Catalog No.S1455 Synonyms: SB-207499

For research use only.

Cilomilast (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.

Cilomilast Chemical Structure

CAS No. 153259-65-5

Selleck's Cilomilast has been cited by 8 Publications

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Biological Activity

Description Cilomilast (SB-207499) 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.
LPDE4 [1]
(Cell-free assay)
HPDE4 [1]
(Cell-free assay)
100 nM 120 nM
In vitro

Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. [2] 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. [2] 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. [3] Cilomilast reduces TLR4 expression, IL-8 release and neutrophil chemotactic activity as well as it increased IP-10 release and lymphocyte chemotactic activity. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells MVzGeY5kfGmxbjDhd5NigQ>? NE\V[5FKdmirYnn0bY9vKG:oIHj1cYFvKFCqb4PwbI9lcWW|dHXyZZNmKDSDIHnzc4Zwem1idYPpcoch[2:wc4TyeYN1KHKncILld4VvfGmwZzD0bIUh[2:vbX;uJJJm\2mxbjDv[kB{eGyrY3XkJJZiemmjboTzJIV5eHKnc4Pl[EBieyCJU2St[pV{cW:wIIDyc5RmcW6|IHnuJHNnQSClZXzsd{whUUN3ME2wMlA{QCEQvF2= NFXPcnIyOjJ5MEG5OS=>
sf21 cells NUTnbXpRTnWwY4Tpc44h[XO|YYm= NYmxVolnUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsJIxmdme2aDDQSGU1STRiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKHOoMkGgZ4VtdHNuIFnDOVA:OC5yNkKg{txO MkDUNlM5ODZ3NUO=
human peripheral blood mononuclear cells MkTJSpVv[3Srb36gZZN{[Xl? MmjITY5pcWKrdHnvckBw\iCWTl[tZYxxcGFicnXs[YF{\SCocn;tJIh2dWGwIIDldolxcGW{YXygZoxwd2RibX;uc452[2ynYYKgZ4VtdHNuIFnDOVA:Oy52Nkeg{txO NEizb24yOTd3NUO2Ni=>
U937 cells NFy1NYNHfW6ldHnvckBie3OjeR?= NWDIW4tMSXKkaYThdpkhdWG6aX3hcEBz\XOyb37z[UBnd3JiY1HNVEBmdGW4YYTpc44h\nKxbTDiZZNmdGmwZTDs[ZZmdCC5YYOg[ZZidHWjdHXkJIlvKEi3bXHuJHUuQTN5IHPlcIx{NCCHQ{WwQVMvPjNizszN MWm5OlMzOzZy
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. [1] 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. [1] 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 [5].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: U937 cells
  • Concentrations: 0.1-10 μM
  • Incubation Time: 5 min
  • Method: U937 cells (1-2 × 10 6) are incubated at 37 °C in a shaking water bath with Cilomilast for 1 min before the addition of 0.1 μM PGE2 (total volume of 200 μL). The incubation proceeds for an additional 4 min and is stopped by the addition of 0.1 mL of HClO4 (17.5%), neutralized with 0.15 ml of K23 (1.0 M) and diluted to 1 mL with sodium acetate buffer. Samples are centrifuged at 3000 × g for 10 min. Aliquots of the supernatant fraction are assayed for cAMP content by radioimmunoassay using commercially available kits.
Animal Research:[1]
  • Animal Models: Balb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock
  • Dosages: 3, 6, 12, 25, 50 mg/kg
  • Administration: Gavage

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+95% Corn oil
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 343.42


CAS No. 153259-65-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C(C=C1)C2(CCC(CC2)C(=O)O)C#N)OC3CCCC3

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