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-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-P991335
    BAT6026
    		Inhibitor
    BAT6026 is a human monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. BAT6026 significantly reduces Treg cells and increased CD8+ T cells in tumor.
    BAT6026
  • 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-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-177096
    Ledasorexton
    		Agonist
    Ledasorexton (Example 1 ) is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect.
    Ledasorexton
  • 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-P991339
    ZL-1101
    		Inhibitor
    ZL-1101 is a human monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134.
    ZL-1101
  • HY-171032B
    YNT-3708
    		Agonist
    YNT-3708 is an orexin receptor (OXR) agonist, with EC50 values of 14.6 nM and 277 nm for OX1R and OX2R, respectively.
    YNT-3708
  • HY-P991613
    BGB-A445
    		Ligand
    BGB-A445 is a humanized non-ligand-blocking agonistic OX40 monoclonal antibody with high affinity to OX40. BGB-A445 activates downstream NF-κB pathway to induce immune cell activation, proliferation, and survival. BGB-A445 dose-dependently and significantly depletes regulatory T cells via antibody-dependent cellular cytotoxicity (ADCC). BGB-A445 demonstrates robust and dose-dependent antitumor efficacy in the MC38 mice models. BGB-A445 can be used for the researches of cancer, such as colon adenocarcinoma.
    BGB-A445
  • HY-147403S
    Tebideutorexant
    		Antagonist
    Tebideutorexant (JNJ-61393215) is a potent orexin receptor antagonist. Tebideutorexant can be used for insomnia research.
    Tebideutorexant
  • HY-177085
    Fumiporexant
    		Antagonist
    Fumiporexant (Compound Example 93) is an orally active, brain-penetrant and selective Orexin receptor 2 (OX2R) antagonist. Fumiporexant regulates the sleep-wake cycle and emotion-related pathways in the central nervous system. Fumiporexant is promising for research of nervous system diseases such as insomnia and major depressive disorder.
    Fumiporexant
  • 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
  • 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-P991452
    Anti-CD200R1/OX2R Antibody (I-4P)
    		Inhibitor
    Anti-CD200R1/OX2R Antibody (I-4P) is a human monoclonal antibody (mAb) targeting CD200R1/OX2R. Anti-CD200R1/OX2R Antibody (I-4P) can be used in solid tumors research. Recommended isotype control: Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-CD200R1/OX2R Antibody (I-4P)
Cat. No. Product Name / Synonyms Application Reactivity
Orexin Receptor (OX Receptor) Isoform Comparison

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