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-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 98.08%
    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-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
  • HY-171032A
    (S)-YNT-3708
    		Agonist 99.80%
    (S)-YNT-3708, the S-enantiomer of YNT-3708, with low activity for OX1R and OX2R (EC50 = 3595 nM and 1661 nm, respectively).
    (S)-YNT-3708
  • 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-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-172412A
    Alixorexton enantiomer
    		Agonist 99.42%
    Alixorexton (ALKS 2680) enantiomer is the enantiomer of Alixorexton (HY-172412). Alixorexton is a selective, orally active and brain-penetrant agonist for orexin-2 receptor and can be used for hypersomnias research.
    Alixorexton enantiomer
  • HY-13796
    IPSU
    		Antagonist 98.0%
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
    IPSU
  • HY-12301
    MK-3697
    		Antagonist 98.83%
    MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.
    MK-3697
  • 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-162712
    OX-201
    		Agonist
    OX-201 is an orally active, blood-brain barrier-permeable OX2R agonist with an EC50 of 8.0 nM. OX-201 activates OX2R to induce wakefulness and neuronal activation. OX-201 promotes the release of neuron activity-dependent tau protein from neurons into the interstitial fluid of hippocampal tissues. OX-201 is applicable to research related to Alzheimer's disease and tauopathies.
    OX-201
  • HY-178871
    OX2-2303
    		Antagonist
    OX2-2303 is a potent, selective orexin-2 receptor (OX2R) antagonist. OX2-2303 exhibits excellent binding affinity towards OX2R (Ki = 0.1 nM), and shows >890-fold selectivity over OX1R. OX2-2303 can be used as a positron emission tomography (PET) radioligand for central nervous system (CNS) research.
    OX2-2303
  • HY-168571
    BTF
    BTF shows a selective binding affinity for OX1R with the Ki values of 2.33 nM and 62.8 nM of OX1R and OX2R, respectively.
    BTF
  • 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-P5830A
    Biotin-DEVD-CHO TFA
    		Inhibitor
    Biotin-DEVD-CHO (TFA) is a biotin-conjugated form of the caspase-3 and -7 inhibitor – Ac-DEVD-CHO. Biotin-DEVD-CHO (TFA) can be used for affinity purification of the active caspase-3, -6, -7, and -8. Biotin-DEVD-CHO (TFA) can detect the active caspase-3 in vitro.
    Biotin-DEVD-CHO TFA
  • HY-172672
    Orexin 2 Receptor Agonist 3
    		Agonist
    Orexin 2 Receptor Agonist 3 (Compound 57) is an orally active and brain-penetrant orexin receptor type-2 (OX2) agonist (EC50: 2.5 nM). Orexin 2 Receptor Agonist 3 increases wakefulness in the orexin/ataxin-3 NT1 mouse model and healthy beagle dogs. Orexin 2 Receptor Agonist 3 can be used in the study of narcolepsy.
    Orexin 2 Receptor Agonist 3
  • HY-P992141
    Vedastotug
    		Inhibitor
    Vedastotug is a human monoclonal antibody targeting TNFRSF4/OX40/CD134, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001).
    Vedastotug
  • HY-177096
    Ledasorexton
    		Agonist
    Ledasorexton is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect in mice. Ledasorexton can be used for research of neurological disease.
    Ledasorexton
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.