Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Sphingosine-1-phosphate (S1P) receptor modulators act on S1PR1 to S1PR5, five G protein-coupled lipid receptors. In 1998 S1P was identified as a ligand of the orphan receptor endothelial differentiation gene 1 (EDG-1), now called S1PR1. FTY720 (fingolimod) was shown in 2002 to be phosphorylated in vivo and to act on four of the five S1P receptors. Two years later, lymphocyte egress from thymus and lymph nodes was found to depend on S1PR1. Ozanimod, BAF312 and ponesimod are further S1PR1-directed modulators, CYM 5442 HCl is a selective S1PR1 agonist and TY-52156 blocks S1PR3. Opaganib inhibits sphingosine kinase 2 (SphK2) and so limits S1P synthesis upstream of the receptors.
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 value of 398 nM. This compound is instrumental in studying the role of S1PR1 in various biological processes, including immune modulation and cardiovascular function. W146 TFA is valuable for research applications involving cytokine signaling and cellular proliferation pathways.
AB1 is a highly selective antagonist of the sphingosine-1-phosphate receptor 2 (S1P2) with an IC50 of 3.5 nM. It effectively inhibits S1P signaling pathways, leading to the suppression of tumor cell migration, angiogenesis, and the expression of the profibrotic mediator CTGF, while promoting apoptosis in cancer cells. This compound demonstrates significant potential for research focused on solid tumors and their microenvironment.
Out of stock
All 3 sizes
(S)-FTY-720 Vinylphosphonate is a chiral phosphonate analogue of Fingolimod that functions as an S1P1 receptor agonist. It demonstrates significant biological activity, activating the S1P1 receptor with an EC50 of 75 nM and effectively inhibiting Camptothecin-induced apoptosis in IEC-6 cells. This reagent is relevant for research into autoimmune diseases, providing insights into therapeutic mechanisms and potential interventions.
Pro-FTY is a sphingosine-1-phosphate (S1P) inhibitor functioning as an anticancer prodrug derived from FTY720. It selectively disrupts S1P signaling in cancer cells using a drug delivery system that reacts with acrolein, demonstrating significant cytotoxic effects on breast cancer cells, including multidrug-resistant variants. Pro-FTY effectively suppresses tumor growth in xenograft models with 4T1 cells and organoids, while maintaining immune cell integrity by avoiding lymphocytopenia. This reagent is valuable for research in cancer therapy and resistance mechanisms.
Out of stock
All 3 sizes
S118 is an orally active inhibitor of the sphingosine-1-phosphate receptor 2 (S1P2 receptor), which blocks the binding of Dpr1, subsequently reducing β-catenin accumulation. This mechanism inhibits nuclear translocation of the S1P2 receptor, contributing to the attenuation of inflammation, fibrosis, and epithelial-mesenchymal transition (EMT). S118 demonstrates potential for use in research related to idiopathic pulmonary fibrosis (IPF) and other fibrotic diseases.
Out of stock
All 3 sizes
Synonyms: S1P
Sphingosine-1-phosphate (S1P) functions as an agonist of S1P1-5 receptors and acts as a ligand for GPR3, GPR6, and GPR12. It serves as an intracellular second messenger, promoting calcium mobilization and influencing various cellular processes. As a key lipid mediator derived from sphingomyelin and other membrane phospholipids, Sphingosine-1-phosphate plays a crucial role in stimulating DNA synthesis, cell proliferation, and migration, making it valuable for studies in cell signaling and cell biology research.
(S)-PF-462991 is a selective agonist of the S1P1 and S1P5 receptors. It exhibits key biological activity by modulating sphingosine 1-phosphate signaling pathways, which are crucial for immune cell trafficking and vascular integrity. This compound is primarily utilized in research to investigate its effects on inflammation, neuroprotection, and cardiovascular health.
Out of stock
All 3 sizes
Synonyms: APD334
Etrasimod is a potent and selective antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor, demonstrating an IC50 value of 1.88 nM in CHO cells. This orally bioavailable compound is primarily utilized in research focused on autoimmune diseases and cardiovascular conditions, where modulation of S1P signaling plays a crucial role in cell trafficking and inflammation. Its specificity makes it a valuable tool for exploring the therapeutic potential of S1P1 receptor inhibition.
CYM-5520 is a selective allosteric agonist of the sphingosine 1-phosphate receptor 2 (S1PR2), exhibiting an EC50 of 480 nM. It specifically activates S1PR2 without influencing S1PR1, S1PR3, S1PR4, and S1PR5. CYM-5520’s unique mechanism allows for co-binding with sphingosine 1-phosphate (S1P) at the S1PR2 site. This compound is valuable for research applications related to osteoporosis and the modulation of related signaling pathways.
Synonyms: S1P1 agonist 3
SAR247799 is a selective S1P1 agonist that acts through G-protein-biased signaling. It exhibits oral bioactivity with EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and human umbilical vein endothelial cells (HUVECs). This compound is valuable for research into endothelial protection mechanisms, particularly in the context of type 2 diabetes and metabolic syndrome.
Synonyms: FTY720 phosphate
Fingolimod phosphate is an orally active sphingosine 1-phosphate (S1P) receptor agonist. This compound is known to enhance the neuroprotective activities of microglia, making it a valuable tool in the study of neuroinflammation. Fingolimod phosphate is primarily used in research related to multiple sclerosis and other neurological disorders.
Synonyms: BML-241
CAY10444 is an antagonist of the sphingosine-1-phosphate receptor 3 (S1P3). This compound effectively inhibits S1P-induced calcium ion (Ca2+) increases by 37% in HeLa cells that express S1P3 receptors. It serves as a valuable tool for research into S1P3-related signaling pathways and their implications in various physiological and pathological processes.
CYM50358 is a potent and selective antagonist of the sphingosine-1-phosphate receptor 4 (S1PR4), exhibiting an IC50 of 25 nM. This compound serves as a valuable tool for investigating the role of S1PR4 in various biological processes, including its implications in influenza infection research. Its selective inhibition of S1PR4 allows for detailed mechanistic studies and potential therapeutic applications in related inflammatory diseases.
GLPG2938 is a potent and selective antagonist of the sphingosine-1-phosphate receptor 2 (S1P2). This compound demonstrates significant efficacy in inhibiting S1P2-mediated signaling pathways, making it a valuable tool for investigating mechanisms underlying idiopathic pulmonary fibrosis. Researchers can utilize GLPG2938 to explore its therapeutic potential and role in fibrotic disease models.
Synonyms: MT-1303 hydrochloride
Amiselimod hydrochloride is a selective sphingosine 1-phosphate receptor-1 (S1P1) modulator that is converted in vivo to its active metabolite, amiselimod phosphate. It is orally active and designed to minimize bradycardia effects commonly seen with other S1P receptor modulators. Key biological activities include the inhibition of chronic colitis through the reduction of Th1 and Th17 cell infiltration into the colon, as well as the suppression of autoreactive T cell infiltration in lupus nephritis. Amiselimod hydrochloride is of considerable interest for research in autoimmune diseases.
CYM-5478 is a potent and highly selective sphingosine-1-phosphate receptor 2 (S1P2) agonist, demonstrating an EC50 of 119 nM in TGFα shedding assays. This compound exhibits significant protective effects on neural-derived cell lines against Cisplatin-induced toxicity. Its applications include investigating the role of S1P2 in neural cell protection and exploring potential therapeutic strategies for mitigating chemotherapy-induced neurotoxicity.
Synonyms: RPC-1063 hydrochloride
Ozanimod hydrochloride, an S1P receptor modulator, selectively binds to sphingosine 1-phosphate receptor subtypes 1 (S1P1) and 5 (S1P5) with high affinity, exhibiting EC50 values of 1.03 nM and 8.6 nM, respectively. This compound demonstrates immunomodulatory effects, making it relevant for investigating mechanisms of action in relapsing multiple sclerosis (MS). Ozanimod hydrochloride serves as a valuable tool for research focused on S1P receptor signaling pathways and their implications in autoimmune disorders.
2-Acetyl-4-tetrahydroxybutyl imidazole is a potent inhibitor of sphingosine-1-phosphate (S1P) lyase, demonstrating significant biological activity in vivo. This compound is useful for investigating the role of S1P metabolism in various physiological and pathological processes. Research applications include studying cell signaling pathways and exploring therapeutic targets in diseases related to S1P dysregulation.
RP101988 is a potent and selective agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 of 0.19 nM for S1PR1. Additionally, it demonstrates moderate activity at S1PR5 with an EC50 of 32.8 nM. This compound is valuable for research into immune modulation and inflammation pathways, making it a useful tool for studying S1PR1-related physiological processes and potential therapeutic applications.
CYM50260 is a highly selective agonist for the sphingosine-1-phosphate receptor 4 (S1P4-R), exhibiting an EC50 value of 45 nM. This compound demonstrates no activity against other S1P receptors, including S1P1-R, S1P2-R, S1P3-R, and S1P5-R. CYM50260 is primarily utilized in research applications focused on immune regulation and modulation of signal transduction pathways involving the S1P4 receptor.
A-971432 is a selective agonist for the sphingosine-1-phosphate receptor 5 (S1P5), exhibiting IC50 values of 0.006 μM for S1P5, and demonstrating significantly lower activity for S1P1 and S1P3. This compound has shown efficacy in preserving blood-brain barrier (BBB) integrity and has potential therapeutic effects in reversing age-related cognitive decline. A-971432 is a valuable tool for research applications related to neurodegenerative diseases, including Alzheimer's disease and multiple sclerosis.
LX2931 is an inhibitor of Sphingosine 1-Phosphate Lyase (S1PL), which functions by elevating levels of Sphingosine 1-Phosphate (S1P) both intracellularly and extracellularly. This inhibition results in a marked increase in S1P concentrations in lymphoid tissues, potentially leading to restricted lymphocyte trafficking from secondary immune sites and contributing to lymphocytopenia and immunosuppressive effects in the peripheral circulation. LX2931 is valuable for research in autoimmune disease studies, particularly in the context of rheumatoid arthritis.
CYM50179 is a selective agonist of the Sphingosine-1-phosphate receptor 4 (S1P4-R), exhibiting a potency with an EC50 of 46 nM. This compound has notable biological activity in modulating immune responses and is utilized in research applications related to immunology and neurobiology. Its ability to selectively activate S1P4-R makes it a valuable tool for studying receptor signaling pathways and related physiological processes.
RP-001 hydrochloride is a potent and selective agonist of the S1P1 receptor, exhibiting a remarkable EC50 of 9 pM. This compound promotes the internalization and polyubiquitination of S1P1, making it valuable for studies in cell signaling and receptor regulation. RP-001 hydrochloride shows minimal activity on S1P2-S1P4 receptors and moderate affinity for S1P5, thereby enabling focused investigations on S1P1-mediated pathways in various biological contexts.
A6770 is a potent inhibitor of sphingosine 1-phosphate lyase (S1PL), an enzyme involved in sphingolipid metabolism. As an orally active compound, A6770 is phosphorylated to exert direct inhibitory effects on S1PL, leading to an increase in [3H]dhS1P levels. This reagent is valuable for research applications focused on sphingolipid signaling pathways and their roles in various biological processes.
