Cilomilast

ArtNr	S1455-10
Hersteller	Selleckchem
CAS-Nr.	153259-65-5
Menge	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Kategorie	Food Safety Allergenes Neuroscience Neural Lineage Markers Neuroinflammation Metabolism Diabetes Glucose Homeostasis Aging & Neurological Disorders Inhibitors & Compound Libraries Small Molecules
Typ	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
Lieferbar
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.

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