1-(5-hydroxyhexyl)-3,7-dimethyl-purine-2,6-dione

生物活性靶点体外研究体内研究 1-(5-hydroxyhexyl)-3,7-dimethyl-purine-2,6-dione 试剂级价格

CAS号:100324-81-0
英文名:1-(5-hydroxyhexyl)-3,7-dimethyl-purine-2,6-dione
中文名:1-(5-hydroxyhexyl)-3,7-dimethyl-purine-2,6-dione
CBNumber:CB21454169
分子式:C13H20N4O3
分子量:280.32
MOL File:100324-81-0.mol

1-(5-hydroxyhexyl)-3,7-dimethyl-purine-2,6-dione化学性质

熔点 :105-107°C
比旋光度 :D20 -5.6° (c = 6.7 in ethanol)
沸点 :511.2±56.0 °C(Predicted)
密度 :1.32±0.1 g/cm3(Predicted)
储存条件 :Hygroscopic, -20°C Freezer, Under Inert Atmosphere
溶解度 :Chloroform, Methanol
形态 :Solid
酸度系数(pKa) :15.22±0.20(Predicted)
颜色 :White to Off-White
稳定性 :Hygroscopic

1-(5-hydroxyhexyl)-3,7-dimethyl-purine-2,6-dione性质、用途与生产工艺

生物活性 (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。
靶点

IC50: 0.6 µM (Lysophosphatidic acid acyltransferase)
STAT4
体外研究

(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.
体内研究

(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 .