s1p4

CYM50374 inhibits Sphingosine-1-phosphate receptor 4 (S1P4 ) with an IC50 of µM.

CYM50308 is a high affinity agonist of sphingosine-1-phosphate receptor 4 (S1P4-R) (EC50: 56 nM). CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM and it shows 37-fold more selective for S1P4-R than S1P5-R.

BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits >1000-fold over S1P2, S1P3 and S1P4 receptors.

CYM50260 is a potent and highly selective agonist of the sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM), exhibiting no activity against S1P1-R, S1P2-R, S1P3-R, and S1P5-R.

CYM50358 HCl is an S1P4 antagonist.

RP-001 is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

RP-001 hydrochloride is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

Cenerimod (ACT-334441) is an orally active, selective, and potent sphingosine 1-phosphate receptor (S1P1) agonist (EC50: 1 nM).Cenerimod inhibits multiple S1P isoforms and can be used to study murine experimental autoimmune encephalomyelitis (EAE) and murine scleroderma.

VPC 23019 is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively). It is also an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).

ML-178, a dichlorobenzene, is a potent and selective agonist of sphingosine-1-phosphate receptor 4 (S1PR4), with an EC50 of 46 nM, and has no effect on other S1P receptors at a concentration of 25 μM.

CYM-5478 is a potent and selective S1P2 agonist that significantly increases the viability of C6 cells in a dose-dependent manner at concentrations above 100 nM under nutrient-deprivation stress (produced by serum-starvation).

Ponesimod (ACT-128800) is an orally available sphingosine-1-phosphate receptor 1 (S1PR1, S1P1) agonist with potential immunomodulating activity.

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.

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.

Sphinganine 1-phosphate is an intermediate in the sphingolipid metabolic pathway and is structurally similar to sphingosine. It has a protective effect on the kidney and liver through activation of the S1P1 receptor in mice. D-erythro-Dihydrosphingosine 1-phosphate acts as an agonist for S1P4 in Homo sapiens and may activate GPR63 (G protein-coupled receptor), mainly used in the study of Fabry disease, Gaucher disease, Krabbe disease and Leukodystrophy.

Siponimod (BAF-312) hemifumarate, a selective and potent modulator of sphingosine-1-phosphate (S1P) receptors, can be used in the study of multiple sclerosis (MS).

N-(4-(aminomethyl)-2,6-dimethylphenyl)-5 is a potent, selective antagonist of the sphingosine-1-phosphate receptor 4 (S1P4). CYM50358 inhibits S1P4 with an IC50 of 25 nM.