ox2

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

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.

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).

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.

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).

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

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.

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.

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.

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

[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).

OX2-2303 is a potent and selective orexin-2 receptor (OX2R) antagonist with excellent binding affinity to OX2R (Ki= 0.1 nM) and over 890-fold selectivity for OX2R over OX1R. OX2-2303 can serve as a positron emission tomography (PET) radioligand for research related to the central nervous system (CNS).

TCS-OX2-29 is a selective orexin-2 receptor antagonist (IC50 = 40 nM), which plays an important role in pain modulation.

IOX2 (IOX 2) is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with the IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20uM).

OX2R-IN-2 (compound 63c) is an agonist of the type 2 orexin receptor (OX2R) with an EC50 value of 339 nM. It can cross the blood-brain barrier and exhibits no cytotoxicity.

OX2R-IN-3 (Compound 53) functions as an orally active agonist for the type 2 orexin receptor (OX2R), exhibiting an EC50 value of less than 100 nM [1].

NOX2-IN-2 diTFA (compound 33) is an effective inhibitor of NOX2, targeting the p47phox-p22phox protein-protein interaction with a Ki of 0.24 μM. This compound effectively suppresses the production of ROS generated by NOX2 in cells.

OX2R-IN-1 is an OX2R antagonist (a potential OX2R binding agent) that exhibits low cytotoxicity (IC50: 484 μM). oX2R-IN-1 has blood-brain barrier permeability and a short drug half-life.

NOX2-IN-2 (compound 33) is a potent inhibitor of NOX2, disrupting the p47phox-p22phox protein-protein interaction with a dissociation constant (Ki) of 0.24 μM, and effectively suppressing reactive oxygen species (ROS) production from NOX2 in cellular contexts [1].