Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Spns2 Inhibitor
SLF1081851 is a selective inhibitor of Spns2, effectively inhibiting sphingosine-1-phosphate (S1P) release with an IC50 of 1.93 μM. This compound is crucial for studying developmental processes and immune responses, making it a valuable tool in research focused on modulating these biological pathways. Its ability to target Spns2 provides insight into the mechanisms regulating S1P availability and its subsequent effects on cell signaling and function. -
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. -
LPA1 Antagonist
H2L 5765834 is a potent antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, exhibiting IC50 values of 94 nM, 752 nM, and 463 nM, respectively. This compound is valuable for studies investigating the role of LPA receptors in various biological processes, including cell proliferation, migration, and survival. Its ability to selectively inhibit these receptors makes it a useful tool for research in cancer biology, fibrosis, and neurobiology. -
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. -
LPA1 Agonist
ONO-0740556 is a potent agonist of the Gi-coupled human lysophosphatidic acid receptor 1 (LPA1), exhibiting an EC50 value of 0.26 nM. This compound plays a significant role in modulating cellular signaling pathways associated with LPA1 activation. ONO-0740556 is valuable for research applications focused on investigating LPA1-related physiological and pathological processes, including cell proliferation, migration, and inflammatory responses. -
Spns2 Inhibitor
SLF80821178 is a potent inhibitor of the Sphingosine-1-Phosphate Transporter (Spns2), exhibiting an IC50 of 51 nM for the inhibition of S1P release in HeLa cells. This orally active compound demonstrates a half-life of 2.4 hours in mouse models. Research applications include the investigation of sphingosine metabolism and transport in cellular signaling pathways. -
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. -
LPA5/GPR92 Antagonist
TC LPA5 4 is a selective antagonist of LPA5 (GPR92) with a non-lipid structure. It effectively inhibits LPA-induced aggregation of isolated human platelets, demonstrating an IC50 value of 800 nM. Additionally, TC LPA5 4 shows potent inhibition of cell proliferation and migration in thyroid cancer cells, making it a valuable tool for research in cancer biology and cell signaling pathways associated with LPA5. -
LPA1 Antagonist
ONO-9780307 is a potent antagonist of the LPA1 (lysophosphatidic acid receptor 1) with an IC50 value of 2.7 nM. This compound effectively inhibits LPA1-mediated signaling pathways, making it a valuable tool for studying the role of lysophosphatidic acid in various biological processes. It is suitable for research applications involving cellular signaling, inflammation, and cancer biology. -
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. -
LPA1 NAM
TAK-615 is a negative allosteric modulator (NAM) of the lysophosphatidic acid receptor 1 (LPA1). It exhibits high-affinity binding with a Kd of 1.7 nM, along with a lower affinity of 14.5 nM. This compound is primarily used in research focused on pulmonary fibrosis, enabling investigations into the role of LPA1 in fibrotic pathways and potential therapeutic interventions. -
LPL Receptor Inhibitor
S1PR1 modulator 1 is a selective inhibitor of the S1PR1 receptor, demonstrating a pIC50 of 7.6 and exhibiting greater than 40-fold selectivity over S1PR2 and over 80-fold selectivity over S1PR3 and S1PR4. This compound is valuable for investigating S1PR1-mediated signaling pathways and its role in various biological processes, including immune response regulation and cardiovascular function. Its specificity makes it an important tool for research applications focused on the modulation of S1P receptor activity in disease models. -
Autotaxin Inhibitor
CRT0273750 is an inhibitor of autotaxin (ATX), which plays a crucial role in the modulation of lysophosphatidic acid (LPA) levels, exhibiting an IC50 of 0.014 μM. This compound is valuable in the study of ATX/LPA-dependent cancer models, contributing to research on tumor progression and metastasis. Its specificity for ATX provides a useful tool for elucidating the underlying mechanisms of LPA-mediated signaling pathways in various biological contexts. -
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. -
LPL Receptor Agonist
Ceralifimod is a potent and selective agonist for the sphingosine 1-phosphate receptors 1 and 5, exhibiting effective EC50 values of 27.3 pM and 334 pM for human S1P receptor 1 and 5, respectively. This compound is primarily utilized in research applications investigating immune modulation and cardiovascular disease. Its targeted mechanism provides valuable insights into receptor signaling pathways relevant to inflammation and tissue homeostasis. -
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. -
Spns2 Inhibitor
SLB1122168 is a selective inhibitor of Spns2 that significantly impairs the release of sphingosine-1-phosphate (S1P) with an IC50 of 94 nM. This compound is useful for investigating the role of S1P in various biological processes, including immune response and cardiovascular regulation. Its application in research can help elucidate the mechanisms underlying Spns2 activity and S1P signaling pathways. -
LPL Receptor Agonist
S1P1 Agonist 1 targets the sphingosine-1-phosphate receptor 1 (S1P1) as an agonist, exerting significant immunomodulatory effects. This compound plays a crucial role in modulating immune responses and inflammation, making it valuable for research in immunology and related fields. S1P1 Agonist 1 is instrumental in studies exploring the therapeutic potential of S1P1 activation in various 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. -
LPL Receptor Agonist
(S)-FTY720-phosphonate is a selective agonist of the S1P receptor 1 (S1PR1). This compound is primarily employed in research related to acute inflammatory diseases, including but not limited to acute lung injury. By activating S1PR1, (S)-FTY720-phosphonate may facilitate studies on its role in immune response modulation and tissue repair mechanisms. -
Sphingosine-1-phosphate Lyase Inhibitor
S1PL-IN-1 is a selective sphingosine-1-phosphate lyase inhibitor with an IC50 of 210 nM. This compound exhibits potential in modulating S1P signaling pathways and may serve as a Smoothened receptor antagonist with an IC50 of 440 nM. S1PL-IN-1 is primarily utilized in the study of experimental autoimmune encephalomyelitis and related neurological disorders. Its capacity to influence sphingolipid metabolism makes it a valuable tool for research into neuroinflammatory conditions. -
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.
