S1P Receptor

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  1. S1P Receptor antagonist

    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.
  2. S1P3 receptor antagonist

    TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM.
  3. SphK2 inhibitor

    ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.
  4. S1PR1/S1PR5 inhibitor

    BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 and S1P5.
  5. S1P1 receptor modulator

    Ponesimod is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
  6. S1PR1 inhibitor

    KRP-203 is a selective Sphingosine-1-phosphate receptor agonist. It shows to reduce peripheral lymphocyte infiltration and to prolong survival in rat transplant models.
  7. EDG-1 (S1P1) agonist

    CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM).
  8. S1PR1 modulators

    RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases.
  9. SK2 modulator

    NS13001 is a selective SK2/3 modulator that acts as a potential therapeutic agent for treatment of SCA2 and possibly other cerebellar ataxias.
  10. S1P antagonist

    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.
  11. S1P agonist

    ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively.
  12. S1P1 and S1P5 agonist

    ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
  13. S1P antagonist

    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).
  14. S1P receptor agonist

    S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.
  15. S1P3 receptor agonist

    CYM-5541 (ML249) is an selective and allosteric S1P3 receptor agonist with an EC50 between 72 and 132 nM.
  16. S1PR1 antagonist

    W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
  17. S1P1/S1P5 receptor agonist

    GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
  18. S1P1 agonist

    Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.
  19. S1PR1 agonist

    FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.
  20. S1P inhibitor

    PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.
  21. sphingosine-1-phosphate receptor 4 (S1P4-R) agonist

    CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM.
  22. S1P(1) antagonist

    NIBR-0213 is a potent and selective antagonist of S1P(1) with efficacy in experimental autoimmune encephalomyelitis.
  23. S1P2 antagonist

    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.

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