芬戈莫德
CAS号 | 162359-55-9 | 货号 | BCP05969 |
中文名 | 芬戈莫德 | ||
英文名 | Fingolimod | ||
中文别名 | 2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇; | ||
英文别名 | FTY720 free base;Gilenya;FTY 720 free base;FTY-720 free base; | ||
分子式 | C19H33NO2 | 分子量 | 307.47 |
生物活性 | Fingolimod(FTY720 free base) is a S1P antagonist with IC50 of 0.033 nM. The inhibitory effect of S1P is revered by various concentrations of FTY720, with IC50 effect of 173 nM. In addition, FTY720 (10 nM) alone exerts no effect on the expression of co-stimulatory molecules. FTY720 reverses the increased expression of HLA-I induced by S1P for both the percentages of cells and the MFI, upon comparing the effect of S1P to the effect of combining S1P with FTY720 . Medium and high-dose FTY720-P also enhances the levels of TGF-β1. TGF-β1 and Foxp3 mRNA expression are upregulated in the high-dose FTY720-P group. The proliferation of effector T cells is suppressed significantly in the medium and high-dose FTY720-P group at a Treg/Teff cell ratio of 1:1. At a ratio of 1:1, the proliferation of effector T cells is also suppressed in the high-dose FTY720 group. FTY720 is effective in Ph+ but not Ph- ALL xenografts using an early disease model. FTY720 produces a significant reduction in disease bu | ||
信号通路 | Cell Cycle/DNA Damage GPCR/G Protein | ||
靶 点 | S1P Receptor PAK |
结构式
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