Catalog No.
Product Name
Application
Product Information
Citations
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S1PL Inhibitor
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. -
S1PR5 Antagonist, S1PR5 Inhibitor
S1PR5-IN-1 is a selective antagonist of the sphingosine-1-phosphate receptor 5 (S1PR5), exhibiting an IC50 of 85.4 nM in human assays and a binding affinity (Ka) of 2.173 nM. This orally bioavailable inhibitor effectively impedes the migration of natural killer cells towards sphingosine-1-phosphate. S1PR5-IN-1 is a valuable tool for research applications related to multiple sclerosis and other conditions involving S1PR5 signaling pathways. -
S1PR1 Antagonist
KSI-6666 is a competitive antagonist of the sphingosine 1-phosphate receptor 1 (S1PR1) with an IC50 of 6.4 nM. This compound demonstrates significant anti-inflammatory effects in models of autoimmune encephalomyelitis and T cell transfer colitis. KSI-6666 is valuable for research aimed at understanding the role of S1PR1 in inflammation and autoimmune diseases. -
S1P1 Antagonist
Ex26 is a potent and selective antagonist of the sphingosine 1-phosphate receptor 1 (S1P1), with an IC50 of 0.93 nM. This compound exhibits over 3,000-fold selectivity for S1P1 compared to other sphingosine 1-phosphate receptors, making it a valuable tool for dissecting S1P1-related pathways. Ex26 is applicable in research focused on autoimmune encephalomyelitis and related neurological disorders, providing insights into receptor function and therapeutic potential. -
S1P1 Agonist
CS-2100 is a potent and selective S1P1 agonist, demonstrating an EC50 of 4.0 nM for human S1P1 while sparing S1P3. This compound has shown in vivo immunosuppressive efficacy in rat models, with an ID50 of 0.407 mg/kg for HvGR. CS-2100 is suitable for research applications focused on immunomodulation and the investigation of S1P1 signaling pathways. -
S1P1 Agonist
IMMH001 is a potent and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1). It effectively decreases the levels of various chemokines and pro-inflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 serves as a valuable tool for research in inflammatory conditions, particularly rheumatoid arthritis (RA). -
S1P Receptor Agonist
TRV045 is a selective agonist of the sphingosine-1-phosphate receptor subtype 1, exhibiting minimal impact on lymphocyte transport. It demonstrates significant antiepileptic activity, making it a valuable tool in the study of epilepsy and related neurological disorders. Researchers can leverage TRV045 to investigate the therapeutic potential of S1P receptor modulation in various biological contexts. -
S1PR1 Agonist
RP101075 is a potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 of 0.27 nM. This compound demonstrates greater than 100-fold selectivity for S1PR1 over S1PR5 and over 10,000-fold selectivity over S1PR2, S1PR3, and S1PR4. Additionally, RP101075 is noted for its superior cardiovascular safety profile, making it a valuable tool in research focused on immunology and cardiovascular health. -
S1P Receptor Agonist
Siponimod hemifumarate is a selective sphingosine-1-phosphate (S1P) receptor modulator, primarily targeting S1P1 and S1P5 receptors. It demonstrates potency with EC50 values of 0.39 nM and 0.98 nM, respectively, while showing significantly reduced activity against S1P2, S1P3, and S1P4. This compound is essential for investigating therapeutic strategies in multiple sclerosis (MS) and related neurological disorders. -
S1P Receptor Agonist
L-threo Lysosphingomyelin (d18:1) is a bioactive sphingolipid that functions as a potent agonist of the S1P receptor. It exhibits effective activation of human S1P receptors, with EC50 values of 19.3 nM for hS1P1, 131.8 nM for hS1P3, and 313.3 nM for hS1P2. This compound is valuable in research applications related to cell signaling, immunology, and inflammation studies. -
S1PR2 Agonist
CYM-5482 is a potent and selective agonist of the Sphingosine 1-phosphate receptor 2 (S1PR2), exhibiting IC50 and EC50 values of 1.0 and 1.03 μM, respectively. This compound is valuable for investigating the role of S1PR2 in cancer biology and may contribute to the understanding of cancer pathogenesis and potential therapeutic strategies. -
S1P1 Antagonist
TASP0277308 is a highly selective antagonist of the S1P1 receptor. It displays significant immunomodulatory effects, including inducing lymphopenia, disrupting T cell egress from the thymus, and causing marginal zone B cell displacement, along with upregulating CD69 expression on lymphocytes. This compound is useful for studying collagen-induced arthritis in murine models, providing insights into the modulation of immune responses and potential therapeutic approaches. -
S1P1 Agonist
S1P1 Agonist III is a potent orally active agonist of the human sphingosine-1-phosphate receptor 1 (S1P1), exhibiting an EC50 value of 18 nM. This compound demonstrates selectivity with minimal activity against the hS1P3 receptor. S1P1 Agonist III is primarily utilized in research related to multiple sclerosis, facilitating investigations into its therapeutic potential and the modulation of immune responses. -
S1PR1 Modulator
Amiselimod is a selective sphingosine 1-phosphate receptor-1 (S1P1) modulator that is converted to its active metabolite, Amiselimod phosphate, by sphingosine kinases in vivo. Exhibiting oral bioactivity, Amiselimod effectively inhibits chronic colitis by restricting the infiltration of Th1 and Th17 colitogenic cells into the colon. Additionally, it shows potential in the treatment of lupus nephritis by decreasing the presence of autoreactive T cells in the kidneys. This compound is valuable for research into various autoimmune diseases. -
S1P Receptor Modulator
Tamuzimod is a potent S1P receptor modulator, exhibiting significant immunomodulatory effects. With an EC50 value of less than 1 μM, it effectively influences S1P receptor signaling pathways. This compound is primarily utilized in research applications focused on immune modulation and related disease models. -
S1P Agonist
ASP-4058 hydrochloride is a selective and orally active agonist of Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5). This compound has demonstrated efficacy in ameliorating rodent models of experimental autoimmune encephalomyelitis, suggesting its potential for neurological applications. Its favorable safety profile makes it a valuable tool for research into autoimmune diseases and therapies targeting S1P signaling pathways. -
S1P5 Receptor Agonist
S1P5 receptor agonist-1 is a selective agonist for the S1P5 receptor, demonstrating an EC50 of 20 nM for S1P5 and greater than 3 μM for S1P1, indicating its specificity. This compound is valuable in research focused on neuroprotection and immune regulation, facilitating studies on signaling pathways and therapeutic applications related to these processes. Its selective activation of the S1P5 receptor makes it a useful tool for elucidating mechanisms in neuroinflammation and immune responses. -
S1P1/EDG1 Receptor Agonist
Vibozilimod is a selective agonist of the S1P1/EDG1 receptor, exhibiting an EC50 of less than 1 nM. This compound effectively promotes the internalization of S1P1/EDG1 receptors, leading to the inhibition of lymphocyte migration, induction of lymphopenia, and reduction in lymphocyte counts. Vibozilimod is utilized in research related to inflammatory diseases, including psoriasis and atopic dermatitis, providing valuable insights into immune modulation and therapeutic strategies. -
S1P Modulator
Etrasimod arginine is an orally bioavailable sphingosine-1-phosphate (S1P) receptor modulator, acting as a potent full agonist at the S1P1 receptor while displaying partial agonist activity at the S1P4 receptor. This compound exhibits significant anti-inflammatory effects, demonstrated in a CD4+CD45RBhigh T cell-transferred mouse model of colitis. Etrasimod arginine is valuable for research applications targeting immune modulation and inflammatory diseases. -
S1PR5 Agonist
S1P receptor agonist 2 is a selective agonist for the S1P5 receptor, demonstrating minimal activity on S1P1 and S1P3 receptors. This compound is valuable for studying the endogenous sphingosine-1-phosphate signaling system and is relevant in investigations aimed at alleviating or preventing central nervous system disorders, including neurodegenerative diseases. Its specificity makes it a significant tool for advancing research in both neurobiology and therapeutic applications. -
S1P Agonist
Ginkgolic acid 2-phosphate is a potent agonist of sphingosine 1-phosphate (S1P), primarily targeting the S1P1 receptor. It induces phosphorylation of extracellular signal-regulated kinase (ERK), highlighting its role in modulating signaling pathways associated with cell proliferation and differentiation. This compound is valuable for research in studying S1P-mediated processes and the subsequent effects on cellular behaviors. -
S1PR1 Receptor Agonist
S1PR1 agonist 3 is a selective agonist for the S1PR1 receptor, exhibiting an EC50 of 0.98 nM. This compound has shown potential in modulating immune responses, making it a valuable tool for studying autoimmune diseases, including multiple sclerosis and ulcerative colitis. Its specificity and potency support its use in elucidating the role of S1PR1 in various biological contexts. -
S1P1 Antagonist
W140 hydrobromide is a selective antagonist of the sphingosine-1-phosphate receptor 1 (S1P1), exhibiting a Ki value of 2.84 μM. It plays a significant role in enhancing capillary leakage and facilitating the restoration of lymphocyte egress. This compound is valuable for research applications focused on immune response modulation and vascular biology. -
S1P1 Agonist
S1P1 Agonist 5 selectively targets the S1P1 receptor, demonstrating oral bioactivity. This compound effectively inhibits lymphocyte egress from lymphoid tissues into peripheral circulation, making it a valuable tool for researching multiple sclerosis (MS) and related immunological disorders. -
S1P1 Agonist
BMS-520 is a selective sphingosine-1-phosphate 1 (S1P1) agonist with an EC50 of 0.47 nM, exhibiting approximately 3400-fold selectivity over S1P3. This compound has been shown to possess significant efficacy in models of arthritis and experimental autoimmune encephalomyelitis (EAE), making it valuable for research in autoimmune diseases. BMS-520 is a promising tool for studying the therapeutic potential of S1P1 modulation in various inflammatory conditions. -
S1P1R Modulator
Udifitimod (BMS-986166) is a selective, orally active modulator of the sphingosine-1-phosphate receptor 1 (S1P1R). This compound demonstrates significant potential in the modulation of immune responses, making it valuable for research focused on autoimmune diseases. Its ability to influence lymphocyte egress and migration underscores its relevance in therapeutic investigations. -
S1P4 Antagonist
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. -
hS1PL Inhibitor
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. -
S1P1 Agonist
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. -
S1P1 Receptor Agonist
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. -
S1P1 Agonist
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. -
EDG/S1P Receptor Ligand
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. -
S1P4 Receptor Agonist
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. -
S1P1/S1P5 Agonist
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. -
S1P1 Receptor Agonist
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
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. -
S1P1 Antagonist
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. -
S1P1 Receptor Agonist Prodrug
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. -
S1P1 Agonist
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 Inhibitor
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. -
S1P Modulator
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. -
S1P/S1PR Signaling Axis Modulator
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. -
S1P1 Agonist
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. -
S1P1 Receptor Agonist
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. -
S1P4 Receptor Antagonist
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
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. -
S1PR1 Agonist
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
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
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. -
S1PR1 ligand
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.
