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

Orexin Receptor (OX Receptor)

Hypocretin Receptor; HCRT Receptor

Orexin Receptor (OX Receptor)

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The orexin receptors (hypocretin receptors) are a family of G protein-coupled receptors and consist of orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) subtypes. Orexin receptors are expressed throughout the central nervous system and are involved in the regulation of the sleep/wake cycle.

Orexin A binding to OX1R and OX2R with similar affinity, and orexin B binding to OX2 with higher affinity than OX1R. OX1R is mainly expressed in the prefrontal and infralimbic cortex, hippocampus, paraventricular thalamic nucleus, and locus coeruleus. OX2R is mainly distributed in the cerebral cortex, septal nuclei, lateral hypothalamus, hippocampus, and hypothalamic nuclei.

Both OX1R and OX2R are coupled via Gq/11 to the activation of phospholipase C, leading to an elevation of intracellular Ca2+ levels. Moreover, OX2R also couples via Gs and Gi/o to the cAMP pathways.

Orexin Receptor (OX Receptor) Isoform Specific Products:

Orexin Receptor (OX Receptor) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-154789
    RTIOXA-43
    		Agonist 99.94%
    RTIOXA-43 is a orexin receptor agonist with EC50s of 24 nM and 24 nM for OX2 and OX1 receptors, respectively.
    RTIOXA-43
  • HY-19914
    MK-1064
    		Antagonist 99.95%
    MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia.
    MK-1064
  • HY-P99249
    Vonlerolizumab
    		Agonist 99.70%
    Vonlerolizumab (Pogalizumab; MOXR 0916) is a humanized IgG1 monoclonal antibody targeting OX40 (CD134). Pogalizumab partially blocks the interaction between OX40 and its natural ligand OX40L upon binding, thereby activating the NF-κB signaling pathway. Pogalizumab enhances T cell activation and proliferation and has shown antitumor activity in mouse models.
    Vonlerolizumab
  • HY-10898
    SB-674042
    		Antagonist 99.87%
    SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively.
    SB-674042
  • HY-108682
    EMPA
    		Antagonist 99.92%
    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.
    EMPA
  • HY-136181A
    YNT-185
    		Agonist 98.46%
    YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models.
    YNT-185
  • HY-70068
    SB-408124
    		Antagonist 98.93%
    SB-408124 is a non-peptide OX1 receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor.
    SB-408124
  • HY-172412
    Alixorexton
    		Agonist 99.96%
    Alixorexton (ALKS 2680) is an orally bioavailable, blood-brain barrier-permeable OX2R-selective activator and wake-promoting agent. Alixorexton can be used for the research of narcolepsy and idiopathic hypersomnia.
    Alixorexton
  • HY-109012A
    Seltorexant hydrochloride
    		Antagonist 99.90%
    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.
    Seltorexant hydrochloride
  • HY-P1341
    OXA(17-33)
    		Agonist
    OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy.
    OXA(17-33)
  • HY-10900
    TCS 1102
    		Antagonist 99.73%
    TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats.
    TCS 1102
  • HY-10895A
    SB-334867 free base
    		Antagonist 99.88%
    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.
    SB-334867 free base
  • HY-P1349
    Orexin B, rat, mouse
    		Agonist 99.66%
    Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
    Orexin B, rat, mouse
  • HY-137440
    Firazorexton
    		Agonist 99.56%
    Firazorexton (TAK-994 free base) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton (TAK-994 free base) can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice.
    Firazorexton
  • HY-P99836
    Cudarolimab
    		Inhibitor
    Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research.
    Cudarolimab
  • HY-171032
    (R)-YNT-3708
    		Agonist 99.07%
    (R)-YNT-3708 is a selective orexin 1 (OX1R) agonist, with an EC50 of 7.48 nM. (R)-YNT-3708 has antinociceptive effects.
    (R)-YNT-3708
  • HY-P991336
    Ordastobart
    		Agonist 98%
    Ordastobart (INBRX-106; ES-102) is a hexavalent OX40 agonist antibody. Ordastobart enhances OX40 receptor clustering, signaling, and downstream activation, thereby increasing the proliferation and activation of CD4+ and CD8+ T cells in vitro and in vivo. Ordastobart exhibits anti-tumor effects and improves survival in mouse models of cancer. Ordastobart is indicated for research in cancers such as fibrosarcoma and colorectal cancer.
    Ordastobart
  • HY-101534
    GSK1059865
    		Antagonist 99.68%
    GSK1059865 is a potent orexin 1 receptor antagonist.
    GSK1059865
  • HY-136181
    YNT-185 dihydrochloride
    		Agonist 99.78%
    YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models.
    YNT-185 dihydrochloride
  • HY-134188
    JNJ-54717793
    		Antagonist 98.06%
    JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
    JNJ-54717793
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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