Cilomilast

Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC₅₀s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC₅₀=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD)^[1][2][3]. In Vitro: Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions^[2].
Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response^[2].
Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood^[2]. In Vivo: SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice^[1].
SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED₅₀ of 2.3 mg/kg^[1].
SB-207499 (500 μg/ear; b.i.d. for 6 d) inhibits the chronic oxazolone-induced inflammatory response and intralesional IL-4 concentrations in mice^[1].