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-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-103333
    Arvanil
    		99.1%
    Arvanil (N-Vanillylarachidonamide) is a mixed agonist of CB1 and TRPV1 receptors. Arvanil downregulates CD25, HLA-DR, CD134/OX40, blocks G1/S phase transition, and induces phosphorylation of Akt. Arvanil does not induce apoptosis in cells. Arvanil inhibits lymphocyte activation and ameliorates autoimmune encephalomyelitis. Arvanil can be used in research related to Huntington's disease, vomiting, and multiple sclerosis.
    Arvanil
  • HY-101834
    ACT-462206
    		Antagonist 99.54%
    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-162235
    CVN766
    		Antagonist 98.31%
    CVN766 is an orally active inhibitor of orexin 1 receptor antagonist with blood-brain permeability with the IC50 values of 8 nM and >10 μM for OX1R and OX2R, respectively. CVN766 can be used for study schizophrenia.
    CVN766
  • HY-147294
    Nivasorexant
    		Antagonist 99.74%
    Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder.
    Nivasorexant
  • HY-152843
    Fazamorexant
    		Antagonist 98.95%
    Fazamorexant (YZJ-1139) is an orally active dual orexin receptor antagonist, with an IC50 of 32 nM against OX1R and an IC50 of 41 nM against OX2R. Fazamorexant prolongs total sleep time and improves sleep efficiency. Fazamorexant is applicable to related research on insomnia.
    Fazamorexant
  • HY-10806
    SB-649868
    		Antagonist 99.45%
    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-P1349A
    Orexin B, rat, mouse TFA
    		Agonist 98.68%
    Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation.
    Orexin B, rat, mouse TFA
  • HY-137452
    Suntinorexton
    		Agonist 98.66%
    Suntinorexton is an OX2R agonist. Suntinorexton is used to study respiratory function during sleep.
    Suntinorexton
  • 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-P990175
    Anti-Mouse OX40L/CD134L Antibody (RM134L)
    		Inhibitor
    Anti-Mouse OX40L/CD134L Antibody (RM134L) is an anti-mouse OX40L/CD134L IgG2b monoclonal antibody. Anti-Mouse OX40L/CD134L Antibody (RM134L) reduces immune response by inhibiting the OX40/OX40L signaling pathway. Anti-Mouse OX40L/CD134L Antibody (RM134L) can inhibit plasma cell differentiation and antibody secretion. Anti-Mouse OX40L/CD134L Antibody (RM134L) can prolong the survival time of cell transplantation by inhibiting CD4+ T cells. Anti-Mouse OX40L/CD134L Antibody (RM134L) can be used for researches on inflammation and cancer such as graft versus host disease (GVHD), allergic reaction, lupus nephritis and hepatocellular carcinoma (HCC).
    Anti-Mouse OX40L/CD134L Antibody (RM134L)
  • HY-177073
    Cleminorexton
    		Agonist
    Cleminorexton is an orally active orexin-2 receptor (OX2R) agonist with a pEC50 between 9 and 10.4. Cleminorexton can be used for narcolepsy and other conditions associated with orexin deficiency and/or excessive sleepiness.
    Cleminorexton
  • HY-P99911
    Efizonerimod alfa
    		Agonist 98.57%
    Efizonerimod alfa (MEDI-6383) is a recombinant human OX40L IgG4P Fc fusion protein that assembles into a hexameric structure and exerts potent agonist activity upon binding to OX40. The activity of Efizonerimod alfa is enhanced by Fcγ receptor-mediated aggregation. Efizonerimod alfa binds to OX40 on the surface of activated T cells, induces NF-κB promoter activity in OX40-expressing T cells, and triggers the production of Th1-type cytokines, T cell proliferation, and resistance to regulatory T cell (Treg)-mediated suppression. Efizonerimod alfa enhances the cytolytic activity of tumor-reactive T cells and slows tumor growth in immunodeficient mice. Efizonerimod alfa induces the proliferation of CD4, CD8, and B cells in the peripheral blood of healthy non-human primates. Efizonerimod alfa can be used in the research of advanced solid malignancies and melanoma.
    Efizonerimod alfa
  • 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-P990115
    Anti-Mouse OX40/CD134 Antibody (OX-86)
    		Agonist ≥99.0%
    Anti-Mouse OX40/CD134 Antibody (OX-86) is an anti-mouse OX40/CD134 IgG1 monoclonal antibody. Anti-Mouse OX40/CD134 Antibody (OX-86) can enhance the anti-tumor function of CD8+ T cells. Anti-Mouse OX40/CD134 Antibody (OX-86) can reverse immune suppression, enhance antigen presentation and T cell activation. Anti-Mouse OX40/CD134 Antibody (OX-86) can be used for research on cancer such as papilloma and leukemia.
    Anti-Mouse OX40/CD134 Antibody (OX-86)
  • 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
  • HY-147403S
    Tebideutorexant
    		Antagonist 98.95%
    Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders.
    Tebideutorexant
  • HY-137440B
    (2R,3R)-Firazorexton
    		99.85%
    (2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton (HY-137440). Firazorexton is an orally active, brain-penetrating orexin type 2 receptor (OX2R) agonist that may improve narcolepsy-like symptoms..
    (2R,3R)-Firazorexton
  • HY-N7325
    Valerosidate
    		Antagonist
    Valerosidate is an OX2R antagonist. Valerosidate increases expression of tumor suppressor proteins p53 and PTEN, selectively reduces colon cancer cell viability, and suppresses colon cancer cell migration. Valerosidate can be used for the research of colon cancer and insomnia.
    Valerosidate
  • HY-108683
    ACT-335827
    		Antagonist 98.0%
    ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.
    ACT-335827
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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