hypocretin 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.

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.

Hypocretin (70-98), human, is a polypeptide that binds to the orexin receptor OX1R and facilitates apoptosis [1].

Orexin A-13C18,15N3 (human, rat, mouse) ((Hypocretin-1-13C18,15N3 (human, rat, mouse)) TFA) is a compound labeled with 13C and 15N, and it is a form of Orexin A (human, rat, mouse). Orexin A, also known as Hypocretin-1, is a 33 amino acid excitatory neuropeptide involved in various central and peripheral processes. It binds to and activates two G protein-coupled receptors: the Orexin-1 receptor (OX1R) and Orexin-2 receptor (OX2R), playing a crucial role in regulating feeding behavior. Orexin A is also an active molecule with potent antinociceptive and anti-hyperalgesic properties.

Orexin A-13C6,15N (human, rat, mouse) (also known as Hypocretin-1-13C6,15N (human, rat, mouse)) TFA is an isotopically labeled version of Orexin A (human, rat, mouse). This 33-amino acid excitatory neuropeptide is involved in various central and peripheral processes. It binds to and activates two G protein-coupled receptors, the Orexin-1 receptor (OX1R) and the Orexin-2 receptor (OX2R), playing a crucial role in regulating feeding behavior. Additionally, Orexin A (human, rat, mouse) is an effective agent against nociception and hyperalgesia.