pde4d3

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.

Zatolmilast (BPN14770) is an allosteric inhibitor of selective phosphodiesterase 4D (PDE4D; IC50s: 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3).

CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).

PF-04822163 is a potent inhibitor of PDE1 with IC50 value of 0.0024 μM.

UK-500001 is a potent PDE4 inhibitor with robust anti-inflammatory activity.

LEO-32731 is a bioactive chemical.

PDE4-IN-19 (compound 1) acts as a PDE4 inhibitor and exhibits potent inhibition with IC 50 values below 10 nM for PDE4B1 and between 10-100 nM for PDE4D3.

Phosphodiesterase-IN-3 (Example 20) is an inhibitor of phosphodiesterase 4B, with IC50 values for PDE4B1 and PDE4D3 of less than 10 nM and between 10-100 nM, respectively. Phosphodiesterase-IN-3 shows potential for research in idiopathic pulmonary fibrosis.

(S)-Gebr32a is a potent PDE4 inhibitor, exhibiting IC50 values of 19.5 µM for PDE4cat and 2.1 µM for PDE4D3.

PDE4-IN-29 (Compound 55) is an orally active and selective inhibitor of PDE4, targeting subtypes such as PDE4A1, PDE4B2, and PDE4D3, with an IC50 value for PDE4D3 of less than 5 nM. It inhibits the degradation of cyclic adenosine monophosphate (cAMP), elevating intracellular cAMP levels and suppressing the release of inflammatory mediators like TNF-α. PDE4-IN-29 holds potential for research in inflammatory diseases such as psoriasis, atopic dermatitis, and chronic obstructive pulmonary disease.

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].