中文名 | 芬戈莫德 |
英文名 | Gilenya |
别名 | 芬戈利德 芬戈莫德 芬戈莫德碱 芬戈莫德-D4 芬格莫德及中间体 芬戈莫德 FINGOLIMOD 2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇 |
英文别名 | Gilenya Gilenia fenogliMod Fingolimod FingoliMod Base Fingolimod(FTY720) 2-(4-octylphenylethyl)-2-aminopropane-1,3-diol 2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol 2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol 1,3-Propanediol,2-aMino-2-[2-(4-octylphenyl)ethyl]- |
CAS | 162359-55-9 |
EINECS | 1308068-626-2 |
化学式 | C19H33NO2 |
分子量 | 307.47 |
密度 | 1.016 |
熔点 | 103-105° |
沸点 | 479.5±45.0 °C(Predicted) |
溶解度 | 氯仿 (非常轻微,加热),DMSO (轻微,加热),甲醇 (轻微, |
酸度系数 | 12.20±0.20(Predicted) |
存储条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | Off-White |
体外研究 | The monocyte-derived immature dendritic cells (iDCs) are pretreated with various concentrations of S1P for various periods of time prior to their incubation with NK cells. Four hours incubation of autologous or allogeneic iDCs with 0.2-20 μM of S1P significantly protectes these cells from NK cell lysis. The IC 50 values of S1P are calculated at 160 nM for autologous iDCs, and 34 nM for allogeneic iDCs. Next, the inhibitory effect of S1P is revered by various concentrations of Fingolimod or SEW2871, with an IC 50 effect of 173 or 15 nM, respectively. Fingolimod has been reported to reduce LPA synthesis via inhibition of the lysophospholipase autotaxin. Fingolimod treatment correlates with a significant elevation of axonal cAMP, a crucial factor for axonal outgrowth. Additionally, Fingolimod significantly reduces LPA levels in the injured nerve. PF-8380 treatment correlates with improved myelin thickness. |
体内研究 | Fingolimod treatment results in significantly increased nerve conduction at 14 days post-crush in wildtype C57BL/6 mice. However, Foxn1 -/- mice, which are devoid of T- but not B-lymphocytes, show an improvement of nerve regeneration under fingolimod treatment. Although the mean increase in nerve conduction velocity in both fingolimod-treated and control Foxn1 -/- mice implies a potentially positive role of T-lymphocyte deficiency on nerve regeneration, only fingolimod-treated Foxn1 -/- mice show a significant improvement compared to C57BL/6 controls and performed better in the functional analysis. Treatment of the animals with Fingolimod for 28 d results in a clear reduction in the binding of 18 F-GE180 when compare with vehicle-treated animals and evaluated by ex vivo autoradiography. Quantification of the binding of the radiotracer revealed a significant reduction in the binding potential of 18 F-GE180 (P<0.0001) after treatment with Fingolimod. |
上游原料 | N-[2,2-二甲基-5-[2-(4-辛基苯基)乙基]-1,3-二氧六环-5-基]氨基甲酸叔丁酯 2-NitrodeaMino FingoliMod 2-羟甲基-2-硝基-4-(4-辛基苯基)-1,4-丁二醇 2-乙酰胺基-2-(4-辛基苯乙基)丙烷-1,3-二基二乙酸酯 |
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