pde4

IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5 26.3 31.7 μM). IBMX enhances the intracellular cAMP level.

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.

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.

Tofimilast (CP-325366), a PDE4 inhibitor, is used potentially for the treatment of asthma and chronic obstructive pulmonary 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).

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

Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

ICI 63197 (2-Amino-6-methyl-4-propyl-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-one) is a PDE4 inhibitor.

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.

Cilomilast (SB-207499) is a potent PDE4 inhibitor with an IC50 of approximately 110 nM, demonstrating anti-inflammatory activity and minimal central nervous system effects. Phase 3.

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.

Pumafentrine(BY 343) is a dual PDE3 PDE4 inhibitor that reduces clinical scores and TNF expression in experimental colitis in mice.

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-21 (Compound L19) is an effective PDE4 inhibitor with an IC50 of 0.48 μM. It demonstrates substantial inhibitory activity and notable metabolic stability in rat liver microsomes.

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].

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].

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-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].

PDE4-IN-26 (Compound A5) is an orally active, highly selective inhibitor of PDE4. It exhibits anti-inflammatory properties by inhibiting p38 MAPK phosphorylation. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 reduces lung inflammation, damage, and fibrosis, while promoting sputum secretion and alleviating cough. It is useful for researching lung injury-related diseases.

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.

PDE4-IN-18 (compound 1l) is a PDE4 inhibitor with an IC50 value of 1.55 μM and exhibits anti-inflammatory activity. It mitigates inflammation by reducing excessive infiltration of immune cells and enthesial formation, as well as decreasing the mRNA expression of pro-inflammatory cytokines (such as TNF-α and IL-6) in the synovial tissues. PDE4-IN-18 is suitable for research into rheumatoid arthritis and psoriasis.

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.

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.