pdeδ

PDE IV-IN-1 is a potent phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory activity for the treatment of asthma, chronic obstructive pulmonary disease and other inflammatory diseases, and is a potential compound for the study of depression.

PDE-I2 is a parasite schizogony inhibitor.

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ that binds to the farnesyl binding pocket of PDEδ (Kd of 8 nM).

ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate, also known as EAPT, is a potent and selective PDE4 inhibitor that regulates intracellular cyclic adenosine monophosphate (cAMP) levels. It has been used in a variety of scientific applications, including the study of cAMP-mediated signaling pathways, and has potential as a therapeutic agent for the treatment of inflammatory and immune-related diseases.

PDE9-IN-1 is a selective and orally bioavailable Inhibitor of PDE9A(IC50 of 8.7 nM).

KRAS4b-PDEδ stabilizer C19 is a stabilizer of the KRAS4b-PDEδ complex which decreases the proliferation of colorectal cancer cells, and increases apoptosis via decreased activation of oncogenic KRAS4b signaling.

PDE1-IN-7 (Compound 13h), with an IC50 value of 10 nM, selectively inhibits bPDE1. This compound demonstrates significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model and is useful for research purposes in studying liver fibrosis [1].

PDE4-IN-13 is a phosphodiesterase 4 (PDE4) inhibitor exhibiting anti-inflammatory and antioxidant activities, with an half maximal inhibitory concentration (IC50) value of 1.56 μM. It is used in the research of chronic obstructive pulmonary disease (COPD) [1].

PDE4-IN-9 (Compound 5j) is a potent PDE4 inhibitor with an IC50 value of 1.4 μM against PDE4 in vitro enzyme assays, which is lower than the 2.0 μM of parent rolipram, and demonstrates good in vivo activity in LPS-induced animal models of asthma COPD and sepsis [1].

PDE7-IN-3 (Example 2) serves as an inhibitor of phosphodiesterase PDE7 and exhibits potential analgesic properties. It is applicable in the research of various pain types including inflammatory, neuropathic, visceral, and nociceptive pain [1].

PDE5-IN-10 (compound 4b), a potent phosphodiesterase type 5 (PDE5) inhibitor, exhibits an effective half-maximal inhibitory concentration (IC50) of 20 nM, enhanced in vitro microsomal stability (t 1/2 = 44.6 min), and excellent efficacy in restoring long-term potentiation, making it suitable for Alzheimer’s disease (AD) research [1].

PDE4-IN-14 (Compound 1) is a phosphodiesterase 4 (PDE4) inhibitor used in research on PDE4-related diseases, such as inflammatory and immune disorders, cancer, and metabolic diseases [1].

PDE4B-IN-3 is a potent PDE4B inhibitor (IC50: 0.94 μM) with anti-inflammatory effects.

PDE5-IN-6c is a potent and selective inhibitor of PDE5A1.

PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor with an IC50 of 7.01 μM for PDE4B, demonstrating selectivity, microsomal stability, TNF-α inhibition, and no major toxicities in vitro [1].

PDE4-IN-8 (Example 5) is a potent Phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 0.93 nM for PDE4B2. However, it has minimal effects on IL13, IL4, and IFNy, with IC50 values of 4.04 nM, 36.33 nM, and 2394 nM, respectively [1].

PDE5-IN-11 is a potent PDE5 inhibitor with an IC50 of 40 nM and displays inhibitory activity against PDE4 and PDE6 with IC50 values of 1.78 μM and 0.09 μM, respectively [1].

PDE4B-IN-2 (A 33) is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.

PDE7-IN-2 is an inhibitor of phosphodiesterase 7 (IC50 = 2.1 µM) and can be used in Parkinson's disease studies.

PDE5/HDAC-IN-1 is a potent inhibitor of phosphodiesterase 5 (PDE5) and HDAC, with IC50 values of 46.3 nM and 14.5 nM, respectively.

PDE4-IN-6 is a safe, potent and moderately selective inhibitor of PDE4, acting on PDE4B (IC50: 0.125 μM) and PDE4D (IC50: 0.43 μM). PDE4-IN-6 is able to down-regulate TNF-α and IL-6 expression levels, exhibits anti-inflammatory and anti-arthritic effects, and has potent immunomodulatory activity. PDE4-IN-6 has potential for anti-rheumatoid arthritis studies.

PDE2 PDE10-IN-1 is an inhibitor of phosphodiesterase 2 (PDE2) and PDE10, with IC50 values of 29 nM and 480 nM, respectively.

PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).

PDE5-IN-42 is a selective inhibitor of second-generation phosphodiesterase type 5 (PDE5).

PDE4-IN-4 is a compound acting as both a potent M3 antagonist (p IC 50 = 10.2) and a PDE4 inhibitor (p IC 50 = 8.8), designed for inhalation-based treatment of pulmonary diseases.

Compound 8a (PDE10A-IN-3) serves as an inhibitor of phosphodiesterase 10A (PDE10A) and is utilized in schizophrenia research [1].

PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor with an IC50 of 15 nM, exhibiting anti-inflammatory properties through the inhibition of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 expression induced by LPS. It has demonstrated efficacy in mitigating inflammatory bowel disease (IBD) symptoms in a dextran sodium sulfate (DSS)-induced colitis mouse model, suggesting its potential utility for IBD research [1].

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

Compound 22, a 5-hydroxynitrile rubber 7 receptor antagonist (5-HT1A Ki=8 nm, Kb=0.04 nm; 5-nitrile rubber 7K I=451 nm, Kb=460 nm), exhibits inhibitory activity against PDE4B/PDE7A (PDE4B IC50=80.4 μM; PDE7A IC50=151.3 μM). It demonstrates significant passive biofilm penetration capabilities and high metabolic stability in vitro. Pharmacological assessment has revealed precognitive and antidepressant effects in rat behavioral tests, highlighting its potential therapeutic applications.

PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1).

PDE11-IN-1 is a PDE11 inhibitor used for adrenal insufficiency research [1].

PDE5-IN-4, a phosphodiesterase 5 (PDE5) inhibitor, is utilized in research concerning acute myocardial infarction and reperfusion-related damage, gastrointestinal diseases, diabetic complications, and liver failure.

PDE4-IN-3 is a newly developed oral compound that acts as a potent inhibitor of the enzyme phosphodiesterase 4 (PDE4), displaying a high affinity for inhibition with an IC50 value of 4.2 nM.

PDE4-IN-11 is a potent phosphodiesterase isoenzyme 4 (PDE4) inhibitor, exhibiting remarkable bronchodilatory and anti-inflammatory characteristics. It is specifically designed for studying obstructive or inflammatory airway diseases [1] [2] [3].

PDE11A4-IN-1 (compound 23b) is a potent, selective inhibitor of PDE11A4 with an IC50 of 12 nM, demonstrating high selectivity against PDE1, PDE2, PDE7, PDE8, and PDE9 [1].

PDE1-IN-6 (compound 6c) functions as a highly selective PDE1 inhibitor, exhibiting an IC 50 value of 7.5 nM. It notably inhibits proliferation and induces apoptosis in acute myelogenous leukemia cells [1].

PDE2A-IN-1 is a phosphodiesterase 2A (PDE2A) inhibitor with an IC50 value of 1.3 nM.

PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5 (IC50 of 0.31 nM).

PDE5-IN-5 is a selective inhibitor of phosphodiesterase 5 (PDE5) (IC50: 2.0 nM).

PDE12-IN-1 is a powerful and specific inhibitor of PDE12, exhibiting a pIC 50 value of 9.1 for enzyme inhibition. It effectively enhances levels of 2′,5′-linked adenylate polymers (2-5A), with a pEC 50 value of 7.7. Additionally, PDE12-IN-1 demonstrates antiviral activity.

PDE5-IN-3 (compound 11j) is a potent inhibitor of PDE5 (IC50: 1.57 nM) and has a moderate inhibitory effect on EGFR (IC50: 5.827 μM). It markedly inhibits the Wnt β-catenin pathway (IC50: 1286.96 ng mL), induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells, and exhibits significant antitumor effects.

AChE PDE4-IN-1 (compound 12c) is a highly effective and specific dual inhibitor of PDE4 and AChE, with IC50 values of 0.28 μM for AChE and 1.88 μM for PDE4D. This compound shows notable potential in reducing neuroinflammation associated with Alzheimer's disease research [1].

PDE4 inhibitor intermediate 1 is a PDE4 inhibitor synthesis intermediate.

PDE10A-IN-8 is a potent inhibitor of PDE10A.

PDE5-IN-9 inhibits Phosphodiesterase PDE1c and is used to treat hypertension, heart failure, myocardial infarction, kidney failure, asthma, bronchitis, and dementia.