PDE4A

Rolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.

ML-030 is a potent and selective inhibitor of PDE4(PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2 with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM, respectively)

BC8-15 is a PDE inhibitor with IC50 values of 0.28 µM for PDE8A, 0.22 µM for PDE4A, and 6.46 µM for PDE7A. It enhances steroid production in mouse Leydig cells.

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.

L-869298 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4).

PF-06445974 has good selectivity for PDE4D, excellent brain permeability, and has a high level of specific binding in the cold tracer study.

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].

LASSBio-1632 is a novel anti-asthmatic lead candidate that selectively inhibits PDE4A and PDE4D isoenzymes, leading to the suppression of airway hyper-reactivity (AHR) and TNF-α production in lung tissue. With high experimental BBB permeability, LASSBio-1632 (7j) efficiently crosses the blood-brain barrier through passive diffusion [1].

Enoximone is a selective inhibitor of phosphodiesterase III (PDE3), with treatment of congestive heart failure.