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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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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V78552 | Almorexant-13C,d3 (ACT 078573-13C,d3) | Almorexant-13C,d3 is a 13C and deuterium labelled Almorexant. | |
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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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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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V3346 | GSK1059865 | 1191044-58-2 | GSK1059865 is a novel, potent and highly selective OX1R antagonist. |
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V3446 | GSK1059865 HCl | 1191044-58-2 | GSK1059865 is a novel, potent and highly selective OX1R antagonist. |
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V2142 | IPSU | 1373765-19-5 | IPSU is a novel, potent, selective, orally bioavailable and brain penetrant orexin receptor (OX2R) antagonist with potential to be used for insomnia. |
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V2874 | MK-1064 | 1207253-08-4 | MK-1064 (MK1064) is a novel, potent, selective and orally bioavailable antagonist of Orexin OX2 Receptor (OX2R), with the potential to be used for the treatment of insomnia. |
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V4318 | MK-3697 | 1224846-01-8 | MK-3697 is a novel and potent isonicotinamide small molecule that acts as an orally bioavailable, selective Orexin 2 receptor antagonist with Ki of 0.95 nM. |
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V3447 | MK-6096 (Filorexant) | 1088991-73-4 | Filorexant (formerly known as MK-6096) is a novel, orally bioavailable, potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. |
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V2946 | Orexin 2 Receptor Agonist | 1796565-52-0 | Orexin 2 Receptor Agonist is a potent and selective Orexin2 receptor agonist with EC50 of 0.023 μM on OX2R; it is OX2R-selective (OX1R/OX2R EC50 ratio is 70). |
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V69987 | Orexin 2 Receptor Agonist 2 | 2114324-60-4 | Orexin 2 Receptor Agonist 2 is a selective orexin 2 receptor agonist. |
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V76678 | Orexin A (human, rat, mouse) (acetate) (Hypocretin-1 (human, rat, mouse) (acetate)) | Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the BBB (blood-brain barrier)). |
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