roflumilast

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.

Roflumilast Impurity E is an impurity of Roflumilast, which acts as a selective and long-acting enzyme PDE-4 inhibitor (IC50 value of 0.8 nM).

Roflumilast N-oxide is an inhibitor of PDE type 4.

Roflumilast N-Oxide-d4 is a deuterated compound of Roflumilast N-Oxide. Roflumilast N-Oxide has a CAS number of 292135-78-5. Roflumilast N-oxide is a PDE type 4 inhibitor.

D-159404, as an allosteric inhibitor, demonstrates superior inhibitory effects on the full-length PDE 4D3 compared to its truncated form and exhibits higher cellular activity. This sets it apart from competitive inhibitors like roflumilast and cilomilast. These findings indicate that D-159404 and related compounds may offer valuable insights into PDE 4 pharmacology and serve as strong candidates for further study on cAMP signaling's impact on disease treatment.

PDE4B-IN-6 (Compound 4i) is a potent and highly selective inhibitor of phosphodiesterase 4B (PDE4B) with an IC50 of 7.42 nM. As a roflumilast analogue, it exhibits significantly higher selectivity for PDE4B over PDE4A (IC50 = 1540 nM, ~195-fold) and PDE4C (IC50 = 1260 nM, ~169-fold). PDE4B-IN-6 exerts anti-inflammatory effects by elevating intracellular cAMP levels and suppressing the expression of the pro-inflammatory cytokine TNF-α. Additionally, it demonstrates good antioxidant properties and low cytotoxicity, making it suitable for research on chronic obstructive pulmonary disease (COPD) and related inflammatory conditions.