S1P1

Sphingosine-1-phosphate (S1P) is an agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, and GPR12. As an intracellular second messenger, it mobilizes Ca2+ and acts as an extracellular ligand for G-protein coupled receptors. This important lipid mediator is generated from sphingosine or other membrane phospholipids.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

AMG-369 (AMG 247) is an S1P1 S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats. encephalomyelitis in rats.

TASP 0277308 is a selective and potent inhibitor of sphingosine 1-phosphate receptor 1 ( S1P1) with immunomodulatory and anticancer activity that inhibits S1P- as well as VEGF-induced cellular responses and blocks VEGF-induced tube formation. TASP 0277308 is used in the study of immune and cardiovascular disorders.

Amiselimod hydrochloride (MT-1303 hydrochloride) is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.

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.

CYM5442 is an S1P agonist, targeting to Sphingosine.

Ex26 (S1P1-IN-Ex26) is a selective and potent sphingosine 1-phosphate receptor 1 (S1P1) antagonist that disrupts SR-B1-S1PR1 interactions and inhibits S1P-S1PR1 signaling. Ex26 is used in experimental autoimmune encephalomyelitis, atherosclerosis, and gastric cancer.

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

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.

Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclerosis.

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor (IC50: 1.88 nM in CHO cells).

S1P1 Agonist III is an effective and orally active S1P1 agonist (EC50: 18 nM).

S1P1 agonist 4 exhibits enhanced potency with an EC 50 value of less than 0.05 mg kg and a predicted human half-life (t1 2) of approximately 5 days, indicating a favorable pharmacological profile.

S1P1 agonist 5 is a selective, orally active S1P1 agonist. S1P1 agonist 5 inhibits the drainage of lymphocytes from lymphoid tissue into peripheral blood. S1P1 agonist 5 has potential for studies in multiple sclerosis (MS).

Compound I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive agent in autoimmune disease research [1].

Compound I (S1P1 agonist 6 hemicalcium) is an S1P1 agonist that diminishes autoimmune activity by inhibiting lymphocyte trafficking, and serves as an immunosuppressive agent in researching a range of autoimmune diseases [1].

ASP-4058 is a selective, safe, and orally active second-generation agonist of sphingosine phosphate receptors 1 and 5 (S1P1 and S1P5).ASP-4058 ameliorates experimental autoimmune encephalomyelitis in mice.

GC7 Sulfate is a potent inhibitor of deoxyhypusine synthase (DHS). Eukaryotic translation initiation factor 5A2 (eIF5A2) is the only known substrate for DHS, so GC7 inhibits the activation of eIF5A2 by inhibiting DHS activity.

S1PR1 modulator 1 is a selective inhibitor of S1PR1, with a pIC50 of 7.6.

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.

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

[(3S)-3-amino-4-(3-hexylanilino)-4-oxobutyl]phosphonic acid;hydrobromide is a S1P1 antagonist with Ki of 2.84 μM.

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).