fty720 phosphate

FTY720 (S)-Phosphate is an S1P receptor 1 (S1PR1) agonist. It is used in the research of acute inflammatory diseases such as acute lung injury.

Fingolimod hydrochloride (FTY720) 是一种新型免疫调节剂，是一种 1-磷酸鞘氨醇(S1P) 拮抗剂，作用于 K562 和 NK 细胞，IC50为 0.033 nM。它诱导 S1P1 的内化，从而抑制 S1P 活性。它被鞘氨醇激酶磷酸化，尤其是被 SK2 磷酸化，从而可与 S1PR1、3、4 和 5 结合

FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs. FTY720 is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Down-regulation of S1P1 receptors on T and B lymphocytes by FTY720 results in defective egress of these cells from spleen, lymph nodes, and Peyer's patch. azido-FTY720 is a highly photoreactive analog of FTY720 that can be used to identify receptor binding sites for this ligand.

FTY720 (S)-Phosphate，作为S1P受体1 (S1PR1) 激动剂，可用于研究急性肺损伤等急性炎症。

FTY720, an immune modulator, down-regulates sphingosine-1-phosphate (S1P) receptors, enhances the activity of sphingosine transporter Abcb1 and leukotriene C4 transporter Abcc1, and inhibits cytosolic phospholipase A2 activity. Its efficacy relies on in vivo phosphorylation by sphingosine kinases, resulting in FTY720-phosphate which also down-regulates S1P receptors. NBD-FTY720, a fluorescently-labeled analog of FTY720, retains the hydroxy methyl side chain targeted for phosphorylation, suggesting potential phosphorylation in vivo.