s1p

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

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).

4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhibits sphingosine-1-phosphate (S1P) lyase and reduces cyclic stretch-induced apoptosis in alveolar epithelial MLE-12 cells. 4-DPD (5 mg, i.p.) reduces lysyl oxidase activity by 26% and reduces collagen and elastin crosslinking, resulting in limb abnormalities in chick embryos. It decreases latency to first seizure in mice (ED50 = 1 mmol kg) and increases the occurrence and duration of myoclonic responses in baboons with photosensitive epilepsy. 4-DPD reduces TNF-α and IL-6 production in mice infected with T. spiralis.

PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P, with an IC50 of 175 nM.

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

Ozanimod hydrochloride (RPC-1063 hydrochloride) is an orally available, selective and potent sphingosine 1-phosphate (S1P) receptor modulator that shows high affinity for S1P1 and S1P5.Ozanimod has potential anticancer activity and can be used in the study of multiple sclerosis (MS), ulcerative multiple sclerosis (UMS), and other diseases. (MS), ulcerative colitis, coronavirus infections and myelodysplasia.

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.

S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.

S1P receptor agonist 2 (compound 1) is a selective agonist of the S1P5 receptor, exhibiting higher selectivity than for S1P1 and or S1P3 receptors. It is useful in the endogenous SIP signaling system and for mitigating or preventing central nervous system (CNS) diseases, including neurodegenerative diseases.

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

S1PR1 agonist 2 is a potent activator of S1PR1 with potential applications in autoimmune disease research.

S1PR1 agonist 1 is a potent activator of S1PR1 with potential applications in autoimmune diseases.

S1PL-IN-31 is a dual-function chemical compound acting as an inhibitor of sphingosine-1-phosphate (S1P) lyase with an IC50 value of 210 nM and as an antagonist of the Smoothened (Smo) receptor with an IC50 of 440 nM. Demonstrating therapeutic potential, this compound, at a dosage of 2 mg/kg per day, effectively mitigates cervical and thoracic lymphocyte infiltration and neuromuscular weakness in rats suffering from experimental autoimmune encephalomyelitis (EAE), a condition triggered by the MOG29-152 peptide from myelin oligodendrocyte glycoprotein. Additionally, it significantly decreases the total lymphocyte count, including reductions in subsets of CD4+ T cells, CD8+ T cells, and B cells. At a higher dosage of 100 mg/kg, S1PL-IN-31 elevates S1P levels within the heart and lymph nodes, while doses of 3 and 10 mg/kg per day notably lower heart rates in female rats, showcasing its multifaceted biological impacts and potential for clinical application.

S1PR-MO-1 is a modulator of sphingosine-1-phosphate receptor and is used to study hyperproliferative inflammatory diseases.

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

S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist used in the treatment of fibrotic diseases.

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).

S1P5 Receptor Agonist-1 (example 6) is a highly potent and selective agonist for the S1P5 receptor, exhibiting an EC50 value of 20 nM.

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].

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.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.