Catalog No.S1455 Synonyms: SB-207499
Molecular Weight(MW): 343.42
Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.
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LNCaP-C4 prostate cancer cells were suspended in matrigel and transplanted under the kidney capsule of male nude mice hosts. Mice were treated with vehicle-only (10% EtOH, 90% olive oil) control, cilomilast or NVP-ABE171 by gavage (n=7-11 for each respective group)The xenografts LNCaP-C4 xenografts were excised, fixed in formalin, and embedded in paraffin blocks. IHC with Ki67 (proliferation), TUNEL (apoptosis), or p21 (senescence) was performed. Representative Ki67 and TUNEL photomicrographs for cilomilast and NVP-ABE171 treatment group are shown.
Mol Cancer Res 2014 10.1158/1541-7786.MCR-14-0110. Cilomilast purchased from Selleck.ALP activity levels relative to control: (a) samples treated with 300 ng/mL of BMP-2; (b) samples treated with 30 ng/mL of BMP-2. Cells cultured with 1% DMSO for 11 days were used as control cells. Bar represent mean SD for 8 experiments. PDE4 I =PDE4 inhibitor, SM =standard medium, OM =osteogenic medium.
Biochimie 2012 94, 2360e2365 . Cilomilast purchased from Selleck.
ALP activity levels relative to samples treated with DMSO. Cells cultured with1% DMSO for 11 days were used as control cells. The inset shows a schematic representation of the PDE4 inhibitor (PDE4 I) and H89 pathways. PDE4 I blocks thedegradation of the intracellular cAMP signalling by PDE, and increases the PKA levels. By the use of an efficient PKA inhibitor, H89, the pathway activated downstream by PKA is completely blocked. Bar represent mean SD for 8 experiments.
Biochimie 2012 94, 2360e2365 . Cilomilast purchased from Selleck.
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|Description||Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.|
|Features||Cilomilast has been used to treat chronic obstructive pulmonary disease (COPD) for many years.|
Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells.  In isolated human monocytes, Cilomilast and (R)-rolipram are equipotent at suppressing LPS-induced TNF-α formation with -log (IC50) of 7.0 and 7.2, respectively. Both Cilomilast and (R)-rolipram produces a modest prevention of fMLP-induced degranulation of human neutrophils. Cilomilast and (R)-rolipram are equipotent at suppressing neutrophil activation with -log (IC50) of 7.1 and 6.4, respectively.  Cilomilast significantly decreases the expression of TNF-α in the cornea and IL-1α, IL-1β, and TNF-α in the conjunctivaas compared to vehicle control. Cilomilast treatment markedly decreases the presence of CD11b+ antigen-presenting cells in the central and peripheral cornea, and leads to decreased conjunctival expression of cytokines IL-6, IL-23, and IL-17. Moreover, 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 TNFα production with oral ED50 of 4.9 mg/kg. In contrast to their equipotent activity against TNFα 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.  In time course studies, Cilomilast (30 mg/kg, p.o.) suppresses TNFα production for at least 10 hour. The ability of Cilomilast to modulate interleukin-4 productionin vivo is assessed in a chronic oxazolone-induced contact sensitivity model in Balb/c mice. Topical administration of Cilomilast (1000 μg) inhibits intralesional concentrations of interleukin-4.  Orally administered cilomilast dose-dependently inhibits production of interleukin-4, TNF-α, and cysteinyl leukotrienes, as well as leukocyte infiltration in bronchoalveolar lavage fluid from the airways of ovalbumin-sensitized Brown Norway rats .|
-  Griswold DE,et al. J Pharmacol Exp Ther. 1998, 287(2),705-711.
-  Barnette MS, et al. J Pharmacol Exp Ther. 1998, 284(1), 420-426.
-  Sadrai Z, et al. Invest Ophthalmol Vis Sci. 2012.
|In vitro||DMSO||69 mg/mL (200.92 mM)|
|Ethanol||50 mg/mL (145.59 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+95% Corn oil
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00103922||Completed||Pulmonary Disease, Chronic Obstructive||GlaxoSmithKline||November 2004||Phase 3|
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