Cilomilast

Catalog No.S1455 Synonyms: SB-207499

Cilomilast Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 210 In stock
USD 670 In stock
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3 Customer Reviews

  • 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 with
    1% 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 the
    degradation 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.

Purity & Quality Control

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Biological Activity

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.
Targets
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 MY\GeY5kfGmxbjDhd5NigQ>? MXnJcohq[mm2aX;uJI9nKGi3bXHuJHBpd3OyaH;kbYV{fGW{YYPlJFRCKGm|b3\vdo0hfXOrbnegZ49ve3S{dXP0JJJmeHKnc3XueIlv\yC2aHWgZ49udW:wIILl[4lwdiCxZjDzdIxq[2WmII\hdolidnS|IHX4dJJme3OnZDDhd{BIW1RvZoXzbY9vKHC{b4TlbY5{KGmwIGPmPUBk\WyuczygTWM2OD1yLkCzPEDPxE1? MUCxNlI4ODF7NR?=
sf21 cells M2nDcWZ2dmO2aX;uJIF{e2G7 MlSyTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCSRFW0RVQh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnOjFiY3XscJMtKEmFNUC9NE4xPjJizszN M2[3dlI{QDB4NUWz
human peripheral blood mononuclear cells MYfGeY5kfGmxbjDhd5NigQ>? MnnnTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFicnXs[YF{\SCocn;tJIh2dWGwIIDldolxcGW{YXygZoxwd2RibX;uc452[2ynYYKgZ4VtdHNuIFnDOVA:Oy52Nkeg{txO MofkNVE4PTV|NkK=
U937 cells NIrWU5FHfW6ldHnvckBie3OjeR?= M4jSdmFz[mm2YYL5JI1igGmvYXygdoV{eG:wc3Wg[o9zKGODTWCg[YxmfmG2aX;uJIZzd21iYnHz[YxqdmVibHX2[Ywhf2G|IHX2ZYx2[XSnZDDpckBJfW2jbjDVMVk{PyClZXzsd{whTUN3ME2zMlY{KM7:TR?= MWm5OlMzOzZy

... Click to View More Cell Line Experimental Data

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

Cell Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Balb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock
  • Formulation: Olive oil
  • Dosages: 3, 6, 12, 25, 50 mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 69 mg/mL (200.92 mM)
Ethanol 50 mg/mL (145.59 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+95% Corn oil
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 343.42
Formula

C20H25NO4

CAS No. 153259-65-5
Storage powder
Synonyms SB-207499

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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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID