pde4b1

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.

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.

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.

PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.

PDE3/4-IN-2 is a potent dual PDE3/PDE4 inhibitor with IC50 values of 0.13 nM for PDE3A and 50 nM for PDE4B1. It is used to investigate PDE-related diseases such as asthma, COPD, sepsis, and nephritis. the dual-target activity of PDE3/4-IN-2 provides a mechanistic basis for dissecting cAMP regulation and inflammatory signaling pathways.

LEO-32731 is a bioactive chemical.

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).

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)

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.