Cilomilast

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

4 Customer Reviews

Purity & Quality Control

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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.
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 Mn\zSpVv[3Srb36gZZN{[Xl? MXXJcohq[mm2aX;uJI9nKGi3bXHuJHBpd3OyaH;kbYV{fGW{YYPlJFRCKGm|b3\vdo0hfXOrbnegZ49ve3S{dXP0JJJmeHKnc3XueIlv\yC2aHWgZ49udW:wIILl[4lwdiCxZjDzdIxq[2WmII\hdolidnS|IHX4dJJme3OnZDDhd{BIW1RvZoXzbY9vKHC{b4TlbY5{KGmwIGPmPUBk\WyuczygTWM2OD1yLkCzPEDPxE1? Mn;KNVIzPzBzOUW=
sf21 cells M{X0bWZ2dmO2aX;uJIF{e2G7 M4XhWGlvcGmkaYTpc44hd2ZiaIXtZY4h\nWubDDs[Y5ofGhiUFTFOGE1KGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EB{\jJzIHPlcIx{NCCLQ{WwQVAvODZ{IN88US=> Mn32NlM5ODZ3NUO=
human peripheral blood mononuclear cells NU\LS3RWTnWwY4Tpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKFSQRj3hcJBp[SC{ZXzlZZNmKG[{b32gbJVu[W5icHXybZBp\XKjbDDicI9w\CCvb37vcpVkdGWjcjDj[YxteyxiSVO1NF0{NjR4NzFOwG0> NEXGUo8yOTd3NUO2Ni=>
U937 cells M2j5[mZ2dmO2aX;uJIF{e2G7 NF35[2hCemKrdHHyfUBu[XirbXHsJJJme3CxboPlJIZweiClQV3QJIVt\X[jdHnvckBnem:vIHLhd4VtcW6nIHzleoVtKHejczDleoFtfWG2ZXSgbY4hUHWvYX6gWU06OzdiY3XscJMtKEWFNUC9N{43OyEQvF2= MWO5OlMzOzZy
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.
  • (Only for Reference)
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
  • (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 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

* 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 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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

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.

Handling Instructions

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