1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Orexin Receptor (OX Receptor)

Orexin Receptor (OX Receptor)

Orexin receptors (OX receptor) include orexin 1 receptor and orexin 2 receptor. Orexin receptor type 1 (Ox1R or OX1), is a protein that in humans is encoded by the HCRTR1gene. The orexin 1 receptor (OX1), is a G-protein coupled receptor expressed in the hypothalamus and involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A neuropeptide. It shares 64% identity with OX2. The OX2 receptors, also known as hypocretin receptor 2, are located primarily in the cerebral cortex, paraventricular hypothalamus, nucleus accumbens, subthalamic and paraventricular thalamus where they are thought to regulate sleep-wakefulness. The OX2 receptor displays equal affinity for Orexin A and Orexin B. The human OX2 receptor gene has been localized to chromosome 6.

Orexin Receptor (OX Receptor) Related Products (23):

Cat. No. Product Name Effect Purity
  • HY-19320
    Orexin 2 Receptor Agonist Agonist 99.72%
    Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.
  • HY-10895A
    SB-334867 free base Antagonist 99.77%
    SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
  • HY-10805
    Almorexant Antagonist 99.17%
    Almorexant (ACT 078573) 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, respectively.
  • HY-16725
    Lemborexant Antagonist 99.71%
    Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.
  • HY-100452
    TCS-OX2-29 Antagonist 99.82%
    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.
  • HY-109012
    Seltorexant 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). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
  • HY-108682
    EMPA Antagonist >99.0%
    EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively.
  • HY-15653
    Filorexant Antagonist 98.95%
    Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
  • HY-19914
    MK-1064 Antagonist 99.97%
    MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.
  • HY-101534
    GSK1059865 Antagonist 99.91%
    GSK1059865 is a potent orexin 1 receptor antagonist.
  • HY-70068
    SB-408124 Antagonist 98.87%
    SB408124 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.
  • HY-10898
    SB-674042 Antagonist 99.70%
    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.
  • HY-10805A
    Almorexant hydrochloride Antagonist 99.88%
    Almorexant hydrochloride (ACT 078573 hydrochloride) 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, respectively.
  • HY-P1339A
    Orexin B, human TFA Agonist 98.15%
    Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
  • HY-10806
    SB-649868 Antagonist 99.88%
    SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).
  • HY-13796
    IPSU Antagonist >98.0%
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
  • HY-109095
    Nemorexant Antagonist 99.47%
    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.
  • HY-P1349
    Orexin B, rat, mouse Agonist
    Orexin B, rat, mouse is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
  • HY-10900
    TCS 1102 Antagonist 99.89%
    TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
  • HY-12301
    MK-3697 Antagonist 99.46%
    MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
Isoform Specific Products

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