| 货号 | 10006408-10mg |
| 描述 | FTY720 is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.1 FTY720 is phosphorylated by sphingosine kinases in vivo, and then acts as a potent agonist at four of the five sphingosine-1-phosphate (S1P) receptors.2 FTY720 (S)-phosphate is the single stereoisomer formed by phosphorylation of FTY720 in vivo, as determined in rats and humans.3 It exhibits Ki values of 2.1, 5.9, 23, and 2.2 nM for S1P1,3,4,5, respectively, whereas the R enantiomer binds with 5 to 130-fold lower affinity.4 FTY720 (S)-phosphate causes internalization of S1P1 on lymphocytes, abrogating S1P-dependent egress of lymphocytes from lymphoid organs.5 It also enhances endothelial barrier function,5 stimulates the activity of the sphingosine transporter Abcb1 and the leukotriene C4 transporter Abcc16 and inhibits cytosolic phospholipase A2activity.7 |
| 别名 | (S)-FTY 720P; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Brinkmann, V.,Pinschewer, D.D.,Feng, L., et al. FTY720: Altered lymphocyte traffic results in allograft protection. Transplantation 72, 764-769 (2001). 2.Brinkmann, V.,Davis, M.D.,Heise, C.E., et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. The Journal of Biological Chemisty 277(24), 21453-21457 (2002). 3.Albert, R.,Hinterding, K.,Brinkmann, V., et al. Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer. Journal of Medicinal Chemistry 48, 5373-5377 (2005). 4.Kiuchi, M.,Adachi, K.,Tomatsu, A., et al. Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate. Bioorganic & Medicinal Chemistry 13, 425-432 (2005). 5.Brinkmann, V. FTY720: Mechanism of action and potential benefit in organ transplantation. Yonsei Medical Journal 45(6), 991-997 (2004). 6.Honig, S.M.,Fu, S.,Mao, X., et al. FTY720 stimulates multidrug transporter- and cysteinyl leukotriene-dependent T cell chemotaxis to lymph nodes. Journal of Clinical Investigation 111(5), 627-637 (2003). 7.Payne, S.G.,Oskeritizian, C.A.,Griffiths, R., et al. The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors. Blood 109(3), 1077-1085 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 387.5 |
| 分子式 | C19H34NO5P |
| CAS号 | 402616-26-6 |
| 稳定性 | ≥ 2 years |
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