orexin receptor (ox receptor)

EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively)

Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain. Seltorexant is a high-affinity and selective orexin-2 receptor antagonist (pKi: 8.0 and 8.1 for human and rat OX2R).

Filorexant (MK-6096) is an orally bioavailable, effective, and selective reversible antagonist of OX1 and OX2 receptors, with (Ki <3 nM).

MK-3697, an isonicotinamide small molecule, acts as a potent and selective Orexin 2 receptor antagonist (Ki: 0.95 nM).

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

ACT-462206 is an orally available Orexin 1/Orexin 2 receptor antagonist that crosses the blood-brain barrier.ACT-462206 is highly potent and can be used in studies of sleep and anxiety.

TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2/3 nM for OX2/1 receptors).

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

MK-1064 (Urokinase inhibitor 1) is a selective orexin 2 receptor antagonist (2-SORA).

TCS-OX2-29 is a potent and selective OX2 receptor antagonist (IC50: 40 nM). It displays >250-fold selectivity for OX2 over OX1.

SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

IPSU is an antagonist of OX2 receptor. IPSU Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors.

SB-334867 free base (SB334867A free base) is a selective orexin-1 (OX1) receptor antagonist. In CHO-OX1 cells, SB-334867 inhibits calcium responses mediated by the human OX1 receptor in a concentration-dependent manner, with a binding pKi value of 7.17 for the human OX1 receptor.

Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.

Orexin B, rat, mouse Acetate (Rat orexin B) is an endogenous agonist at Orexin receptor with Kis of 420 and 36 nM for OX1 and OX2, respectively.

Potent and selective orexin OX2 receptor agonist (EC50 = 28 nM at human OX2 expressed in CHO cells). Displays approximately 100-fold selectivity for OX2 over OX1 (EC50 = 2.75 μM at human OX1 expressed in CHO cells). Depolarizes OX2-expressing histaminergic neurons in mouse brain slices. Increases wake time in wild type mice. Suppresses cataplexy-like symptoms in OX knockout mice. Nagahara et al (2015) Design and synthesis of non-peptide, selective orexin receptor 2 agonists. J.Med.Chem. 58 7931 PMID:26267383 |Irukayama-Tomobe et al (2017) Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models. Proc.Natl.Acad.Sci.USA. 144 5731 PMID:28507129

Orexin B, human-13C6,15N (Human orexin B-13C6,15N) TFA is a variant of Orexin B, human, labeled with 13C and 15N isotopes. This compound acts as an agonist of the orexin receptors (Orexin Receptor, OX Receptor), with Ki values of 420 nM for OXR1 and 36 nM for OXR2. Orexin B, human plays a role in the regulation of appetite, wakefulness, cardiovascular function, and neuroendocrine activity.

Orexin B, human-13C18,15N3 (Human orexin B-13C18,15N3) TFA is the 13C and 15N labeled form of Orexin B, human. This compound acts as an agonist for the orexin receptor (Orexin Receptor, OX Receptor) with Ki values of 420 nM for OXR1 and 36 nM for OXR2. Orexin B, human plays a role in regulating appetite, wakefulness, cardiovascular functions, and neuroendocrine processes.

[Ala11,D-Leu15]-Orexin B acetate is a selective agonist of orexin-2 receptor (OX2) with an EC50 of 0.13 nM, showing 400-fold selectivity over OX1 (52 nM).

Orexin B, human acetate is the acetate form of Orexin B, human. It acts as an agonist for the orexin receptors (Orexin Receptor, OX Receptor), with a Ki of 420 nM for OXR1 and 36 nM for OXR2. Orexin B, human acetate plays a role in modulating appetite, wakefulness, cardiovascular function, and neuroendocrine activity.