fty720

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

Fingolimod (FTY-720A) 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。它还是pak1激活剂和免疫抑制剂。

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.

FTY720-C2 is an FTY720 analog. It acts as an effective stimulator of the activity of the protein phosphatase 2A.

(R)-FTY720-OMe is a structural analogue of FTY720 which acts as a specific competitive inhibitor of sphingosine kinase 2 (SK2). Furthermore, (R)-FTY720-OMe does not inhibit sphingosine kinase 1 (SK1) activity.

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.

MP07-66 是 FTY720 的一种类似物，没有免疫抑制作用。MP07-66通过破坏 SET-PP2A 复合物导致PP2A 重新激活。MP07-66在慢性淋巴细胞白血病中显示出良好的抗肿瘤作用。

FTY720-Mitoxy is an FTY720 analog that can be uesd as a novel stimulator of the activity of the protein phosphatase 2A (PP2A), targeting mitochondria.

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.

(R)-FTY-720 Vinylphosphonate is a sphingosine 1-phosphate type 1 (S1P1) receptor agonist and lacks anti-apoptotic activity.

(S)-FTY-720 Vinylphosphonate inhibits sphingosine kinase 1 and promotes its proteasomal degradation in human pulmonary artery smooth muscle, breast cancer cells, and androgen-independent prostate cancer cells.

BMS-986104是一种选择性很高的S1P1受体调节剂，具有显著的疗效。在小鼠EAE模型中，它的效果可与FTY720媲美。此外，在三维脑细胞培养中针对溶血磷脂酰胆碱(LPC)诱导的脱髓鞘现象，BMS-986104也展示了有效的再髓鞘能力。

AAL-149 是 FTY720 的类似物和一种 TRPM7 抑制剂 (IC50= 1.081 μM)，具有多重抗炎作用，不靶向 S1P 受体，适用于抗炎研究。