Orexin Receptor (OX Receptor)
Hypocretin Receptor; HCRT Receptor
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
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Orexin Receptor (OX Receptor) Inhibitors
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Orexin Receptor (OX Receptor) Agonists
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Orexin Receptor (OX Receptor) Antagonists
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Orexin Receptor (OX Receptor) Activators
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Orexin Receptor (OX Receptor) Modulators
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Orexin Receptor (OX Receptor) Related Products (130)
Related Products (130)
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Antibodies (2)
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Orexin Receptor (OX Receptor) Isoform Comparison
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23ME-00610
0 ImagesCat. No.: HY-P99216223ME-00610 is a humanized effector-function-null IgG1 antibody targeting CD200R1, with a Kd of <0.1 nM for hCD200R1. 23ME-00610 blocks the binding of CD200 to CD200R1 and inhibits the recruitment of the downstream adaptor protein DOK2 to CD200R1. 23ME-00610 restores IL-2 production suppressed by CD200. 23ME-00610 induces cytokine production in cells. 23ME-00610 enhances cell-mediated tumor cell killing in vitro. 23ME-00610 can be used for melanoma research.
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OX2R-IN-1
0 ImagesCat. No.: HY-149014CAS No.: 2639148-08-4OX2R-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.
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INCAGN1949
0 ImagesCat. No.: HY-P991334INCAGN1949 is a human IgG1 monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. INCAGN1949 selectively deplete intratumoral regulatory T cells.
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DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite
0 ImagesCat. No.: HY-402873CAS No.: 2382942-38-1DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite (Compound 5) is an RNAi agent and an inhibitor of Ataxin-2 (ATXN2). DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite can be studied in research on ATXN2-associated neurological diseases.
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Orexin receptor antagonist 7
0 ImagesCat. No.: HY-177790CAS No.: 2096315-41-0Orexin receptor antagonist 7 (Compound 34) is an antagonist of the orexin receptor (OX1R), with a Ki value of 4.05 nM. Orexin receptor antagonist 7 shows no detectable activity towards OX2R and has very low affinities for the three opioid receptors (μ, δ, κ) (Ki > 1,000 nM). Orexin receptor antagonist 7 can be used for research on opioid addiction.
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OX2R agonist 3
0 ImagesCat. No.: HY-163276OX2R agonist 3 (compound 63c) is an agonist for orexin receptor type 2 (OX2R) with EC50 of 339 nM. OX2R agonist 3 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells
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Rocavorexant
0 ImagesCat. No.: HY-172436CAS No.: 2115665-09-1Rocavorexant is the antagonist for orexin-1 receptor with pIC50 of 9.1 for human OX1 (while pIC50 for human OX2 is 6.0).
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OX2R agonist 1
0 ImagesCat. No.: HY-159731CAS No.: 2648347-78-6OX2R agonist 1 is an OX2R antagonist with an EC50 of less than 100 nM. OX2R agonist 1 can be used in research related to excessive daytime sleepiness or narcolepsy.
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SB-334867 (Standard)
0 ImagesSynonyms: SB 334867A (Standard)SB-334867 (Standard) is the analytical standard of SB-334867. This product is intended for research and analytical applications. 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.
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Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86)
0 ImagesCat. No.: HY-P990176Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) is an anti-mouse OX40/CD134 (LALA-PG) IgG2a monoclonal antibody. Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) is a chimeric antibody of the original OX86 antibody (HY-P990115). Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) can significantly enhance the generation of antigen-specific effector T cells. Anti-Mouse OX40/CD134 (LALA-PG) Antibody (OX86) can be used for research on cancer .
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MEDI-6469
0 ImagesCat. No.: HY-P991338Purity: 98.3%MEDI-6469 is a human monoclonal antibody (mAb) targeting TNFRSF4/OX40/CD134. MEDI-6469 targets the OX40 receptor on activated T cells to enhance the immune response against cancer cells..
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ACT-462206 (Standard)
0 ImagesCat. No.: HY-101834RCAS No.: 1361321-96-1ACT-462206 (Standard) is the analytical standard of ACT-462206 (HY-101834). This product is intended for research and analytical applications. ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research.
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OX2R agonist-4
0 ImagesCat. No.: HY-187354CAS No.: 3132407-42-9OX2R agonist-4 is an orexin receptor type 2 (OX2R) agonist with an EC50 value of 0.061 nM against human OX2R. OX2R agonist-4 can be used in studies related to narcolepsy.
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Orexin receptor antagonist 6
0 ImagesCat. No.: HY-179324CAS No.: 1451412-34-2Orexin receptor antagonist 6 (Compound 72) is a selective orexin 1 receptor (OX1) antagonist with a Ke of 8.5 nM and > 1180-fold selectivity for OX2. Orexin receptor antagonist 6 does not produce its own conditioned place preference (CPP) or aversive effects, and can inhibit the formation of CPP induced by psychoactive substances. Orexin receptor antagonist 6 can be used for research of neurological disease.
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SB-674042 (Standard)
0 ImagesCat. No.: HY-10898RCAS No.: 483313-22-0SB-674042 (Standard) is the analytical standard of SB-674042 (HY-10898). This product is intended for research and analytical applications. SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively.
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TCS-OX2-29 (Standard)
0 ImagesCat. No.: HY-100452RCAS No.: 372523-75-6TCS-OX2-29 (Standard) is the analytical standard of TCS-OX2-29 (HY-100452). This product is intended for research and analytical applications. 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.
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DORA 42
0 ImagesCat. No.: HY-113555CAS No.: 1030377-48-0DORA 42 is a dual orexin 1 and orexin 2 receptor antagonist with sleep efficacy in rats. DORA 42 is promising for research of insomnia.
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TCS 1102 (Standard)
0 ImagesCat. No.: HY-10900RCAS No.: 916141-36-1TCS 1102 (Standard) is the analytical standard of TCS 1102 (HY-10900). This product is intended for research and analytical applications. TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats.
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EMPA (Standard)
0 ImagesCat. No.: HY-108682RCAS No.: 680590-49-2EMPA (Standard) is the analytical standard of EMPA (HY-108682). This product is intended for research and analytical applications. EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with Kd values of 1.1 and 1.4 nM respectively.
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Seltorexant hydrochloride (Standard)
0 ImagesCat. No.: HY-109012ARCAS No.: 1293284-49-7Synonyms: JNJ-42847922 hydrochloride (Standard)Seltorexant hydrochloride (Standard) is the analytical standard of Seltorexant (hydrochloride) (HY-109012A). This product is intended for research and analytical applications. Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
