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Synonyms | SB-207499 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H25NO4 |
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分子量 | 343.42 | CAS No. | 153259-65-5 | |
Solubility (25°C)* | 体外 | DMSO | 69 mg/mL (200.92 mM) | |
Ethanol | 50 mg/mL (145.59 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * 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. |
製品説明 | 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. |
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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] |
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]. |
特徴 | Cilomilast has been used to treat chronic obstructive pulmonary disease (COPD) for many years. |
細胞アッセイ | 細胞株 | U937 cells |
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濃度 | 0.1-10 μM | |
反応時間 | 5 min | |
実験の流れ | 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. | |
動物実験 | 動物モデル | Balb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock |
投薬量 | 3, 6, 12, 25, 50 mg/kg | |
投与方法 | Gavage |
Data from [Data independently produced by Mol Cancer Res, 2014, 10.1158/1541-7786.MCR-14-0110]
Data from [Biochimie, 2012, 94, 2360e2365 ]
Data from [Biochimie, 2012, 94, 2360e2365 ]
Inhibition of PDE4/PDE4B improves renal function and ameliorates inflammation in cisplatin-induced acute kidney injury. [ Am J Physiol Renal Physiol, 2020, 318(3):F576-F588] | PubMed: 31961716 |
A multi-targeted liquid chromatography–mass spectrometryscreening procedure for the detection in human urine of drugsnon-prohibited in sport commonly used by the athletes [Mazzarino M, et al. J Pharm Biomed Anal, 2016, 117:47-60] | PubMed: 26342446 |
Inhibitors of Phosphodiesterase 4, but Not Phosphodiesterase 3, Increase β2-Agonist–Induced Expression of Antiinflammatory Mitogen-Activated Protein Kinase Phosphatase 1 in Airway Smooth Muscle Cells [Patel BS Am J Respir Cell Mol Biol, 2015, 52(5):634-40] | PubMed: 25296132 |
Phosphodiesterase 4D inhibitors limit prostate cancer growth potential [ Mol Cancer Res, 2015, 13(1):149-60] | PubMed: 25149359 |
Phosphodiesterase 4D Inhibitors Limit Prostate Cancer Growth Potential [Powers GL, et al. Mol Cancer Res, 2015, 13(1):149-60] | |
Inhibitors of Phosphodiesterase 4, but Not Phosphodiesterase 3, Increase b2-Agonist–Induced Expression of Antiinflammatory Mitogen-Activated Protein Kinase Phosphatase 1 in Airway Smooth Muscle Cells [Patel BS, et al. AM J Resp Cell Mol, 2014, 10.1165/rcmb.2014-0344OC] | |
Monitoring phosphodiesterase‐4 inhibitors using liquid chromatography/(tandem) mass spectrometry in sports drug testing [Thevis M Rapid Commun Mass Spectrom, 2013, 27(9):993-1004] | PubMed: 23592202 |
Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2. [Munisso MC, et al. Biochimie, 2012, 94(11):2360-5] | PubMed: 22706281 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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