Catalog No.
Product Name
Application
Product Information
Citations
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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
- 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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SphK2 inhibitor
ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. -
S1PR1/S1PR5 inhibitor
BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 and S1P5. -
EDG-1 (S1P1) agonist
CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM). -
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 antagonist
Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant. -
S1P receptor agonist
S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2. -
S1P1/S1P5 receptor agonist
GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis. -
S1PR1 agonist
FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury. -
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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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 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. -
S1PR1 Antagonist
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. -
S1P2 Receptor Antagonist
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. -
S1P2 Receptor Inhibitor
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. -
S1P Inhibitor
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. -
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.
