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-162977
    Orexin receptor activator-1
    		Activator
    Orexin receptor activator-1 is an Orexin Receptor agonist. Orexin receptor activator-1 can be used to study orexin-related diseases.
    Orexin receptor activator-1
  • HY-P992462
    SHR-1806
    		Agonist
    SHR-1806 is a OX40 agonist and a NF-κB activator, with antitumor activity. SHR-1806 mediates ADCC and CDC effects, enhances the function and expansion of effector T cells, suppresses regulatory T cells, and increases γ-interferon secretion. SHR-1806 exhibits typical pharmacokinetic characteristics and favorable safety profiles. SHR-1806 can be used in studies related to solid tumors and colon cancer.
    SHR-1806
  • HY-161567
    OX2R-IN-3
    		Antagonist
    OX2R-IN-3 (Compound 53) is an orally active type 2 orexin receptor (OX2R) agonist (EC50<100 nM.).
    OX2R-IN-3
  • HY-P3867
    Hypocretin (70-98), human
    		Agonist
    Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes apoptosis.
    Hypocretin (70-98), human
  • HY-P991339
    ZL-1101
    		Inhibitor
    ZL-1101 is a human monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134.
    ZL-1101
  • HY-P99434A
    Amlitelimab (FUT8-KO)
    		Inhibitor
    Amlitelimab (FUT8-KO) is Amlitelimab (HY-P99434) expressed in cells with the fucosyltransferase 8 gene (FUT8) knocked out. Amlitelimab (KY1005) is a monoclonal antibody (mAb) against OX40 ligand (OX40L). Amlitelimab inhibits the OX40-OX40L interaction and can be used for research on atopic dermatitis.
    Amlitelimab (FUT8-KO)
  • HY-171032B
    YNT-3708
    		Agonist
    YNT-3708 is an orexin receptor (OXR) agonist, with EC50 values of 14.6 nM and 277 nm for OX1R and OX2R, respectively.
    YNT-3708
  • HY-106224AS
    Orexin A-13C5,15N (human, rat, mouse) TFA
    Orexin A-13C6,15N (human, rat, mouse) (Hypocretin-1-13C6,15N (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.
    Orexin A-<sup>13</sup>C<sub>5</sub>,<sup>15</sup>N (human, rat, mouse) TFA
  • HY-177085
    Fumiporexant
    		Antagonist
    Fumiporexant (Compound Example 93) is an orally active, brain-penetrant and selective Orexin receptor 2 (OX2R) antagonist. Fumiporexant regulates the sleep-wake cycle and emotion-related pathways in the central nervous system. Fumiporexant is promising for research of nervous system diseases such as insomnia and major depressive disorder.
    Fumiporexant
  • HY-P10079
    Xenopus orexin A
    		Activator
    Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin A is a potent agonist of OX1R.
    Xenopus orexin A
  • HY-P1341A
    OXA(17-33) TFA
    		Agonist
    OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM).
    OXA(17-33) TFA
  • HY-146517
    Orexin receptor antagonist 4
    		Antagonist
    Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist with an IC50 of 4.27 nM. Orexin receptor antagonist 4 is 61-fold selective for the OX2R over the OX1R (IC50 of 295 nM) (WO2018206959A1; example 1).
    Orexin receptor antagonist 4
  • HY-P991452
    Anti-CD200R1/OX2R Antibody (I-4P)
    		Inhibitor
    Anti-CD200R1/OX2R Antibody (I-4P) is a human monoclonal antibody (mAb) targeting CD200R1/OX2R. Anti-CD200R1/OX2R Antibody (I-4P) can be used in solid tumors research. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-CD200R1/OX2R Antibody (I-4P)
  • 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-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-P992162
    23ME-00610
    		Inhibitor
    23ME-00610 is a humanized effector-function-null IgG1 antibody targeting CD200R1, with a Kd of <0.1 nM for hCD200R1. 23ME-00610 blocks the binding of CD200 to CD200R1 and inhibits the recruitment of the downstream adaptor protein DOK2 to CD200R1. 23ME-00610 restores IL-2 production suppressed by CD200. 23ME-00610 induces cytokine production in cells. 23ME-00610 enhances cell-mediated tumor cell killing in vitro. 23ME-00610 can be used for melanoma research.
    23ME-00610
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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