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)

Related Products

PDF 0.59 MB

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-152843
    Fazamorexant
    		Antagonist 99.73%
    Fazamorexant (YZJ-1139) is a potent orexin receptor antagonist. Fazamorexant can be used for insomnia research.
    Fazamorexant
  • HY-108683
    ACT-335827
    		Antagonist ≥98.0%
    ACT-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.
    ACT-335827
  • 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-P1349
    Orexin B, rat, mouse
    		Agonist
    Orexin B, rat, mouse (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
    Orexin B, rat, mouse
  • 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-134188
    JNJ-54717793
    		Antagonist 98.06%
    JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
    JNJ-54717793
  • 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-123176
    GYKI-13380
    		Inhibitor
    GYKI-13380 is an appetite suppressant. GYKI-13380 has the potential for the research of neurology diseases.
    GYKI-13380
  • 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-162712
    OX-201
    		Agonist
    OX-201 is a selective agonist for OX2R with an EC50 of 8 nM. Pathological proteins produced by neurons are released into the interstitial fluid (ISF) in a manner dependent on neuronal activity and are cleared from the brain via lymphatic pathways. The outflow of pathological proteins to the ISF is related to the arousal state of neurons. OX-201 can induce neuronal awakening and promote the release of tau into the hippocampal ISF. Although OX-201 does not alter hippocampal tau levels, it has potential applications for Alzheimer's disease (AD) associated with sleep/wake rhythm disturbances.
    OX-201
  • 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-159835
    Oveporexton
    		Agonist
    Oveporexton is an orexin type 2 receptor (OX2R) agonist.
    Oveporexton
  • HY-137452A
    (R,R)-Suntinorexton
    		Agonist 99.13%
    (R,R)-Suntinorexton is a isomeride of Suntinorexton (HY-137452). Suntinorexton is a orexin type 2 receptor agonist.
    (R,R)-Suntinorexton
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.