pde-4-in-4

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.

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.

Zardaverine (BY 290) is an orally available, selective and potent PDE3 4 inhibitor with bronchodilator activity and anti-hepatocarcinogenic activity.Zardaverine's action in platelets is mediated by PDE III isoenzymes and can be used in studies of acute renal failure and chronic airflow obstruction.

Compound 4p (PDE4B D-IN-4) is an effective inhibitor of PDE-4B and PDE-4D, with IC50 values of 5.50 nM and 6.81 nM respectively. Following the administration of PDE4B D-IN-4, intracellular cAMP levels are elevated.

GPD-1116 is an orally active inhibitor of phosphodiesterase (PDE)4 and PDE1. The compound effectively reduces smoke-induced apoptosis in lung cells. Additionally, GPD-1116 has shown efficacy in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary arterial hypertension.

Eggmanone (EGM1) is a potent, selective phosphodiesterase 4 (PDE4) antagonist, exhibiting an IC50 of 72 nM specifically for PDE4D3. It shows 40- to 50-fold greater selectivity for PDE4D3 over other phosphodiesterases. The mechanism of action involves PDE4 selective antagonism by Eggmanone, which activates protein kinase A, culminating in the blockade of the Hedgehog (Hh) signaling pathway [1].

CBS-3595 is a potent and dual Inhibitor of p38α MAPK/PDE-4 with a superior profile regarding its anti-inflammatory effects. CBS-3595 features moderate inhibition of p38α MAPK and PDE-4 in the higher nanomolar range in combination with excellent kinetic pr

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.

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor that targets PDE3 to relax airway smooth muscle and is used in asthma and chronic obstructive pulmonary disease (COPD) research. It also functions as an adenosine receptor antagonist, histone deacetylase (HDAC) activator, and exhibits anti-inflammatory activity by increasing IL-10 levels and inhibiting NF-κB nuclear import, while inducing apoptosis [1] [2] [3] [4] [5].

CC-1088 is an analog of thalidomide with potential antineoplastic activity that belongs to the functional class of agents called selective cytokine inhibitory drugs (SelCIDs). SelCIDs inhibit phosphodiesterase-4 (PDE 4), an enzyme involved in tumor necrosis factor alpha (TNF alpha) production. CC-1088 inhibits production of the cytokines vascular endothelial growth factor (VEGF) (a pro-angiogenic factor) and interleukin-6 (IL-6).

(E Z)-Ensifentrine is a potent and selective PDE3 4 inhibitor that acts as a long-acting inhibitor of the phosphodiesterase enzymes PDE-3 and PDE-4, producing both bronchodilator and anti-inflammatory effects. It is being developed by Verona Pharma as a potential treatment for asthma and hay fever and is currently in clinical trials.

Cipamfylline is a xanthine, a theophylline analogue, and is a potent and selective inhibitor of phosphodiesterase type 4 (PDE-4). Cipamfylline was tested in patients with a diagnosis of atopic dermatitis and in two human models of acute and chronic irritant contact dermatitis. The outcome of the study revealed that cipamfylline was more effective than vehicle in treating atopic dermatitis, but less effective than a group II steroid, hydrocortisone-17-butyrate both in the treatment of atopic dermatitis and irritant contact dermatitis. The absorption of cipamfylline and the subsequent systemic exposure might be the reason why further clinical studies with higher doses of cipamfylline have not been published.

Z21090 (ZL40) is a highly effective inhibitor of PDE 4, exhibiting an IC 50 value of 37.4 nM, and possesses oral bioavailability. It is significant in the study of alcohol-related diseases [1].

RS-25344 is a potent and selective phosphodiesterase (PDE) 4 inhibitor. It inhibits eosinophil chemotaxis and increases progressive motility of spermatozoa in vitro.

Vardenafil-d5 is a deuterated compound of Vardenafil. Vardenafil has a CAS number of 224785-90-4. Vardenafil (Levitra) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.