Roflumilast罗氟司特,162401-32-3

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Roflumilast

CAS No. : 162401-32-3

MCE 国际站：Roflumilast

产品活性：Roflumilast (APTA-2217) 是一种选择性的 PDE4 抑制剂，作用于 PDE4A1，PDEA4，PDEB1 和 PDEB2，IC₅₀ 分别为 0.7，0.9，0.7 和 0.2 nM。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Phosphodiesterase (PDE)  |  RSV

In Vitro: Roflumilast does not affect PDE enzymes apart from PDE4, and is a subnanomolar inhibitor of most PDE4 splicing variants tested. It showed no PDE4 subtype selectivity apart from PDE4C (4C1, IC₅₀=3 nM; 4C2, IC₅₀=4.3 nM), which is inhibited with a slightly lower potency. Roflumilast is a potent and selective PDE4 inhibitor. Roflumilast is a monoselective PDE4 inhibitor since it does not affect other PDE isoenzymes, including PDE1, PDE2, PDE3, and PDE5 up to 10,000-fold higher concentrations. Roflumilast inhibits human neutrophil functions. Roflumilast inhibits TNFα synthesis in monocyte-derived dendritic cells. Rolfumilast inhibits proliferation and cytokine synthesis in CD4⁺ T cells. Proliferation is inhibited to a maximum of about 60% by Roflumilast with a potency (IC₃₀) of 7 nM.

In Vivo: Animal studies with Roflumilast demonstrated that it reduced the accumulation of neutrophils in bronchoalveolar lavage fluid following short-term exposure of guinea pigs, mice or rats to tobacco smoke, and following exposure of rats to a combination of tobacco smoke and bacterial lipopolysaccharide, and abolished the lung parenchymal influx of inflammatory cells seen in rats exposed to tobacco smoke for 7 months. Roflumilast blocks COPD progression in pIgR^?/? mice. For these studies, 9-month-old WT or pIgR^?/? mice are treated daily by oral gavage with 100 μg of Roflumilast (5 μg/g) or vehicle (4% methylcellulose, 1.3% PEG400) for 3 months and lungs are harvested at 12 months of age. Unlike pIgR^?/? mice treated with vehicle, mice treated with Roflumilast had no progression of small airway wall remodelling after starting treatment. Strikingly, 12-month-old pIgR^?/? mice treated with Roflumilast had reduced indices of emphysema compared with 9-month-old pIgR^?/? mice, indicating that Roflumilast not only blocks progression of emphysema in this model but apparently facilitates some resolution of the emphysematous destruction of lung parenchyma.

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