Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Anti-LPA mAb
Lpathomab is a human IgG1 monoclonal antibody (mAb) that targets lysophosphatidic acid (LPA). It effectively inhibits the release of pro-inflammatory cytokines IL-8 and IL-6 in SKOV3 cells, while also blocking LPA-induced tumor cell migration. Additionally, Lpathomab demonstrates the ability to reduce neovascularization in Matrigel plug and choroidal neovascularization (CNV) models, and it provides neuroprotection in a controlled cortical impact (CCI) mouse model. This reagent is suitable for research applications in brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. -
LPA Receptor Activator
AzoLPA ammonium is a photoswitchable lipid that functions as an activator of the Lysophosphatidic acid receptors 1-5 (LPA1-5). This compound initiates LPA receptor signaling pathways, enabling researchers to investigate the physiological roles of LPA in various biological processes. It is particularly valuable for applications in cell signaling studies and the exploration of LPA-related mechanisms in cancer, neurobiology, and cell migration. -
Lp(a) Antagonist
Lp(a)-IN-8 is a selective antagonist of lipoprotein(a) [Lp(a)], a recognized causal risk factor for atherosclerotic cardiovascular disease (ASCVD). This compound effectively inhibits Lp(a) accumulation, offering potential for reducing cardiovascular risk. Research applications include investigations into ASCVD mechanisms and therapeutic strategies targeting Lp(a) modulation. -
Spns2 Inhibitor
SLF1081851 TFA is a selective inhibitor of Spns2, effectively inhibiting sphingosine-1-phosphate (S1P) release with an IC50 of 1.93 μM. This compound is instrumental in studies related to developmental biology and immune regulation. Its ability to modulate S1P levels makes it a valuable tool for investigating pathways involved in immune responses and developmental processes. -
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. -
LPL Receptor Modulator
S1P1 agonist 4 is a potent LPL receptor modulator that exhibits high efficacy with an EC50 of less than 0.05 mg/kg. This compound is characterized by a favorable human half-life, approximately 5 days, making it an ideal candidate for studies involving lipid metabolism and cardiovascular disease research. Its ability to selectively activate S1P1 receptors positions it as a valuable tool for exploring therapeutic strategies in metabolic disorders. -
Lp(a) Antagonist
LPA2 antagonist 6 is a potent antagonist targeting lipoprotein(a) [Lp(a)]. It effectively inhibits Lp(a) formation with an IC50 value of 2.33 nM. This compound is instrumental in cardiovascular disease research, allowing for deeper exploration into the mechanisms of lipoprotein metabolism and its role in associated pathologies. -
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. -
LPL Receptor Agonist
GSK2018682 hydrochloride is a specific agonist for the sphingosine-1-phosphate receptors S1P1 and S1P5, exhibiting pEC50 values of 7.7 and 7.2, respectively. It shows no agonist activity toward the S1P2, S1P3, or S1P4 receptors. This compound is primarily utilized in research investigating multiple sclerosis and related neurological disorders, offering insights into the modulation of immune responses and vascular integrity. -
LPA Receptor Modulator
N-PTyrosine PA ammonium is a lysophosphatidic acid (LPA) receptor modulator that functions primarily as a competitive inhibitor at LPA1 and a partial agonist at LPA5. This compound may inhibit LPA receptor activation and downstream signaling pathways by competing for binding sites with native agonists. Additionally, N-PTyrosine PA ammonium is capable of inducing morphological changes and promoting aggregation, as well as preventing LPA-induced morphological alterations through prior receptor desensitization. Its applications extend to the study of various conditions, including atherosclerosis and acute ischemic syndromes, such as unstable angina and myocardial infarction. -
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. -
LPL Receptor Modulator
GSK 1842799 TFA is a selective modulator of the S1P1 receptor, primarily developed for the treatment of multiple sclerosis (MS). The phosphorylated derivative, GSK1842799-P, demonstrates subnanomolar agonist activity for S1P1, with over 1000-fold selectivity against S1P3. This compound exhibits favorable pharmacokinetics, including good oral bioavailability and rapid in vivo conversion, leading to significant lymphocyte count reduction at a dose of 0.1 mg/kg. In preclinical models, it showcased comparable efficacy to FTY720, supporting its potential utility in MS research and other immune-related conditions. -
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. -
LPL Receptor Agonist
CS-0777-P is a potent and selective agonist of the sphingosine 1-phosphate receptor 1 (S1P1). It displays approximately 320-fold higher activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. Biological studies indicate its capability to significantly reduce peripheral blood lymphocyte counts and exert immunosuppressive effects in experimental autoimmune encephalomyelitis models in rats. Pharmacokinetic analysis reveals swift lymphocyte count reductions after oral administration, highlighting CS-0777-P's potential as a therapeutic candidate for multiple sclerosis, currently under clinical investigation. -
R-Isomer of FTY 720P
(R)-FTY 720P is the R-isomer of FTY 720P, primarily targeting sphingosine-1-phosphate receptors S1P1, S1P3, S1P4, and S1P5. It exhibits reduced binding affinities compared to its S-isomer counterpart. This compound is utilized in research applications focused on immune modulation and neuroprotection, contributing to studies involving multiple sclerosis and other autoimmune conditions. -
LPA2 Antagonist
LPA2 antagonist 5 is a specific antagonist of the lysophosphatidic acid receptor 2 (LPA2), demonstrating an IC50 of 4.05 nM. This compound is valuable for research into the regulatory roles of LPA2 in various biological processes, including cancer biology and neurodegenerative diseases. Its ability to inhibit LPA2 signaling makes it an important tool for dissecting the receptor's functions and potential therapeutic targets. -
LPA5 Antagonist
LPA5 antagonist 3 functions as an antagonist of the lysophosphatidic acid receptor 5 (LPA5), exhibiting an IC50 of 170 nM. This compound is primarily utilized in research related to pain disorders and atherosclerosis, providing valuable insights into the role of LPA5 in various pathological conditions. Its effectiveness in modulating LPA5 activity makes it a significant tool for exploring therapeutic approaches in these areas. -
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. -
LPL Receptor Agonist
AUY 954 hydrochloride is a potent and selective agonist of the sphingosine-1-phosphate (S1P(1)) receptor, exhibiting significant immunomodulatory properties. It induces a notable and reversible decrease in circulating lymphocytes following oral administration. In preclinical studies, AUY 954 hydrochloride has shown efficacy in prolonging cardiac allograft survival in conjunction with RAD001, as well as effectively preventing experimental autoimmune neuritis in rat models. This compound holds promising therapeutic potential for various autoimmune conditions. -
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. -
LPA1/LPA3 Antagonist
VPC12249 is a competitive dual antagonist of LPA1 and LPA3, exhibiting Ki values of 137 nM and 428 nM, respectively. It effectively inhibits calcium mobilization in HEK293T cells with a Ki of approximately 130 nM. This compound is useful for investigating the roles of LPA receptors in ovarian cancer and hypertensive diseases, providing valuable insights into potential therapeutic strategies. -
LPL Receptor Agonist
NSC12404 is a selective agonist for the lysophosphatidic acid receptor 2 (LPA2). This compound exhibits weak but specific activity, making it a valuable tool for studying LPA2 receptor signaling pathways. Its applications in research include investigating the role of LPA2 in cellular processes such as proliferation, migration, and differentiation. -
Spns2 Inhibitor
SLF80821178 hydrochloride is a selective inhibitor of the sphingosine-1-phosphate transporter (Spns2), effectively reducing sphingosine-1-phosphate (S1P) release in HeLa cells with an IC50 value of 51 nM. This compound demonstrates the capability to decrease circulating lymphocyte levels in mice without altering plasma S1P concentrations, making it a valuable tool for studying immune response and signaling pathways. Research applications include investigations into lymphocyte trafficking and potential therapeutic strategies targeting sphingosine metabolism. -
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. -
Spns2 Inhibitor
SLF1081851 hydrochloride is a potent inhibitor of Spns2, effectively suppressing sphingosine-1-phosphate (S1P) release with an IC50 of 1.93 μM. This compound is significant for research into immune system development and related biological processes. It serves as a valuable tool for investigating the role of S1P in various cellular functions and pathological conditions. -
SPL Inhibitor
SPL-IN-1 is a selective sphingosine-1-phosphate lyase inhibitor that targets the SPL enzyme. It has demonstrated significant biological activity in modulating sphingolipid metabolism and influencing cellular signaling pathways. This compound is valuable for research applications involving inflammation, cancer progression, and other diseases associated with sphingosine-1-phosphate signaling dysregulation. -
LPL Receptor Modulator
BMS-986104 is a selective modulator of the S1P1 receptor, exhibiting significant biological activity in promoting remyelination. It demonstrates efficacy in a mouse model of experimental autoimmune encephalomyelitis (EAE), showing comparable results to established agents. Mechanistically, BMS-986104 effectively facilitates remyelination in a three-dimensional brain cell culture assay involving lysophosphatidylcholine-induced demyelination, making it a valuable tool for research on neurodegenerative diseases and myelin repair mechanisms. -
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. -
Sphingosine-1-Phosphate Receptor Agonist
Zectivimod is a sphingosine-1-phosphate receptor agonist that plays a crucial role in modulating immune responses. It exhibits significant biological activity in the context of autoimmune diseases, chronic inflammatory conditions, and immunoregulation disorders. This compound is valuable for research aimed at understanding the underlying mechanisms of immune system modulation and the development of therapeutic strategies.
