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Cilomilast

CAS No. : 153259-65-5

MCE 國際站：Cilomilast

產品活性：Cilomilast (SB-207499) 是一種有效的，選擇性的和具有口服活性的磷酸二酯酶 4 (PDE4) 抑制劑，對 LPDE4 和 HPDE4 的 IC₅₀ 值分別約為 100 和 120 nM。 Cilomilast 對 PDE4 的選擇性高于 PDE1，PDE2，PDE3 和 PDE5 (IC₅₀=74，65，>100，83 µM)。Cilomilast 具有抗炎和免疫調節作用，可用于哮喘和慢性阻塞性肺疾病 (COPD) 的研究。

研究領域：Metabolic Enzyme/Protease

作用靶點：Phosphodiesterase (PDE)

In Vitro: 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.

In Vivo: 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.

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