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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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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V76677 | Orexin A (human, rat, mouse) (TFA) (Hypocretin-1 (human, rat, mouse) (TFA)) | Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA is a 33-amino acid (AA) excitatory neuropeptide involved in a variety of central and peripheral processes. | |
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V31846 | Orexin A human, rat, mouse | 205640-90-0 | Orexin A human, rat, mouse is a novel and potent peptide consisting of 33 amino acids, acting as a highly specific and high-affinity agonist for OX1/2R (Ki of 20 and 38 nM for OX1 and OX2 receptors respectively), which is a G-protein-coupled receptor. |
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V76676 | Orexin B, human TFA (Human orexin B TFA) | Orexin B, human (TFA) is an endogenous agonist of the Orexin receptor, binding to OX1 and OX2 with Kis of 420 and 36 nM, respectively. | |
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V76675 | Orexin B, rat, mouse TFA (Rat orexin B TFA; Orexin B (mouse) (TFA)) | Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor (Orexin receptor) agonist. | |
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V69992 | Orexin receptor antagonist 2 | 1457940-75-8 | Orexin receptor antagonist 2 is a potent orexin receptor antagonist (inhibitor) with pKi of 7.69 and 9.78 respectively. |
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V69991 | Orexin receptor antagonist 3 | 1293282-55-9 | Orexin receptor antagonist 3 (example 216) is an antagonist of the orexin receptor, and the information comes from example 216 of patent WO2011050198A1. |
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V69982 | Orexin receptor modulator-1 | 2125735-57-9 | Orexin receptor modulator-1 is an orexin receptor modulator. |
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V83668 | OX2R-IN-2 | ||
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V69983 | OXA(17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) | 343268-91-7 | OXA(17-33) is a potent and specific orexin-1 receptor (OX1) agonist. |
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V81021 | OXA(17-33) TFA (Orexin A (17-33) (human, mouse, rat, bovine) TFA) | OXA(17-33) TFA is a potent and specific orexin-1 receptor (OX1) agonist. | |
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V69984 | Revdofilimab (ABBV-368) | 2230138-89-1 | Revdofilimab (ABBV-368) is a human IgG1 agonist monoclonal antibody (mAb) directed against OX 40. |
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V69996 | RTIOXA-43 | 2832067-72-6 | RTIOXA-43 is an orexin receptor agonist (activator) with EC50s of 24 nM for both OX2 and OX1 receptors. |
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V2577 | SB-334867 | 792173-99-0 | SB-334867 is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with a pKb value of 7.2. |
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V1309 | SB-334867 HCl | 249889-64-3 | SB-334867 HCl (SB-334867A; SB334867; SB 334867),the hydrochloride salt ofSB-334867, is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with the potential for treating sleeping disorders. |
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V3343 | SB-649868 | 380899-24-1 | SB-649868 (GSK-649868) is a novel, potent, selective and orally bioactive orexin (OX) 1 and OX2 receptor antagonist with pKi of 9.4 and 9.5 for OX1 and OX2 receptor, respectively. |
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V4615 | SB-674042 | 483313-22-0 | SB-674042 is a novel, potent and selective non-peptide orexin OX1 receptor antagonist with Kd of 3.76 nM; It exhibits 100-fold selectivity for OX1 over OX2 receptors. |
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