phosphodiesterase 4 inhibitor

Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.

Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

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

Filaminast (UNII-CDD69JC61J) is an analog of a phosphodiesterase 4 inhibitor (PDE4 inhibitor) and roliplam, which is used as an anti-asthma drug.

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.

uk-50001 is a phosphodiesterase (PDE) 4 inhibitor that can be used for many diseases, especially inflammation, allergies, respiratory diseases, disorders and conditions and wounds.

GEBR-7b (3-(Cyclopentyloxy)-4-methoxybenzaldehyde) is a phosphodiesterase-4 (PDE4) inhibitor.

Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.

Tanimilast (CHF-6001) is a novel, potent and selective phosphodiesterase 4 inhibitor with an IC 50 value of 0.026 ± 0.006 nM.Tanimilast has potent anti-inflammatory activity and is indicated for topical use in the lungs.Tanimilast was used in the study of obstructive lung disease.

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).

MK-0873 is a novel and potent selective phosphodiesterase 4 (PDE4) inhibitor.

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.

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.

HT-0712 is a phosphodiesterase 4 (PDE4) inhibitor.

Difamilast is an inhibitor of phosphodiesterase IV.

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].

FCPR03 is a selective inhibitor of phosphodiesterase 4 (PDE4) with IC50s of 31 nM, 47 nM, and 60 nM for PDE4B1, PDE4D7, and PDE4 catalytic domain, respectively. FCPR03 has neuroprotective, anti-inflammatory, and antidepressant-like effects.

MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).

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

RS 25344 hydrochloride is a phosphodiesterase (PDE) 4 inhibitor

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)

CP671305 is an orally active, potent and selective inhibitor of phosphodiesterase-4-D.

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) serves as an inhibitor of phosphodiesterase 4 (PDE4), applicable in research concerning diseases associated with PDE4, including inflammatory and immune disorders, cancer, and metabolic diseases [1].

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.

Crisaborole (AN-2728) is a Phosphodiesterase 4 Inhibitor.

Braylin has anti-inflammatory, antinociceptive and immunomodulatory effects, which possibly act through the glucocorticoid receptor activation and by inhibition of the transcriptional activity of NF-κB. Braylin is also a phosphodiesterase-4 inhibitor, it could represent an ideal prototype of glucocorticoid receptor ligand, able to induce synergic immunomodulatory effects.

Robustine is a natural product, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro.

RS 14203 is a selective type 4 phosphodiesterase (PDE4) inhibitor.

YM976 is an orally active PDE4 inhibitor (IC50:2.2 nM)

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

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent inhibitor of phosphodiesterase (PDE) that inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate can be used for the research of asthma and chronic obstructive pulmonary disease (COPD). Theophylline sodium glycinate is also an adenosine receptor antagonist and histone deacetylase (HDAC) activator. Theophylline sodium glycinate has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB nucleus import. Theophylline sodium glycinate induces apoptosis [1] [2] [3] [4] [5].

Crisaborole-d4 is a deuterated compound of Crisaborole. Crisaborole has a CAS number of 906673-24-3. AN-2728 is a Phosphodiesterase 4 Inhibitor.

Quercetin 3-O-methyl ether is a potent phosphodiesterase (PDE)3/4 inhibitor, it has potential for treating asthma against ovalbumin-induced airway hyperresponsiveness.

L-826141 is an inhibitor of phosphodiesterase 4.

GSK356278 is an effective and selective inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory, anxiolytic, and cognition-enhancing effects.

Mesembrine is a serotonin reuptake inhibitor and is also a weak inhibitor of the enzyme phosphodiesterase 4 (PDE4).

Apremilast, (+/-)-, is a small molecule inhibitor of phosphodiesterase 4 (PDE4) with oral activity. It is used to treat psoriatic arthritis.

EHNA hydrochloride is a chemical compound recognized for its antiviral, antitumor, and antiarrhythmic properties. It functions as a potent and selective inhibitor of both cyclic nucleotide phosphodiesterase 2 (PDE2) with an IC50 of 4 μM and adenosine deaminase (ADA). Additionally, it effectively inhibits the activity of cGMP-stimulated PDE II (cGs-PDE) with IC50 values of 0.8 μM in humans and 2 μM in porcine myocardium, although its inhibitory effects on unstimulated PDE2 activity are less pronounced.

Ro 20-1724 (4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone) is a widely used inhibitor of cyclic nucleotide phosphodiesterase with IC50 of 2.0 μM and Ki of 3.1 μM.

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).

3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 |1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Khan, K.M., Iqbal, S., Lodhi, M.A., et al. Biscoumarin: New class of urease inhibitors; economical synthesis and activity. Bioorg. Med. Chem. 12(8), 1963-1968 (2004).

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.

Mufemilast is an inhibitor of phosphodiesterase 4 (PDE4).

L791943 is a selective, potent) inhibitor of Phosphodiesterase-4 (PDE4,IC50 of 4.2 nM).

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.

ABE171, also known as NVP-ABE171, is a potent and novel phosphodiesterase 4 inhibitor with anti-inflammatory activities. NVP-ABE171 inhibited the activity of phosphodiesterase 4A, 4B, 4C, and 4D with respective IC(50) values of 602, 34, 1230, and 1.5 nM. In human cells, NVP-ABE171 inhibited the eosinophil and neutrophil oxidative burst, the release of cytokines by T cells, and the tumor necrosis factor-alpha release from monocytes, in the nanomolar range. NVP-ABE171 inhibited the airway neutrophil influx and activation with an ED(50) in the range of 3 mg/kg. NVP-ABE171 shows activity both in vitro on human inflammatory cells and in vivo in animal models of lung inflammation.

Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor，and is an antispasmodic drug, used to enhance cervical dilation during childbirth. Drotaverine hydrochloride is structurally related to papaverine

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].