ox2

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

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

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

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

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

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].

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

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].

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.

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

Endogenous agonist at orexin receptors (Ki values are 20 and 38 nM for OX1 and OX2 receptors respectively). Stimulates feeding following central administration and may be involved in the control of sleep-wake cycle and other hypothalamic functions.

Orexin B, human, is an endogenous agonist at Orexin receptors with Ki values of 420 nM for OX1 and 36 nM for OX2, respectively. Orexin B is a hypothalamic neuropeptide that stimulates food intake in rats.

[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).

OXA(17-33) TFA is a potent and selective agonist for the orexin-1 receptor (OX1), with approximately 23-fold higher affinity for OX1 (EC50 = 8.29 nM) compared to the orexin-2 receptor (OX2) (187 nM) [1].

RTIOXA-43 is an OX2R OX1R (orexin receptor) dual agonist that increases wakefulness and attenuates episodic sleep symptoms and is commonly used in studies related to narcolepsy and neural signaling.

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

CVN766 is an orally active orexin 1 receptor antagonist with blood-brain permeability, demonstrating IC50 values of 8 nM for OX1R and >10 μM for OX2R. CVN766 can be used to study schizophrenia [1].