产品
编 号：F181222
分子式：C20H25NO4
分子量：343.42
分子式：C20H25NO4
分子量：343.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 153259-65-5
产品详情
生物活性：
Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 μM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).
体内研究：
SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice.SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED50 of 2.3 mg/kg.SB-207499 (500 μg/ear; b.i.d. for 6 d) inhibits the chronic oxazolone-induced inflammatory response and intralesional IL-4 concentrations in mice.Animal Model:Male Balb/c mice (18-25 g) are injected with human monocytes and LPS
Dosage:1, 5, 10, 50, 100 mg/kg
Administration:P.o. after the injection of human monocytes and before LPS challenge
Result:Inhibited the production of human TNFα, with an ED50 of 4.9 mg/kg.
体外研究：
Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions.Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response.Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood.
Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 μM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).
体内研究：
SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice.SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED50 of 2.3 mg/kg.SB-207499 (500 μg/ear; b.i.d. for 6 d) inhibits the chronic oxazolone-induced inflammatory response and intralesional IL-4 concentrations in mice.Animal Model:Male Balb/c mice (18-25 g) are injected with human monocytes and LPS
Dosage:1, 5, 10, 50, 100 mg/kg
Administration:P.o. after the injection of human monocytes and before LPS challenge
Result:Inhibited the production of human TNFα, with an ED50 of 4.9 mg/kg.
体外研究：
Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions.Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response.Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood.
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