Orexin Receptors

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  1. OX Receptor Antagonist

    SB-408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
  2. orexin 1 receptor antagonist

    GSK1059865 is a potent orexin 1 receptor antagonist.
  3. OX Antagonist

    Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
  4. OX2 Antagonist

    MK-3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists.
  5. Orexin Antagonist

    SB-649868 is an orexin receptor antagonist in development by GlaxoSmithKline.
  6. orexin receptor antagonist

    Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.
  7. OX1 receptor antagonist

    SB 334867 is a selective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.
  8. Orexin A human, rat, mouse is a 33 amino acid excitatory neuropeptide. Orexin A human, rat, mouse works on 2 specific G protein-coupled receptors (GPCRs): orexin-1 (OX1) and orexin-2 (OX2).
  9. Orexin receptor antagonist

    MK6096, also known as filorexant, is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes.
  10. Dual orexin receptor antagonist

    TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
  11. OX1 Antagonist

    ACT-335827 is a selective orexin receptor 1 antagonist.
  12. OX2 receptor antagonist

    JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 μM for OX1R).
  13. OX1/OX2 Antagonist

    Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor 3.
  14. OX Receptor Antagonist

    SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.
  15. OX1 receptor antagonist

    SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors.
  16. Orexin 2 receptor agonist

    A potent and selective Orexin2 receptor agonist.
  17. OX2 Antagonist

    MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for potential treatment of insomnia.
  18. Alverine citrate is a drug used for functional gastrointestinal disorders.
  19. orexin OX1 receptor antagonist

    SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
  20. OX2 receptor antagonist

    TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base)
  21. OX2R antagonist

    Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R).
  22. OX2R antagonist

    TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1.
  23. OX2R antagonist

    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

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