Orexin Receptor (OX Receptor)
Hypocretin Receptor; HCRT Receptor
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
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Orexin Receptor (OX Receptor) Inhibitors
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Orexin Receptor (OX Receptor) Agonists
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Orexin Receptor (OX Receptor) Antagonists
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Orexin Receptor (OX Receptor) Activators
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Orexin Receptor (OX Receptor) Modulators
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Orexin Receptor (OX Receptor) Related Products (130)
Related Products (130)
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Antibodies (2)
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Orexin Receptor (OX Receptor) Isoform Comparison
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ACT-462206
0 ImagesACT-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.
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CVN766
0 ImagesCVN766 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.
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YNT-185 dihydrochloride
0 ImagesYNT-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.
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Cleminorexton
0 ImagesCat. No.: HY-177073CAS No.: 2980518-93-0Cleminorexton 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.
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Nivasorexant
0 ImagesSynonyms: ACT-539313Nivasorexant (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.
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SB-649868
0 ImagesSynonyms: GSK649868SB-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).
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Orexin B, rat, mouse TFA
0 ImagesCat. No.: HY-P1349APurity: 98.68%Synonyms: Rat orexin B TFA; Orexin B (mouse) TFAOrexin 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.
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Anti-Mouse OX40/CD134 Antibody (OX-86)
0 ImagesCat. No.: HY-P990115Purity: ≥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.
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Suntinorexton
0 ImagesSuntinorexton is an OX2R agonist. Suntinorexton is used to study respiratory function during sleep.
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[Ala11,D-Leu15]-Orexin B(human)
![[Ala11,D-Leu15]-Orexin B(human)](https://file.medchemexpress.com/product_pic/hy-p1340.gif "Click to View [Ala11,D-Leu15]-Orexin B(human) Product Detail")
0 Images[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).
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Anti-Mouse OX40L/CD134L Antibody (RM134L)
0 ImagesCat. No.: HY-P990175Anti-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).
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Tebideutorexant
0 ImagesSynonyms: JNJ-61393215Tebideutorexant 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.
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Orexin A-13C18,15N3 (human, rat, mouse) TFA
0 ImagesCat. No.: HY-106224AS1Purity: 98.60%Synonyms: Hypocretin-1-13C18,15N3 (human, rat, mouse) TFAOrexin A-13C18,15N3 (human, rat, mouse) ((Hypocretin-1-13C18,15N3 (human, rat, mouse)) TFA is the 13C- and 15N-labeled Orexin A (human, rat, mouse) (HY-106224). Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). 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.
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Efizonerimod alfa
0 ImagesSynonyms: MEDI-6383Efizonerimod 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.
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Firazorexton hydrate
0 ImagesSynonyms: TAK-994Firazorexton 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.
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Alixorexton enantiomer
0 ImagesSynonyms: ALKS 2680 enantiomerAlixorexton (ALKS 2680) enantiomer is the enantiomer of Alixorexton (HY-172412). Alixorexton is a selective, orally active and brain-penetrant agonist for orexin-2 receptor and can be used for hypersomnias research.
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SB-408124 Hydrochloride
0 ImagesSB-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.
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(2R,3R)-Firazorexton
0 ImagesSynonyms: (2R,3R)-TAK-994 free base(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..
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Valerosidate
0 ImagesCat. No.: HY-N7325CAS No.: 29505-31-5
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ACT-335827
0 ImagesACT-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.
