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-P99955
    Rocatinlimab
    		99.95%
    Rocatinlimab (AMG 451) (KHK4083) is a fully human immunoglobulin G1 (IgG1) anti-OX40 monoclonal antibody. Rocatinlimab can be used for the research of atopic dermatitis (AD).
    Rocatinlimab
  • HY-106224
    Orexin A (human, rat, mouse)
    		Agonist 99.93%
    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 (human, rat, mouse)
  • HY-10895
    SB-334867
    		Antagonist 99.48%
    SB-334867 (SB 334867A) is an excellent,selective and blood-brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
    SB-334867
  • HY-133898
    Danavorexton
    		Activator 99.56%
    Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms.
    Danavorexton
  • HY-106224B
    Orexin A (human, rat, mouse) acetate
    		Agonist 99.67%
    Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate 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) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging.
    Orexin A (human, rat, mouse) acetate
  • HY-106224AS1
    Orexin A-13C18,15N3 (human, rat, mouse) TFA
    		98.60%
    Orexin A-13C18,15N3 (human, rat, mouse) ((Hypocretin-1-13C18,15N3 (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>18</sub>,<sup>15</sup>N<sub>3</sub> (human, rat, mouse) TFA
  • HY-P1339AS1
    Orexin B, human-13C18,15N3 TFA
    Orexin B, human-13C18,15N3 (Human orexin B-13C18,15N3) TFA is the 13C- and 15N-labeled Orexin B, human (HY-P1339). Orexin B, human is the agonist for Orexin Receptor, with Kis of 420 nM and 36 nM for OX1 and OX2. Orexin B, human participates in the regulation of appetite, wakefulness, cardiovascular function and neuroendocrine.
    Orexin B, human-<sup>13</sup>C<sub>18</sub>,<sup>15</sup>N<sub>3</sub> TFA
  • HY-P1339AS
    Orexin B, human-13C6,15N TFA
    Orexin B, human-13C6,15N (Human orexin B-13C6,15N) TFA is the 13C- and 15N-labeled Orexin B, human (HY-P1339). Orexin B, human is the agonist for Orexin Receptor, with Kis of 420 nM and 36 nM for OX1 and OX2. Orexin B, human participates in the regulation of appetite, wakefulness, cardiovascular function and neuroendocrine.
    Orexin B, human-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N TFA
  • HY-10805
    Almorexant
    		Antagonist 99.96%
    Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
    Almorexant
  • HY-P1339A
    Orexin B, human TFA
    		Agonist 99.46%
    Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.
    Orexin B, human TFA
  • HY-159835
    Oveporexton
    		Agonist 99.68%
    Oveporexton (TAK-861) is an orally active and selective orexin receptor 2 (OX2R) agonist with an EC50 of 2.5 nM. Oveporexton exhibits 3000-fold selectivity for OX2R over OX1R. Oveporexton can be used for the study of hypersomnia disorders including narcolepsy.
    Oveporexton
  • HY-109012
    Seltorexant
    		Antagonist 99.83%
    Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
    Seltorexant
  • HY-139559
    Vornorexant
    		Antagonist 98.41%
    Vornorexant (ORN-0829; TS-142) is a potent dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively. Vornorexant exhibits potent sleep-promoting effects in vivo and can be used for insomnia research research.
    Vornorexant
  • HY-15653
    Filorexant
    		Antagonist 99.40%
    Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
    Filorexant
  • HY-100452
    TCS-OX2-29
    		Antagonist 99.17%
    TCS-OX2-29 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
  • HY-10805A
    Almorexant hydrochloride
    		Antagonist 99.98%
    Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
    Almorexant hydrochloride
  • HY-P1339B
    Orexin B, human acetate
    		Agonist 99.68%
    Orexin B, human acetate is the acetate form of Orexin B, human (HY-P1339). Orexin B, human acetate is the agonist for Orexin Receptor, with Ki of 420 nM and 36 nM for OX1 and OX2. Orexin B, human acetate participates in the regulation of appetite, wakefulness, cardiovascular function and neuroendocrine.
    Orexin B, human acetate
  • HY-10896
    JNJ-10397049
    		Antagonist 99.19%
    JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R.
    JNJ-10397049
  • HY-106224A
    Orexin A (human, rat, mouse) TFA
    		Agonist 98.13%
    Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA 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) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
    Orexin A (human, rat, mouse) TFA
  • HY-154789
    RTIOXA-43
    		Agonist 99.94%
    RTIOXA-43 is a orexin receptor agonist with EC50s of 24 nM and 24 nM for OX2 and OX1 receptors, respectively.
    RTIOXA-43
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.