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

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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) Related Products (61):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-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-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-13796
    IPSU
    		Antagonist 98.10%
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
    IPSU
  • 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-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-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-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-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-137452
    Suntinorexton
    		Agonist
    Suntinorexton, a heterocyclic compound, is an orexin type 2 receptor agonist extracted from patent WO2019027058A1, page 288.
    Suntinorexton
  • 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-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
  • HY-163276
    OX2R-IN-2
    		Agonist
    OX2R-IN-2 (compound 63c) is an agonist for orexin receptor type 2 (OX2R) with EC50 of 339 nM. OX2R-IN-2 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells
    OX2R-IN-2