ox2

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).

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).

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.

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).

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].

NOX2-IN-1 (compound 10) is an inhibitor of nicotinamide adenine dinucleotide phosphate oxidase isoform 2 (NOX2), disrupting the p47phox-p22phox protein-protein interaction with high binding affinities and potent activity in cellular assays [1].

NOX2-IN-3 (compound 3), functioning as an inhibitor of NOX2 (NADPH Oxidase 2), enhances the sensitivity of tumor cells to MRTX1133 [1].

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].

OX2R agonist 1 is an OX2R activator with an EC50 of less than 100 nM. It is utilized in research related to narcolepsy and cataplexy.

Potent and selective peptide orexin OX1 receptor agonist (EC50 values are 8.29 and 187 nM for OX1 and OX2 receptors respectively). Truncated form of orexin A.

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).

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)

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).

ACT-335827 is an orally available, brain-penetrant, orexin type 1 receptor-selective antagonist, with IC50 values of 6 nM for OXR1 and 417 nM for OXR2. It is suitable for studies related to neurological disorders [1].

OX2 receptor antagonist

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.

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