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-P990479
    Anti-OX2R/CD200R1 Antibody
    		Inhibitor
    Anti-OX2R/CD200R1 Antibody is a CHO-expressed human antibody that targets OX2R/CD200R1. The predicted molecular weight (MW) of Anti-OX2R/CD200R1 Antibody is 146.58 kDa. The isotype control for Anti-OX2R/CD200R1 Antibody can refer to Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-OX2R/CD200R1 Antibody
  • HY-P10080
    Xenopus orexin B
    		Agonist
    Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R.
    Xenopus orexin B
  • HY-P991337
    YH-002
    		Inhibitor
    YH-002 is a human IgG1 monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. YH-002 binds to OX40 by mimicking the function of OX40L.
    YH-002
  • HY-P4792
    Orexin A (16-33)
    Orexin A (16-33) is a fragment of orexin A.
    Orexin A (16-33)
  • HY-10805S
    Almorexant-13C,d3
    		Antagonist
    Almorexant-13C,d3 is the 13C- and deuterium labeled Almorexant. 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.
    Almorexant-<sup>13</sup>C,d<sub>3</sub>
  • HY-P1339
    Orexin B, human
    		Agonist
    Orexin B, human is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
    Orexin B, human
  • HY-149014
    OX2R-IN-1
    		Inhibitor
    OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life.
    OX2R-IN-1
  • HY-P991334
    INCAGN1949
    		Inhibitor
    INCAGN1949 is a human IgG1 monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. INCAGN1949 selectively deplete intratumoral regulatory T cells.
    INCAGN1949
  • HY-402873
    DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite
    		Inhibitor
    DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite (Compound 5) is an RNAi agent and an inhibitor of Ataxin-2 (ATXN2). DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite can be studied in research on ATXN2-associated neurological diseases.
    DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite
  • HY-163276
    OX2R-IN-2
    		Agonist
    OX2R-IN-2 (compound 63c) is an agonist for orexin receptor type 2 (OX2R) with EC50 of 339 nM. OX2R-IN-2 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells
    OX2R-IN-2
  • HY-101260
    DORA-22
    		Antagonist
    DORA-22 is an orally active dual orexinergic receptor antagonist, and improves the sleep disruption and memory impairment. DORA-22 can be used for study of insomnia.
    DORA-22
  • HY-P991336
    INBRX-106
    		Agonist
    INBRX-106 is a human monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. INBRX-106 is a novel hexavalent OX40 agonist.
    INBRX-106
  • HY-172436
    Rocavorexant
    		Antagonist
    Rocavorexant is the antagonist for orexin-1 receptor with pIC50 of 9.1 for human OX1 (while pIC50 for human OX2 is 6.0).
    Rocavorexant
  • HY-159731
    OX2R agonist 1
    		Agonist
    OX2R agonist 1 is an OX2R antagonist with an EC50 of less than 100 nM. OX2R agonist 1 can be used in research related to excessive daytime sleepiness or narcolepsy.
    OX2R agonist 1
  • HY-10895R
    SB-334867 (Standard)
    		Antagonist
    SB-334867 (Standard) is the analytical standard of SB-334867. This product is intended for research and analytical applications. SB-334867 (SB 334867A) 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 (Standard)
  • HY-113555
    DORA 42
    		Antagonist
    DORA 42 is a dual orexin 1 and orexin 2 receptor antagonist with sleep efficacy in rats. DORA 42 is promising for research of insomnia.
    DORA 42
  • HY-123737
    MK-8133
    		Antagonist
    MK-8133 is an orexin-2 receptor antagonist. MK-8133 can be used in the study of insomnia.
    MK-8133
  • HY-76612R
    SB-408124 Hydrochloride (Standard)
    		Antagonist
    SB-408124 (Hydrochloride) (Standard) is the analytical standard of SB-408124 (Hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-10805R
    Almorexant (Standard)
    		Antagonist
    Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) 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 reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
    Almorexant (Standard)
  • HY-70068R
    SB-408124 (Standard)
    		Antagonist
    SB-408124 (Standard) is the analytical standard of SB-408124. This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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