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 (26):

Cat. No. Product Name Effect Purity
  • HY-106224
    Orexin A (human, rat, mouse) Agonist 99.15%
    Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • 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-16725
    Lemborexant Antagonist 99.71%
    Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia.
  • HY-10805
    Almorexant Antagonist 99.01%
    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-10895A
    SB-334867 free base Antagonist 99.51%
    SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
  • HY-109012A
    Seltorexant hydrochloride Antagonist
    Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
  • HY-106224A
    Orexin A (human, rat, mouse) (TFA) Agonist
    Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • 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-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-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-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-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-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-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-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-13796
    IPSU Antagonist >98.0%
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
  • 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).
Isoform Specific Products

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