s1pr3

S1PR1 modulator 1 是 S1PR1 的特异性抑制剂，pIC50 为 7.6。

Ponesimod (ACT-128800) 是一种选择性 S1P1可口服激动剂，在放射性配体结合试验中的 IC50值为 6 nM。它可高效激活 S1P1介导的信号转导，EC50为5.7 nM。它可预防淋巴细胞介导的组织炎症，具有潜在的免疫调节活性。

Siponimod (BAF-312) 是有效，选择性的鞘氨醇-1-磷酸 (S1P)受体调节剂，对 S1P1 和 S1P5 受体具有特异性，EC50 分别为 0.39 nM 和 0.98 nM。 BAF312 对 S1P1 和 S1P5 受体的特异性比 S1P2、S1P3 和 S1P4 受体高 1000 倍以上。

TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1].

Siponimod (BAF-312) hemifumarate 是一种选择性的、有效的鞘氨醇 -1- 磷酸 (S1P) 受体调节剂。Siponimod hemifumarate 对 S1P1 受体 (EC50: 0.39 nM) 和 S1P5 受体 (EC50: 0.98 nM) 的选择性高于 S1P2 (EC50>10000 nM)、S1P3 (EC50>1000 nM) 和 S1P4 (EC50: 750 nM) 。Siponimod hemifumarate 能够用于研究多发性硬化症 (MS)。

Benzyl butyl phthalate (1,2-benzenedicarboxylic acid) 是邻苯二甲酸酯的一员，可激活乳腺癌细胞中的芳香烃受体，刺激 SPHK1 S1P S1PR3 信号传导，促进转移性乳腺癌干细胞的形成。它通过上调 Zeb1 的表达，可引起血管瘤细胞的迁移和侵袭。

CYM-5478 is a potent and selective S1P2 agonist. Under nutrient-deprivation stress produced by serum-starvation, CYM-5478 induced a significant increase in the viability of C6 cells in a dose dependent manner at concentrations above 100 nM.

L-threo Lysosphingomyelin (d18:1) (L-threo-Sphingosylphosphorylcholine) is a naturally occurring bioactive sphingolipid. It acts as a potent agonist for S1P receptors, with EC50 values of 19.3, 131.8, and 313.3 nM for hS1P1, hS1P3, and hS1P2, respectively.

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.