OX Receptor

OX Receptor

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.

OX Receptor related products

Structure Cat No. Product Name CAS No. Product Description
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.
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.
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.
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.
V78552 Almorexant-13C,d3 (ACT 078573-13C,d3) Almorexant-13C,d3 is a 13C and deuterium labelled Almorexant.
V69986 Cudarolimab (IBI101) 2244739-29-3 Cudarolimab (IBI101) is a fully human anti-OX40 (CD134, a costimulatory molecule expressed by activated immune cells) antibody.
V83367 CVN766 1803557-42-7
V69979 Danavorexton (TAK-925) 2114324-48-8 Danavorexton (TAK-925) is a brain-permeable (penetrable) orexin receptor agonist.
V69981 Efizonerimod alfa 1635395-27-5 Efizonerimod alfa is a potent monoclonal antibody (mAb) OX40 activator.
V40710 EMPA 680590-49-2 EMPA is a high-affinity, reversible and specific orexin OX2 receptor antagonist.
V69989 Fazamorexant (YZJ-1139) 1808918-69-5 Fazamorexant (YZJ-1139) is a potent orexin receptor blocker (antagonist).
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).
V69977 Firazorexton hydrate (TAK-994) 2861934-86-1 Firazorexton hydrate (TAK-994) is a potent orexin type 2 receptor (OX2R) agonist (EC50= 19 nM).
V3346 GSK1059865 1191044-58-2 GSK1059865 is a novel, potent and highly selective OX1R antagonist.
V3446 GSK1059865 HCl 1191044-58-2 GSK1059865 is a novel, potent and highly selective OX1R antagonist.
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.
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.
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.
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.
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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