OX Receptor

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).

YNT-185 is a nonpeptide, selective agonist of the orexin type-2 receptor (OX2R), with EC50 values of 0.028 μM for OX2R and 2.75 μM for OX1R. Additionally, YNT-185 effectively alleviates symptoms of narcolepsy-cataplexy in mouse models.

Daridorexant hydrochloride (Nemorexant hydrochloride) is a New Dual Orexin Receptor Antagonist. Daridorexant hydrochloride can be used for Insomnia research.

SB-334867 free base (SB334867A free base) is a selective antagonist of the orexin-1 (OX1) receptor.

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).

DORA-22 is a dual orexin receptor antagonist, improves mild stress-induced insomnia with minimal effect on memory

L-368,899 hydrochloride is an orally available and selective nonpeptide oxytocin receptor (OXTR) antagonist for the prevention of preterm labor.L-368,899 hydrochloride prevents oxytocin-induced anti-anomalous pain and anti-nausea, and may be useful for the study of depression.

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)

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

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.

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).

PF3274167 (Cligosiban) is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.

SB-674042 is a potent, selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50 values of 3.76 nM and 531 nM, respectively. SB-674042 is suitable for the treatment of depression.

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

[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, 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.

OXA (17-33) acetate is a more potent agonist of orexin-1 receptor (OX1, EC50 = 8.29 nM)) over OX2 (EC50 = 187 nM).

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).

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

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.

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.