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(R)-Lisofylline

CAS No. : 100324-81-0

MCE 国际站：(R)-Lisofylline

产品活性：(R)-Lisofylline ((R)-Lisophylline) 是一种 Pentoxifylline 代谢产物的 (R)-型对映体，具有抗炎特性。(R)-Lisofylline 是一种溶血磷脂酸酰基转移酶 (lysophosphatidic acid acyltransferase ) 抑制剂，IC₅₀ 为 0.6 µM，可中断 IL-12 信号介导的 STAT4 激活。(R)-Lisofylline 可用于 1 型糖尿病，自身免疫性疾病的研究。

研究领域：JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：STAT

In Vitro: (R)-Lisofylline blocks IL-12-driven Th1 differentiation and T cell proliferation in vitro, yet has no effect on IL-12 secretion from APCs ex vivo or in vitro.

In Vivo: (R)-Lisofylline reduces the impairment of insulin secretion induced by IL-1β in cultured rat islet cells, suppresses IFN-γ production, the onset of diabetes, and macrophage infiltration into islets from NOD mice, as well as Lisofylline improves insulin response and lowers glucose levels in Streptozotocin-treated rats after the oral glucose tolerance test.
(R)-Lisofylline prevents β cell dysfunction in NOD mice by inhibition of STAT4 phosphorylation which interrupts IL-12 signaling. (R)-Lisofylline ameliorates experimental allergic encephalomyelitis in mice.
(R)-Lisofylline also improves survival in mice injected with a lethal dose of LPS and ameliorates sepsis-induced lung injury in minipigs. In rats given IL-1 intratracheally (R)-Lisofylline pretreatment reduces lung leak but does not decrease neutrophil accumulation in lungs.
(R)-Lisofylline also suppresses release of TNF-α in vivo in mice and ex vivo in human blood stimulated with endotoxin derived from Salmonella or Escherichia coli.

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