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.
CYM50374 is a potent antagonist of sphingosine-1-phosphate receptor 4 (S1P4), exhibiting an IC50 value of 34 nM. This compound effectively modulates S1P4 signaling, making it valuable for research applications related to immune response and inflammation. Its selective inhibition of S1P4 provides a useful tool for studying the role of this receptor in various biological processes.
RBM10-8 is an irreversible inhibitor of recombinant human sphingosine-1-phosphate lyase (hS1PL). This compound modulates the sphingosine-1-phosphate (S1P) signaling pathway, which plays a critical role in regulating various biological processes including cell proliferation, differentiation, angiogenesis, and immune responses. RBM10-8 is valuable for research applications focused on inflammation and developmental biology, providing insights into the therapeutic potential of targeting S1P-related pathways.
RP-001 is a potent selective agonist of the S1P1 receptor (EDG1), exhibiting an EC50 of 9 pM. This compound induces internalization and polyubiquitination of the S1P1 receptor, demonstrating significant biological activity. RP-001 is primarily utilized in research applications involving S1P signaling pathways, with minimal activity on S1P2-S1P4 and only moderate affinity for S1P5.
GSK2263167 is an S1P1 receptor agonist that modulates sphingosine-1-phosphate signaling pathways. This compound demonstrates significant biological activity in promoting lymphocyte egress and can be effectively utilized in research focused on immunology, cardiovascular biology, and neurological disorders. Its ability to selectively activate S1P1 receptors makes it a valuable tool for studying S1P-mediated physiological processes.
CYM5181 is a selective agonist for the sphingosine-1-phosphate receptor 1 (S1P1). It demonstrates potent activity with a pEC50 value of -8.47, making it a valuable tool for studying S1P1-mediated signaling pathways. This compound is primarily used in research applications related to immunology, cardiovascular health, and neurobiology, facilitating investigations into the role of S1P1 in various physiological and pathological processes.
C16-Sphingosine-1-phosphate is a derivative of Sphingosine-1-phosphate, functioning as an endogenous ligand for the EDG/S1P receptor. This compound exhibits key biological activity in modulating signaling pathways related to angiogenesis and inflammation. It is a valuable reagent for research applications focused on cardiovascular diseases and related physiological processes.
VPC 23153 is a selective S1P4 receptor agonist that promotes vasoconstriction. By activating the S1P4 receptor, VPC 23153 induces contraction of the pulmonary artery. This reagent is valuable for investigating mechanisms underlying pulmonary arterial hypertension and related vascular responses in research settings.
AMG 369 is a potent, orally bioavailable dual agonist of the sphingosine-1-phosphate receptors S1P1 and S1P5, with minimal activity at S1P3 and no affinity for S1P2 or S1P4. This compound effectively reduces blood lymphocyte counts, demonstrating its immunomodulatory effects. AMG 369 has been shown to delay the onset and diminish the severity of experimental autoimmune encephalomyelitis in rat models, making it a valuable tool for research into autoimmune diseases and inflammatory responses.
BMS-960 free base is a potent and selective agonist of the S1P1 receptor, featuring an isoxazole structure. This compound demonstrates significant biological activity in modulating immune responses and has potential applications in the study of immune and vascular diseases. BMS-960 free base is a valuable tool for researchers investigating the therapeutic implications of S1P1 receptor modulation.
S1P1 agonist 6 is a selective S1P1 receptor agonist that modulates immune responses by inhibiting lymphocyte trafficking. This compound exhibits notable immunosuppressive activity, making it a valuable tool for the investigation of autoimmune diseases. Research applications include studying mechanisms of autoimmunity and evaluating potential therapeutic interventions for related disorders.
Out of stock
All 3 sizes
W123 is an S1P1 receptor antagonist derived from FTY720. This compound exhibits significant biological activity by inhibiting GTPγS activation, MAPK recruitment, and cell migration while also promoting ligand-induced receptor internalization. W123 is valuable for research applications focused on sphingosine 1-phosphate signaling pathways and their role in various physiological and pathological processes.
Out of stock
All 3 sizes
GSK1842799 is an orally active prodrug that selectively targets the S1P1 receptor. Its primary mechanism involves agonistic activity that modulates immune cell trafficking and is of particular interest in the study of multiple sclerosis. This compound is valuable for research focused on autoimmune diseases and neurological disorders.
Out of stock
All 3 sizes
TC-SP 14 is a potent and orally active S1P1 agonist, exhibiting an EC50 of 0.042 μM, while demonstrating minimal activity at S1P3 with an EC50 of 3.47 μM. This compound significantly reduces blood lymphocyte counts and attenuates delayed type hypersensitivity (DTH) responses upon antigen challenge. TC-SP 14 is valuable for research focusing on immune modulation and the therapeutic potential in autoimmune diseases.
S1PL-IN-2 is a potent sphingosine-1-phosphate lyase (S1PL) inhibitor with an IC50 of 120 nM. It effectively inhibits S1PL activity by blocking the conversion of Vitamin B6 into the active cofactor pyridoxal-4-phosphate, which is essential for S1P lyase function. This compound is valuable for research in inflammation and immunology, with potential applications in studying conditions such as rheumatoid arthritis.
Out of stock
All 3 sizes
RP-1859 is a sphingosine 1-phosphate (S1P) modulator that exhibits anti-inflammatory and immunomodulatory properties. This compound is particularly relevant in the study of iatrogenic autoimmune colitis, facilitating investigations into the underlying mechanisms of this condition and potential therapeutic interventions. RP-1859's modulation of S1P signaling pathways may provide valuable insights into inflammatory responses and immune regulation.
Out of stock
All 3 sizes
LX2932 is an orally active modulator of the sphingosine 1-phosphate (S1P) signaling axis, impacting S1PR receptor activity. It demonstrates a dose-dependent reduction in circulating lymphocyte populations, which may aid in the treatment of autoimmune disorders. LX2932 has shown efficacy in improving collagen-induced arthritis, making it a valuable compound for research in immunology and inflammatory disease models.
Out of stock
All 3 sizes
S1P1 agonist 6 hemicalcium is a selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1), primarily functioning to inhibit lymphocyte trafficking. This mechanism results in the reduction of autoimmune responses, making it a valuable tool for studying various autoimmune diseases. Its immunosuppressive properties allow researchers to investigate potential therapeutic applications in immune modulation and related research areas.
Out of stock
All 3 sizes
BMS-960 is a potent and selective agonist of the S1P1 receptor. It has been demonstrated to modulate immune responses and improve vascular function, making it a valuable tool in the study of immune and vascular diseases. Research applications include exploring pathways related to inflammation, lymphocyte trafficking, and cardiovascular health.
Out of stock
All 3 sizes
CYM50358 hydrochloride is a potent and selective antagonist of the sphingosine-1-phosphate 4 (S1P4) receptor. This compound exhibits significant biological activity by inhibiting S1P4-mediated signaling pathways, making it a valuable tool in research focused on the immune response and inflammation. Its application extends to the study of influenza infection, facilitating investigations into viral pathogenesis and potential therapeutic interventions.
S1PR1 Agonist 1 is a potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), a member of the G protein-coupled receptor family. This compound modulates cellular signaling pathways linked to immune response and inflammation, making it a valuable tool for investigating autoimmune diseases. Its application extends to research focused on understanding the role of sphingolipid signaling in various physiological and pathological conditions.
RP101442 is a selective and potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 of 2.6 nM. Additionally, it shows activity toward S1PR5 with an EC50 of 171 nM. This compound is primarily utilized in research exploring immune responses and neuroprotection, making it valuable for studies on inflammatory diseases and related therapeutic areas.
S1PR1 Agonist 2 is a potent agonist targeting the S1P receptor 1 (S1PR1). This compound, derived from sphingosine-1-phosphate (S1P), engages G protein-coupled receptors, influencing various physiological processes. S1PR1 Agonist 2 is primarily utilized in research studies focused on autoimmune diseases, facilitating the exploration of therapeutic strategies in this area.
S1P5 receptor antagonist 1 is a selective antagonist targeting the S1P5 receptor, characterized by an EC50 of 0.1 nM and a Ki of 4.4 nM. This compound is capable of inhibiting the migration of natural killer cells towards sphingosine 1-phosphate in vitro, while leaving T cell migration unaffected. S1P5 receptor antagonist 1 is employed in research focused on central nervous system diseases, providing insights into the modulation of immune responses within the brain.
Out of stock
All 3 sizes
S1PR1 ligand 1 is a specific agonist targeting the S1PR1 receptor with an IC50 of 8.7 nM. This compound demonstrates favorable brain permeability, making it suitable for exploring S1PR1 functions in neurological disorders. Additionally, S1PR1 ligand 1 can be labeled with 18F for imaging studies, facilitating research into its role in brain pathologies.
Out of stock
All 3 sizes
ACT-209905 is an agonist of the S1P1 receptor, demonstrating potent inhibition of glioblastoma (GBM) cell growth and migration. In addition to its antitumor properties, ACT-209905 exhibits immunomodulating activity, making it a valuable tool for investigating autoimmune diseases. This compound is suitable for research applications aimed at elucidating the roles of S1P1 signaling in cancer and immune regulation.
