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-P1341
    OXA(17-33)
    		Agonist
    OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM).
    OXA(17-33)
  • HY-100452
    TCS-OX2-29
    		Antagonist 99.55%
    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.
    TCS-OX2-29
  • HY-P99945
    Revdofilimab
    		Activator 99.35%
    Revdofilimab (ABBV-368) is a human IgG1 agonist monoclonal antibody against OX40. Among them, OX40 is a member of the TNF receptor superfamily expressed on activated and memory T cell subsets and T regulatory cells.
    Revdofilimab
  • 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-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-10806
    SB-649868
    		Antagonist 99.87%
    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).
    SB-649868
  • HY-70068
    SB-408124
    		Antagonist 98.27%
    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-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-10805A
    Almorexant hydrochloride
    		Antagonist 99.98%
    Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
    Almorexant hydrochloride
  • HY-136181A
    YNT-185
    		Agonist 98.36%
    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-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-139559
    Vornorexant
    		Antagonist 99.66%
    Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.
    Vornorexant
  • HY-137440
    Firazorexton
    		Agonist 99.94%
    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-101834
    ACT-462206
    		Antagonist 99.60%
    ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research.
    ACT-462206
  • HY-147294
    Nivasorexant
    		Antagonist 99.74%
    Nivasorexant is a potent orexin receptor antagonist.
    Nivasorexant
  • HY-137440A
    Firazorexton hydrate
    		Agonist 99.94%
    Firazorexton hydrate (TAK-994) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton hydrate can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice.
    Firazorexton hydrate
  • HY-12301
    MK-3697
    		Antagonist 98.83%
    MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.
    MK-3697
  • HY-101534
    GSK1059865
    		Antagonist 99.83%
    GSK1059865 is a potent orexin 1 receptor antagonist.
    GSK1059865
  • HY-P1340
    [Ala11,D-Leu15]-Orexin B(human)
    		Agonist 98.31%
    [Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM).
    [Ala11,D-Leu15]-Orexin B(human)
  • HY-76612
    SB-408124 Hydrochloride
    		Antagonist 98.79%
    SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor.
    SB-408124 Hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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