« Back
Home /
Cilomilast

Cilomilast

Item no.	S1455-5
Manufacturer	Selleckchem
CASRN	153259-65-5
Amount	5 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Category	Food Safety Allergenes Neuroscience Neural Lineage Markers Neuroinflammation Metabolism Diabetes Glucose Homeostasis Aging & Neurological Disorders Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Smiles	COC1=C(C=C(C=C1)C2(CCC(CC2)C(=O)O)C#N)OC3CCCC3
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	SB-207499
Similar products	Cilomilast
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	343, 42
Administration	Gavage
Animal Models	Balb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock
Cell lines	U937 cells
Clinical Trials	A phase III clinical trial of Cilomilast for the treatment of emphysema and bronchitis has been completed.
Concentrations	0.1-10 uM
Dosages	3, 6, 12, 25, 50 mg/kg
Formulation	Olive oil
IC50	100 nM, 100 nM, 100 nM, 100 nM, 100 nM, 100 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-alpha 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-alpha in the cornea and IL-1alpha, IL-1beta, and TNF-alpha 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]
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. [1] In time course studies, Cilomilast (30 mg/kg, p.o.) suppresses TNFalpha 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 ug) inhibits intralesional concentrations of interleukin-4. [1] Orally administered cilomilast dose-dependently inhibits production of interleukin-4, TNF-alpha, and cysteinyl leukotrienes, as well as leukocyte infiltration in bronchoalveolar lavage fluid from the airways of ovalbumin-sensitized Brown Norway rats [5].
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 uM PGE 2 (total volume of 200 uL). 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 K2
Solubility (25C)	DMSO 69 mg/mL, Water <1 mg/mL, Ethanol 50 mg/mL
Information	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.
Chemical Name	4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
Features	Cilomilast has been used to treat chronic obstructive pulmonary disease (COPD) for centuries.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Request Data Sheet

S1455-5-datasheet.pdf

S1455-5-safety-datasheet.pdf