Description
LPDE4 and HPDE4 can be inhibited by cilomilast (SB-207499) with IC50 of 100 nM and 120 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C20H25NO4
Chemical Name
4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
Solubility
DSMO 69 mg/mL Water
In vitro
As a PDEIV inhibitor, Cilomilast inhibited TNFalpha release at concentrations >300 nM, but shows no inhibition to IL-6 release at any of the concentration in COPD lung macrophages. Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. Cilomilast decreases the expression of IL-17 and IL-23 in the draining lymph nodes. Cilomilast reduces TLR4 expression, IL-8 release and neutrophil chemotactic activity as well as it increased IP-10 release and lymphocyte chemotactic activity.
In vivo
Cilomilast inhibits human TNFalpha production with oral ED50 of 4.9 mg/kg. In contrast to their equipotent activity against TNFalpha production, Cilomilast (ED50 = 2.3 mg/kg, p.o.) is 10-fold less potent than R-rolipram (ED50 = 0.23 mg/kg, p.o.) in reversing reserpine-induced hypothermia, a model of antidepressant activity.
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