pde4 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.

Oglemilast (GRC 3886) suppresses pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast is an effective and orally active phosphodiesterase-4 (PDE4) inhibitor (IC50: 0.5 nM for PDE4D3). Oglemilast has the potential for inflammatory airway diseases.

AWD 12-281 is a selective phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory and bronchodilator activity used in the study of chronic obstructive pulmonary disease (COPD).

PF-07038124 HCl is a selective and potent PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2.PF-07038124 HCl inhibits IL-13, IL-4, and IFNγ, and can be used in the study of skin disorders such as atopic dermatitis and plaque psoriasis.

Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor that reduces the production of pro-inflammatory mediators and cytokines. Dovramilast is used in the study of Mycobacterium tuberculosis infections and lupus erythematosus.

PDE4-IN-22 (Compound 2e) is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 2.4 nM. It exhibits anti-inflammatory properties and demonstrates significant anti-psoriatic effects in an Imiquimod-induced psoriasis mouse model.

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].

O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral administrationXenobiotica41(12)1063-1075(2011) 2.Lu, Y., Shen, X., Hang, T., et al.Identification and characterization of process-related substances and degradation products in apremilast: Process optimization and degradation pathway elucidationJ. Pharm. Biomed. Anal.14170-78(2017) 3.Bhole, R.P., Naksakhare, S.R., and Bonde, C.G.A stability indicating HPTLC method for apremilast and identification of degradation products using MS/MSJ. Pharm. Sci. & Res.11(5)1861-1869(2019)

LEO 39652, a dual-soft PDE4 inhibitor, demonstrates potent inhibition of PDE4 subtypes A, B, C, and D with respective IC50 values of 1.2 nM, 1.2 nM, 3.0 nM, and 3.8 nM. Additionally, it inhibits TNF-α with an IC50 of 6.0 nM, indicating its potential for topical Atopic dermatitis (AD) research [1].

Tetomilast (OPC-6535) is a phosphodiesterase-4 (PDE4) inhibitor, potentially effective for treating inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).

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.

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.

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].

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].

(S)-(+)-Rolipram ((+)-Rolipram) inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM and exhibits anti-inflammatory and anti-depressant activity in the central nervous system, though it is less potent than its R enantiomer.

AWD 12-281 is a selective phosphodiesterase 4 (PDE4) inhibitor for the treatment of lung inflammation using inhalative administration. AWD 12-281 Is Active in a New Guinea-Pig Model of Allergic Skin Inflammation Predictive of Human Skin Penetration and Suppresses Both Th1 and Th2 Cytokines in Mice. AWD 12-281 is a very promising drug candidate not only for the treatment of lung inflammation using inhalative administration but also for the treatment of atopic dermatitis.

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg ml, reduces cough induced by citric aci......

LEO-29102 is a potent, selective, and soft-drug phosphodiesterase 4 (PDE4) inhibitor, which may be potentially useful for treatment of dermatological diseases. LEO 29102 shows properties suitable for patient-friendly formulations giving efficient drug delivery to the skin. LEO-29102 has reached phase 2 and demonstrated clinically relevant efficacy in the treatment of atopic dermatitis.

Toddacoumalone, a natural compound, exhibits moderate potency as an inhibitor of phosphodiesterase 4 (PDE4) and possesses traits that are not fully ideal for an agent. It has potential application in the study of inflammatory conditions, including psoriasis [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-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].

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].