Catalog No.
Product Name
Application
Product Information
Citations
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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. -
LPA1 Receptor Antagonist
ACT-1016-0707 is a selective antagonist of the LPA1 receptor, demonstrating oral bioavailability. This compound is primarily utilized in research focused on fibrotic diseases, showcasing its potential to modulate pathways associated with fibrosis and related pathologies. Its specificity for the LPA1 receptor makes it a valuable tool for exploring therapeutic strategies in fibrotic conditions. -
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. -
LPAR1 Antagonist
GS-2278 is an antagonist of the lysophosphatidic acid receptor 1 (LPAR1), which plays a significant role in various signaling pathways associated with cellular proliferation and fibrosis. This compound demonstrates potential in research related to idiopathic pulmonary fibrosis (IPF), making it a valuable tool for elucidating the molecular mechanisms underlying fibrotic diseases. Its ability to modulate LPAR1 activity may provide insights into novel therapeutic strategies for IPF and similar conditions. -
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. -
LPA Receptor Agonist
NAEPA is a phosphate-mimetic derivative that functions as an agonist of lysophosphatidic acid (LPA) receptors. It is known to facilitate cellular signaling pathways associated with cell proliferation, migration, and differentiation. This compound is valuable for research applications exploring the roles of LPA in various biological processes, including cancer biology and neurobiology. -
LPA1 Antagonist
ONO-0300302 is a potent oral antagonist of the lysophosphatidic acid receptor 1 (LPA1), exhibiting an IC50 of 0.086 μM. This compound acts as a slow tight binding inhibitor, with an increasing binding affinity over time, demonstrated by a Kd of 0.34 nM at 37 °C after 2 hours. ONO-0300302 is primarily utilized in research related to benign prostatic hyperplasia (BPH). -
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. -
LPA2 Antagonist
LPA2 antagonist 2 is a selective antagonist of the lysophosphatidic acid receptor 2 (LPA2), exhibiting an IC50 of 28.3 nM and a Ki of 21.1 nM, demonstrating significant potency. This compound shows over 480-fold selectivity against LPA3, with an IC50 of 13.85 μM. LPA2 antagonist 2 is valuable for research applications involving elucidating LPA2-mediated signaling pathways and exploring its role in various biological processes. -
LPAR1 Antagonist
LPAR1 antagonist 1 is a selective antagonist of the lysophosphatidic acid receptor 1 (LPAR1) with an IC50 of 3.3 nM. This compound demonstrates significant oral bioavailability and is primarily utilized in researching pathways related to fibrosis. Its high potency and selectivity make it a valuable tool for investigating LPAR1-related biological processes and therapeutic interventions in fibrotic diseases. -
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. -
LPA5 Antagonist
LPA5 Antagonist 2 is a potent antagonist of the lysophosphatidic acid receptor 5 (LPA5). It exhibits significant efficacy in reducing nociceptive hypersensitivity, making it a valuable tool for studies focused on inflammatory and neuropathic pain mechanisms. This compound's high aqueous solubility facilitates its use in various biological assays and experimental applications. -
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. -
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. -
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. -
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. -
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.
