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-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-177790
    Orexin receptor antagonist 7
    		Antagonist
    Orexin receptor antagonist 7 (Compound 34) is an antagonist of the orexin receptor (OX1R), with a Ki value of 4.05 nM. Orexin receptor antagonist 7 shows no detectable activity towards OX2R and has very low affinities for the three opioid receptors (μ, δ, κ) (Ki > 1,000 nM). Orexin receptor antagonist 7 can be used for research on opioid addiction.
    Orexin receptor antagonist 7
  • HY-163276
    OX2R agonist 3
    		Agonist
    OX2R agonist 3 (compound 63c) is an agonist for orexin receptor type 2 (OX2R) with EC50 of 339 nM. OX2R agonist 3 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells
    OX2R agonist 3
  • 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-P990176
    Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86)
    		Agonist
    Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) is an anti-mouse OX40/CD134 (LALA-PG) IgG2a monoclonal antibody. Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) is a chimeric antibody of the original OX86 antibody (HY-P990115). Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) can significantly enhance the generation of antigen-specific effector T cells. Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) can be used for research on cancer .
    Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86)
  • HY-P991338
    MEDI-6469
    		Inhibitor 98.3%
    MEDI-6469 is a human monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. MEDI-6469 targets the OX40 receptor on activated T cells to enhance the immune response against cancer cells..
    MEDI-6469
  • HY-101834R
    ACT-462206 (Standard)
    		Antagonist
    ACT-462206 (Standard) is the analytical standard of ACT-462206 (HY-101834). This product is intended for research and analytical applications. 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 (Standard)
  • HY-179324
    Orexin receptor antagonist 6
    		Antagonist
    Orexin receptor antagonist 6 (Compound 72) is a selective orexin 1 receptor (OX1) antagonist with a Ke of 8.5 nM and > 1180-fold selectivity for OX2. Orexin receptor antagonist 6 does not produce its own conditioned place preference (CPP) or aversive effects, and can inhibit the formation of CPP induced by psychoactive substances. Orexin receptor antagonist 6 can be used for research of neurological disease.
    Orexin receptor antagonist 6
  • HY-10898R
    SB-674042 (Standard)
    		Antagonist
    SB-674042 (Standard) is the analytical standard of SB-674042 (HY-10898). This product is intended for research and analytical applications. 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 (Standard)
  • HY-100452R
    TCS-OX2-29 (Standard)
    		Antagonist
    TCS-OX2-29 (Standard) is the analytical standard of TCS-OX2-29 (HY-100452). This product is intended for research and analytical applications. 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 (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-10900R
    TCS 1102 (Standard)
    		Antagonist
    TCS 1102 (Standard) is the analytical standard of TCS 1102 (HY-10900). This product is intended for research and analytical applications. 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 (Standard)
  • HY-108682R
    EMPA (Standard)
    		Antagonist
    EMPA (Standard) is the analytical standard of EMPA (HY-108682). This product is intended for research and analytical applications. 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 (Standard)
  • HY-109012AR
    Seltorexant hydrochloride (Standard)
    		Antagonist
    Seltorexant hydrochloride (Standard) is the analytical standard of Seltorexant (hydrochloride) (HY-109012A). This product is intended for research and analytical applications. 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 (Standard)
  • HY-109012R
    Seltorexant (Standard)
    		Antagonist
    Seltorexant (Standard) is the analytical standard of Seltorexant (HY-109012). This product is intended for research and analytical applications. Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
    Seltorexant (Standard)
  • HY-10896R
    JNJ-10397049 (Standard)
    		Antagonist
    JNJ-10397049 (Standard) is the analytical standard of JNJ-10397049 (HY-10896). This product is intended for research and analytical applications. JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R.
    JNJ-10397049 (Standard)
  • HY-10805AR
    Almorexant hydrochloride (Standard)
    		Antagonist
    Almorexant hydrochloride (Standard) is the analytical standard of Almorexant (hydrochloride) (HY-10805A). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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