sphingosine 1-phosphate (s1p)

Ozanimod (RPC-1063) 是一种选择性S1P1和S1P5受体激动剂，在[35S]-GTPγS 结合实验中，EC50分别为 410 pM 和 11 nM。它可研究治疗克罗恩病、溃疡性结肠炎、多发性硬化症和复发性多发性硬化症的试验。

Sphingosine-1-phosphate (S1P) 是 S1P1-5 受体 (S1P1-5 receptors) 的激动剂和 GPR3、GPR6、GPR12 的配体。Sphingosine-1-phosphate 是细胞内的第二信使，动员 Ca2+ 作为 G 蛋白偶联受体的细胞外配体。Sphingosine-1-phosphate 是由鞘磷脂或其他膜磷脂生成的重要脂质介质。

LX-2931(LX-3305) 是一种鞘氨醇-1-磷酸裂解酶（S1P）抑制剂，可用于治疗类风湿性关节炎。

TASP 0277308 是一种具有选择性和高效性的鞘氨醇 1-磷酸受体 1( S1P1) 抑制剂，具有免疫调节活性和抗癌活性，抑制 S1P- 以及 VEGF 诱导的细胞反应，阻断 VEGF 诱导的管形成。TASP 0277308 可用于研究免疫疾病和心血管疾病。

SLP9101555 是一种有效且具有选择性的鞘氨醇激酶 2（SphK2）抑制剂，Ki 为90 nM。SLP9101555对SphK2具有很高的亲和力，是 SphK1 的 200 倍。SLP9101555 显著降低细胞外 S1P 鞘氨醇 1- 磷酸（S1P）水平。

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。

4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。

ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist (EC50s: 7.12 nM, 517 nM for hS1P1 and hS1P3).

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) 是一种具有选择性和高效性的鞘氨醇激酶 1 （SPHK1）抑制剂，也是高效性的 1-磷酸鞘氨醇 (S1P) 形成抑制剂，具有抗癌、抗纤维化和抗炎活性，可用于研究直肠癌。

Cenerimod (ACT-334441) 是一种具有口服活性、选择性和高效性的磷酸鞘氨醇 1 受体（S1P1）激动剂（EC50：1 nM）。Cenerimod 对多种 S1P 的亚型具有抑制作用，可用于研究鼠类实验性自身免疫性脑脊髓炎 (EAE)和鼠类硬皮病。

Ceralifimod (ONO-4641) is a potent agonist for sphingosine 1-phosphate receptors 1 and 5 (EC50s: 27.3, 334 pM for human S1P receptor 1 and 5).

TRV045 是一种选择性激活鞘氨醇-1-磷酸 (sphingosine-1-phosphate) 亚型 1 受体的激动剂，并且不会影响淋巴细胞运输。TRV045 显示出抗癫痫活性。

ML-178 是一种二氯苯，是鞘氨醇-1-磷酸受体4（S1PR4）的强效选择性激动剂，EC50 为 46 nM，在25 μM 的浓度下对其他 S1P 受体没有影响。

Ex26 (S1P1-IN-Ex26) 是一种具有选择性和高效性的 sphingosine 1-phosphate receptor 1 (S1P1) 拮抗剂，可破坏 SR-B1-S1PR1相互作用，抑制 S1P-S1PR1 信号转导。Ex26 可用于实验性自身免疫性脑脊髓炎、动脉粥样硬化和胃癌。

SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat

A6770 is an inhibitor of sphingosine-1-phosphate (S1P) lyase.1It induces accumulation of [3H]sphinganine-1-phosphate ([3H]dhS1P), an S1P lyase substrate, in IT-79MTNC3 cells that endogenously express high levels of S1P lyase (EC50= <0.01 μM), an effect that is reduced in the presence of vitamin B6(EC50= <100 μM). 1.Ohtoyo, M., Tamura, M., Machinaga, N., et al.Scintillation proximity assay to detect the changes in cellular dihydrosphingosine 1-phosphate levelsLipids51(10)1207-1216(2016)

Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (ORG1) that induces calcium accumulation in cells overexpressing OGR1 (EC50= ~35 nM).4Levels of D-erythrolysosphingomyelin are increased in skin isolated from patients with atopic dermatitis, as well as postmortem brain from patients with Niemann-Pick disease type A, but not type B.2,5L-threolysosphingomyelin is also an S1P1-3agonist (EC50s = 19.3, 131.8, and 313.3 nM, respectively).3This product is a mixture of D-erythroand L-threolysosphingomyelin. [Matreya, LLC. Catalog No. 1321] 1.Ito, M., Kurita, T., and Kita, K.A novel enzyme that cleaves the N-acyl linkage of ceramides in various glycosphingolipids as well as sphingomyelin to produce their lyso formsJ. Biol. Chem.270(41)24370-24374(1995) 2.Nixon, G.F., Mathieson, F.A., and Hunter, I.The multi-functional role of sphingosylphosphorylcholineProg. Lipid Res.47(1)62-75(2008) 3.Im, D.-S., Clemens, J., Macdonald, T.L., et al.Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): Structure-activity relationship of sphingosine1-phosphate receptorsBiochemistry40(46)14053-14060(2001) 4.Meyer zu Heringdorf, D., Himmel, H.M., and Jakobs, K.H.Sphingosylphosphorylcholine-biological functions and mechanisms of actionBiochim. Biophys. Acta1582(1-3)178-189(2002) 5.Rodriguez-Lafrasse, C., and Vanier, M.T.Sphingosylphosphorylcholine in Niemann-Pick disease brain: Accumulation in type A but not in type BNeurochem. Res.24(2)199-205(1999)

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.

C16 Sphingosine-1-phosphate (C16 S1P) is a derivative of sphingosine-1-phosphate that binds to S1P1/EDG-1, S1P3/EDG-3, and S1P2/EDG-5 receptors with affinities of 115%, 83%, and 103%, respectively, relative to S1P in CHO cells. C16 S1P was increased in postmortem primary open angle glaucoma trabecular meshwork samples.

Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1 EDG-1, S1P2 EDG-5, S1P3 EDG-3, S1P4 EDG-6, and S1P5 EDG-8. W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 μM (2a = W146; 2b = W140 in supplemental material). It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.

SAR247799（S1P1 agonist 3）是一种选择性和G蛋白偏向性的S1P1激动剂，比β-阻滞蛋白和内化信号通路更优先激活下游G蛋白信号通路，激活内皮细胞上的S1P 1 而不引起受体脱敏，可以保护内皮细胞而不影响淋巴细胞数量，可用于研究2型糖尿病、内皮功能障碍和血管高通透性。

Ozanimod hydrochloride (RPC-1063 hydrochloride) 是一种可口服且具有选择性和高效性的鞘氨醇 1-磷酸 (S1P) 受体调节剂，对S1P1 和 S1P5显示出较高的亲和力。Ozanimod 具有潜在的抗癌活性，可用于研究复发性多发性硬化 (MS) 、溃疡性结肠炎、冠状病毒感染和骨髓增生。

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)。