Catalog No.
Product Name
Application
Product Information
Citations
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S1PR1 modulators
RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases.- Alessia Favaron, .et al. , Eur J Pharm Sci, 2024, Sep 1:200:106845 PMID: 38971433
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S1P inhibitor
PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.- Shiying Xie, .et al. , FEBS J, 2024, Apr;291(7):1575-1592 PMID: 38243371
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S1P Receptor antagonist
FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.- Tina Sepasi, .et al. , Int J Pharm, 2023, Apr 5;636:122815 PMID: 36907279
- Tina Sepasi, .et al. , BioImpacts, 2022, 28 May PMID: 37193076
- Zengzi Zhou, .et al. , Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. , Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. , Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. , Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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S1P1 Receptor Agonist
(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. -
S1PR Regulator
Mocravimod is a sphingosine-1-phosphate receptor (S1PR) modulator that inhibits the signaling necessary for T cell egress from lymph nodes and other lymphoid tissues. It preferentially binds to S1PR1, exhibiting beneficial effects such as a reduction in reactive oxygen species (ROS) levels, prevention of mitochondrial permeability transition pore opening, and enhancement of mitochondrial membrane potential (MMP). Additionally, Mocravimod promotes the phosphorylation of key signaling proteins including AKT, ERK, GSK-3β, JAK2, and STAT3, while preserving T cell effector function. This reagent is suitable for research into acute myelogenous leukemia, diabetes, and myocardial ischemia-reperfusion injury. -
S1P1 Agonist
SEW2871 is a potent and highly selective agonist of the sphingosine-1-phosphate type 1 receptor (S1P1), exhibiting an EC50 of 13.8 nM. This compound activates critical signaling pathways, including ERK, Akt, and Rac, and facilitates S1P1 internalization and recycling. SEW2871 effectively reduces lymphocyte populations in the bloodstream and shows promise for the study of various conditions, such as diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses. -
S1P₁ Agonist
PPI-4955 is a selective agonist of the sphingosine-1-phosphate receptor subtype 1 (S1P₁), displaying an EC50 of 1.62 nM. Its active phosphorylated form, PPI-4955-P, demonstrates exceptional receptor selectivity, with IC50 values of 0.23 nM for hS1P₁, 2000 nM for hS1P₃, 6.5 nM for hS1P₄, and 184 nM for hS1P₅. This compound significantly enhances in vivo phosphorylation efficiency, leading to lymphocyte reduction and a potential decrease in cardiovascular risk. PPI-4955 is applicable for research in immunomodulation and cardiovascular studies. -
S1PR Agonist
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. -
S1P1,5 Agonist
(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. -
S1P1 Receptor Antagonist
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. -
S1PR2 Agonist
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. -
S1P1 Agonist
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. -
S1P Receptor Agonist
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. -
S1P3 Antagonist
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. -
S1PR4 Antagonist
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. -
S1P2 Antagonist
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. -
S1PR1 Modulator
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. -
S1P2 Agonist
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. -
S1P Receptor Modulator
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. -
S1P Lyase Inhibitor
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. -
S1PR1 Agonist
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. -
S1P4 Receptor Agonist
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. -
S1P5 Agonist
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. -
S1PL Inhibitor
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. -
S1P4-R Agonist
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. -
S1P1 Agonist
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. -
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.
