fty-720 phosphate

FTY720 (S)-Phosphate 是 FTY720 的活性磷酸化对映异构体，是一种强效的鞘氨醇-1-磷酸（S1P）受体调节剂。其可与 S1P₁、S1P₃、S1P₄ 和 S1P₅ 受体亚型结合，Ki 值分别为 2.1、5.9、23 与 2.2 nM，并可诱导淋巴细胞受体内化，阻止 S1P 介导的淋巴细胞外流。FTY720 (S)-Phosphate 还能增强内皮屏障完整性，促进 Abcb1 与 Abcc1 等转运体活性，并抑制胞质磷脂酶 A2 活性，展现多重药理特性，是多发性硬化、自身免疫疾病及癌症研究中的关键分子。

VPC03090 is a Sphingosine-1-Phosphate Receptor Inhibitor. VPC03090 is an analog of FTY-720, acts as antagonist for S1PR1 and S1PR3. VPC03090-P, converted from VPC03090 through the phosphorylation by SK-2, causes a reduction in tumor growth in mice with mammary cancer, and its oral bioavailability is determined to be 30 hours.

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