phosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7). It exhibits potent anti-inflammatory effects and can induce apoptosis in cancer cells, making it a valuable tool for research focused on cancer and inflammation. BC-54 is particularly relevant in studies investigating chronic lymphocytic leukemia and other conditions associated with these pathways. -
PDE4 Inhibitor
CC-3052 is a selective phosphodiesterase 4 (PDE4) inhibitor exhibiting immunomodulatory properties. It effectively reduces neutrophil apoptosis in HIV-positive contexts, highlighting its potential in the study of HIV-related diseases. This compound serves as a valuable tool for researchers investigating the modulation of immune responses in viral infections. -
PDE5 Inhibitor
PDE5-IN-3 is a potent phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 of 1.57 nM. In addition to its primary mechanism, PDE5-IN-3 demonstrates moderate inhibition of epidermal growth factor receptor (EGFR) with an IC50 of 5.827 µM and significantly affects the Wnt/β-catenin signaling pathway with an IC50 of 1286.96 ng/mL. This compound has been shown to induce the intrinsic apoptotic mitochondrial pathway in HepG2 cells and displays strong antitumor activity, making it valuable for cancer research applications. -
PDE5/HDAC Inhibitor
PDE5/HDAC-IN-1 is a dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) with IC50 values of 46.3 nM and 14.5 nM, respectively. This compound has demonstrated the capability to induce cell apoptosis and exhibits significant anticancer activities. PDE5/HDAC-IN-1 is a valuable tool for research in cancer therapeutics and epigenetic modulation. -
PDEIII Inhibitor
Anagrelide hydrochloride monohydrate is a selective inhibitor of phosphodiesterase type III (PDE3), with an IC50 value of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and reduces bone marrow megakaryocytopoiesis. Additionally, Anagrelide hydrochloride monohydrate demonstrates the capability to decrease cell proliferation and induce apoptosis in gastrointestinal stromal tumor (GIST) cells in vitro, making it relevant for research in hematology and oncology. Its platelet-lowering properties contribute to its antithrombopoietic effects. -
PDE4 Inhibitor
GPD-1116 is a potent inhibitor of Phosphodiesterase (PDE) 4 and PDE1, demonstrating oral bioactivity. This compound effectively reduces smoke-induced apoptosis in lung cells, making it relevant for respiratory research. GPD-1116 shows promise in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary hypertension, supporting its potential therapeutic applications in pulmonary disorders. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
PDE4 Inhibitor
Morcamilast is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, exhibiting IC50 values of 1.28 nM for PDE4A1A, 2.33 nM for PDE4B1, and 1.63 nM for PDE4D2. This compound demonstrates significant anti-inflammatory activity by inhibiting the lipopolysaccharide (LPS)-induced release of pro-inflammatory cytokines, including TNF-α, IL-12/23p40, IL-23, and IL-17A in human peripheral blood mononuclear cells (PBMCs) and T cells. Morcamilast also exhibits antipruritic effects, making it a valuable tool for investigating psoriasis, atopic dermatitis, and various other inflammatory disorders. -
PDE1C Inhibitor
PDE1-IN-9 is a selective inhibitor of phosphodiesterase 1 (PDE1), demonstrating an IC50 of 11 nM for PDE1C. This compound significantly reduces the mRNA expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α, as well as iNOS, while inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 also showcases favorable metabolic stability in rat liver microsomes, making it a valuable tool for studying PDE1-related pathways and inflammatory responses. -
PDE4 Inhibitor
Mesopram is a selective phosphodiesterase (PDE) 4 inhibitor that effectively reduces the synthesis of pro-inflammatory cytokines, including TNF-α and IFN-γ. This compound has shown efficacy in alleviating Dextran sulfate sodium (DSS)-induced colitis in murine models, making it a valuable tool for research in chronic inflammatory diseases. Mesopram can be employed to investigate therapeutic strategies aimed at modulating inflammatory responses. -
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. -
Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. -
PDE3 inhibitor
Cilostazol is a selective inhibitor of 3-type phosphodiesterase (PDE3) with therapeutic focus on cAMP.
