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.

TCS 1102 is a potent, non-selective dual orexin receptor antagonist with Ki values of 0.2 and 3 nM for OX2 and OX1 receptors respectively.

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.

This is a DEA controlled substance schedule IV Suvorexant (also known as MK-4305) is a potent dual OX receptor antagonist with Ki of 0.55 nM and 0.35 nM for OX1 receptor and OX2 receptor, respectively. Suvorexant is developed by Merck for the treatment of insomnia. It is currently undergoing Phase III trials. Suvorexant works by […]

EMPA is a high-affinity, reversible and specific orexin OX2 receptor antagonist.

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.

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.

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

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.

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).