S1P Receptor

Cat. No.

A10408

CAS No.

162359-56-0

FTY720 (Fingolimod)

Synonyms: Gilenia

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.

Cat. No.

A12265

CAS No.

934369-14-9

TY-52156

TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM.

Cat. No.

A14324

CAS No.

1221878-06-3

XL541

XL541 is a selective antagonist of the sphingosine-1-phosphate receptor 1 (S1P1), effectively inhibiting GDP-GTP exchange. This compound has been shown to induce significant surface hemorrhaging in tumors, highlighting its potential as a therapeutic agent. Additionally, XL541 demonstrates enhanced antitumor activity when used in combination with Paclitaxel, making it a valuable tool for research in breast and lung cancer therapies.

Cat. No.

A17798

CAS No.

162359-55-9

Fingolimod

Synonyms: FTY720 (free base)

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.

Cat. No.

A20102

CAS No.

449173-19-7

VPC 23019

VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5 receptors (pEC50= 6.58 and 7.07, respectively).

Cat. No.

A20580

CAS No.

909725-61-7

W146

W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.

Cat. No.

A22099

CAS No.

1233332-14-3

NIBR-0213

NIBR-0213 is a potent and selective antagonist of S1P(1) with efficacy in experimental autoimmune encephalomyelitis.

Cat. No.

A22583

CAS No.

383150-41-2

JTE-013

JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.

Cat. No.

A30671

CAS No.

909725-62-8

W146 TFA

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.

Cat. No.

A31655

CAS No.

1463912-49-3

AB1

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.

Cat. No.

A61122

CAS No.

1206123-37-6

Etrasimod

Synonyms: APD334

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.

Cat. No.

A61126

CAS No.

298186-80-8

CAY10444

Synonyms: BML-241

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.

Cat. No.

A61128

CAS No.

1314212-39-9

CYM50358

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.

Cat. No.

A61129

CAS No.

2130996-00-6

GLPG2938

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.

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.

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.

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.

A61199

CAS No.

1314212-81-1

CYM50374

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.

Cat. No.

A61219

CAS No.

1345982-24-2

W123

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.

Cat. No.

A61233

CAS No.

1781750-72-8

CYM50358 hydrochloride

CYM50358 hydrochloride is a potent and selective antagonist of the sphingosine-1-phosphate 4 (S1P4) receptor. This compound exhibits significant biological activity by inhibiting S1P4-mediated signaling pathways, making it a valuable tool in research focused on the immune response and inflammation. Its application extends to the study of influenza infection, facilitating investigations into viral pathogenesis and potential therapeutic interventions.

Cat. No.

A61238

CAS No.

1621065-22-2

S1P5 receptor antagonist 1

S1P5 receptor antagonist 1 is a selective antagonist targeting the S1P5 receptor, characterized by an EC50 of 0.1 nM and a Ki of 4.4 nM. This compound is capable of inhibiting the migration of natural killer cells towards sphingosine 1-phosphate in vitro, while leaving T cell migration unaffected. S1P5 receptor antagonist 1 is employed in research focused on central nervous system diseases, providing insights into the modulation of immune responses within the brain.