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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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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V2576 | Almorexant (ACT 078573) | 871224-64-5 | Almorexant (also known as ACT078573) is a novel, potent, orally bioactive, competitive and dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. |
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V1308 | Almorexant HCl (ACT 078573) | 913358-93-7 | Almorexant HCl (also known as ACT-078573; ACT078573), the hydrochloride salt of Almorexant, is a novel, potent, orally bioactive, competitive and dual orexin1/2 receptor antagonist indicated for the treatment of sleep disorders/insomnia. |
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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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V69986 | Cudarolimab (IBI101) | 2244739-29-3 | Cudarolimab (IBI101) is a fully human anti-OX40 (CD134, a costimulatory molecule expressed by activated immune cells) antibody. |
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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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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. |
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V23883 | Lemborexant (E-2006) | 1369764-02-2 | Lemborexant (E2006; E-2006; Dayvigo) is a novel, reversible, competitive and orally bioactive dual antagonist of the orexin OX1 and OX2 receptors (IC50 values of 6.1 nM and 2.6 nM, respectively) which was under development by Eisai for the treatment of 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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