S1P Receptor

Cat. No.

A61154

CAS No.

3107268-28-7

S1PR5-IN-1

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.

Cat. No.

A61157

CAS No.

1807873-14-8

KSI-6666

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.

Cat. No.

A61158

CAS No.

1233332-37-0

Ex26

Synonyms: S1P1-IN-Ex26

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.

Cat. No.

A61159

CAS No.

913827-99-3

CS-2100

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.

Cat. No.

A61160

CAS No.

1418093-75-0

IMMH001

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).

Cat. No.

A61161

CAS No.

2256030-24-5

TRV045

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.

Cat. No.

A61162

CAS No.

1306760-73-5

RP101075

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.

Cat. No.

A61163

CAS No.

1234627-85-0

Siponimod hemifumarate

Synonyms: BAF-312 hemifumarate

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.

Cat. No.

A61169

CAS No.

105615-55-2

L-threo Lysosphingomyelin (d18:1)

Synonyms: L-threo-Sphingosylphosphorylcholine

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.

Cat. No.

A61170

CAS No.

852230-33-2

CYM-5482

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.

Cat. No.

A61171

CAS No.

945725-50-8

TASP0277308

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.

Cat. No.

A61174

CAS No.

1324003-64-6

S1P1 agonist III

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.

Cat. No.

A61177

CAS No.

942399-20-4

Amiselimod

Synonyms: MT-1303

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.

Cat. No.

A61178

CAS No.

2097854-81-2

Tamuzimod

Synonyms: VTX002

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.

Cat. No.

A61179

CAS No.

952510-14-4

ASP-4058 hydrochloride

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.

Cat. No.

A61180

CAS No.

2373330-78-8

S1P5 receptor agonist-1

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.

Cat. No.

A61181

CAS No.

1403232-33-6

Vibozilimod

Synonyms: SCD-044

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.

Cat. No.

A61182

CAS No.

1206123-97-8

Etrasimod arginine

Synonyms: APD334 arginine

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.

Cat. No.

A61183

CAS No.

1354908-17-0

S1p receptor agonist 2

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.

Cat. No.

A61188

CAS No.

2281761-58-6

Ginkgolic acid 2-phosphate

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.

Cat. No.

A61192

CAS No.

3028594-26-2

S1PR1 agonist 3

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.

Cat. No.

A61193

CAS No.

1246817-25-3

W140 hydrobromide

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.

Cat. No.

A61194

CAS No.

2760666-20-2

S1P1 agonist 5

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.

Cat. No.

A61195

CAS No.

1236188-38-7

BMS-520

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.

Cat. No.

A61198

CAS No.

1883345-06-9

Udifitimod

Synonyms: BMS-986166

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.