Orexin receptor 1 (OX1R) and orexin receptor 2 (OX2R) subtypes make up the family of G protein-coupled receptors known as orexin receptors (hypocretin receptors). Orexin receptors play a role in the control of the sleep/wake cycle and are expressed throughout the central nervous system.
Orexin B binds to OX2 with a higher affinity than OX1R, while orexin A binds to OX1R and OX2R with similar affinities. The prefrontal and infralimbic cortex, hippocampus, paraventricular thalamic nucleus, and locus coeruleus are the primary sites of OX1R expression. The cerebral cortex, septal nuclei, lateral hypothalamus, hippocampus, and hypothalamic nuclei are where OX2R is primarily found.
Gq/11 connects the OX1R and OX2R receptors to the activation of phospholipase C, which raises intracellular Ca2+ levels. Furthermore, OX2R connects to the cAMP pathways via Gs and Gi/o.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69995 | (2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) | 2692692-00-3 | (2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton. |
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V105300 | (R)-YNT-3708 | 2923137-94-2 | (R)-YNT-3708 is a selective orexin 1 (OX1R) agonist with EC50 of 7.48 nM. |
|
V122231 | (S)-YNT-3708 | 2923138-00-3 | (S)-YNT-3708 is the S-enantiomer of YNT-3708, with low activity for OX1R and OX2R (EC50 of 3595 nM and 1661 nm, respectively). |
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V3345 | JNJ-10397049 | 708275-58-5 | JNJ-10397049 is a novel, potent, selective and orally bioavailable antagonist of OX2 receptor with pIC50 of 7.4 for chimeric OX2 receptors, pKB values of 5.9 and 8.5 for OX1 and OX2 receptors respectively. |
![[Ala11,D-Leu15]-Orexin B(human) TFA](http://www.invivochem.com/upload/1124/V77467.png)
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V77467 | [Ala11,D-Leu15]-Orexin B(human) TFA | [Ala11,D-Leu15]-Orexin B(human) TFA is a potent and specific orexin-2 receptor (OX2) agonist. | |
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V128528 | Alixorexton | 2648347-56-0 | Alixorexton is an orally bioavailable, blood-brain barrier-crossing selective OX2R activator and wake-up agent. |
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V114505 | Alixorexton enantiomer | 2648350-16-5 | The enantiomer of Alixorexton (ALKS 2680) is the enantiomer of Alixorexton. |
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V78552 | Almorexant-13C,d3 (ACT 078573-13C,d3) | Almorexant-13C,d3 is a 13C and deuterium labelled Almorexant. | |
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V128754 | Amlitelimab (FUT8-KO) | Amlitelimab (FUT8-KO) is Amlitelimab expressed in cells with the fucosyltransferase 8 gene (FUT8) knocked out. | |
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V130181 | Biotin-DEVD-CHO TFA | Biotin-DEVD-CHO TFA is a biotin-conjugated form of the caspase-3 and -7 inhibitor Ac-DEVD-CHO. | |
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V131897 | Cleminorexton | 2980518-93-0 | Cleminorexton is an orally effective orexin-2 receptor (OX2R) agonist with a pEC50 between 9 and 10.4. |
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V83367 | CVN766 | 1803557-42-7 | |
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V69979 | Danavorexton (TAK-925) | 2114324-48-8 | Danavorexton (TAK-925) is a brain-permeable (penetrable) orexin receptor agonist. |
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V134093 | DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite | 2382942-38-1 | DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite is an RNAi reagent and an inhibitor of conamin-2 (ATXN2). |
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V69981 | Efizonerimod alfa | 1635395-27-5 | Efizonerimod alfa is a potent monoclonal antibody (mAb) OX40 activator. |
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V40710 | EMPA | 680590-49-2 | EMPA is a high-affinity, reversible and specific orexin OX2 receptor antagonist. |
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V69989 | Fazamorexant (YZJ-1139) | 1808918-69-5 | Fazamorexant (YZJ-1139) is a potent orexin receptor blocker (antagonist). |
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V69988 | Firazorexton (TAK-994 free base) | 2274802-95-6 | Firazorexton (TAK-994 free base) is an orally bioavailable orexin type 2 receptor (OX2R) agonist (EC50=19 nM). |
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V69977 | Firazorexton hydrate (TAK-994) | 2861934-86-1 | Firazorexton hydrate (TAK-994) is a potent orexin type 2 receptor (OX2R) agonist (EC50= 19 nM). |
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V136398 | Fumiporexant | 2839408-03-4 | Fumiporexant is an orally effective, selective orexin receptor 2 (OX2R) antagonist that can cross the blood-brain barrier. |
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