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-P1349A
    Orexin B, rat, mouse TFA
    		Agonist
    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-152843
    Fazamorexant
    		Antagonist 99.73%
    Fazamorexant (YZJ-1139) is a potent orexin receptor antagonist. Fazamorexant can be used for insomnia research.
    Fazamorexant
  • HY-138695
    Orexin 2 Receptor Agonist 2
    		Agonist 98.06%
    Orexin 2 Receptor Agonist 2 is a selective orexin 2 receptor agonist, extracted from patent WO2017135306A1, example 16.
    Orexin 2 Receptor Agonist 2
  • HY-136922
    Orexin receptor antagonist 2
    		Antagonist 98.04%
    Orexin receptor antagonist 2 (compound 30) is a potent orexin receptor antagonist with pKis of 7.69 and 9.78. Orexin receptor antagonist 2 has the potential for the research of insomnia.
    Orexin receptor antagonist 2
  • HY-P99911
    Efizonerimod alfa
    		Activator 98.57%
    Efizonerimod alfa is a potent monoclonal antibody OX40 activator. Efizonerimod alfa can be used for cancer research.
    Efizonerimod alfa
  • HY-137093
    Orexin receptor antagonist 3
    		Antagonist 99.62%
    Orexin receptor antagonist 3 (example 216) is an orexin receptor antagonist, which is extracted from the patent WO2011050198A1.
    Orexin receptor antagonist 3
  • HY-137452
    Suntinorexton
    		Agonist 98.66%
    Suntinorexton, a heterocyclic compound, is an orexin type 2 receptor agonist extracted from patent WO2019027058A1, page 288.
    Suntinorexton
  • HY-13796
    IPSU
    		Antagonist 98.10%
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
    IPSU
  • 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-100452A
    TCS-OX2-29 hydrochloride
    		Antagonist
    TCS-OX2-29 (hydrochloride) 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 hydrochloride
  • HY-162235
    CVN766
    		Antagonist
    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-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-153458
    Orexin receptor modulator-1
    		Modulator
    Orexin receptor modulator-1 is an orexin receptor modulator. Orexin receptor modulator-1 can be used for the research of substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension.
    Orexin receptor modulator-1
  • HY-P1340A
    [Ala11,D-Leu15]-Orexin B(human) TFA
    		Agonist
    [Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM).
    [Ala11,D-Leu15]-Orexin B(human) TFA
  • HY-137452A
    (R,R)-Suntinorexton
    		Agonist
    (R,R)-Suntinorexton is a isomeride of Suntinorexton (HY-137452). Suntinorexton is a orexin type 2 receptor agonist.
    (R,R)-Suntinorexton
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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