Orexin Receptor (OX Receptor) Agonist

Suntinorexton is an OX2R agonist. Suntinorexton is used to study respiratory function during sleep.

[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC₅₀=0.13 nM) over OX1 (52 nM).

Efizonerimod alfa (MEDI-6383) is a recombinant human OX40L IgG4P Fc fusion protein that assembles into a hexameric structure and exerts potent agonist activity upon binding to OX40. The activity of Efizonerimod alfa is enhanced by Fcγ receptor-mediated aggregation. Efizonerimod alfa binds to OX40 on the surface of activated T cells, induces NF-κB promoter activity in OX40-expressing T cells, and triggers the production of Th1-type cytokines, T cell proliferation, and resistance to regulatory T cell (Treg)-mediated suppression. Efizonerimod alfa enhances the cytolytic activity of tumor-reactive T cells and slows tumor growth in immunodeficient mice. Efizonerimod alfa induces the proliferation of CD4, CD8, and B cells in the peripheral blood of healthy non-human primates. Efizonerimod alfa can be used in the research of advanced solid malignancies and melanoma.

Firazorexton hydrate (TAK-994) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton hydrate can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice.

Alixorexton (ALKS 2680) enantiomer is the enantiomer of Alixorexton (HY-172412). Alixorexton is a selective, orally active and brain-penetrant agonist for orexin-2 receptor and can be used for hypersomnias research.

Orexin 2 Receptor Agonist 2 is a selective orexin 2 receptor agonist, extracted from patent WO2017135306A1, example 16.

(R,R)-Suntinorexton is a isomeride of Suntinorexton (HY-137452). Suntinorexton is a orexin type 2 receptor agonist.

(S)-YNT-3708, the S-enantiomer of YNT-3708, with low activity for OX1R and OX2R (EC₅₀ = 3595 nM and 1661 nm, respectively).

OX-201 is an orally active, blood-brain barrier-permeable OX2R agonist with an EC₅₀ of 8.0 nM. OX-201 activates OX2R to induce wakefulness and neuronal activation. OX-201 promotes the release of neuron activity-dependent tau protein from neurons into the interstitial fluid of hippocampal tissues. OX-201 is applicable to research related to Alzheimer's disease and tauopathies.

[Ala11,D-Leu15]-Orexin B(human) TFA is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) TFA shows a 400-fold selectivity for the OX2 (EC₅₀=0.13 nM) over OX1 (52 nM).

Orexin 2 Receptor Agonist 3 (Compound 57) is an orally active and brain-penetrant orexin receptor type-2 (OX₂) agonist (EC₅₀: 2.5 nM). Orexin 2 Receptor Agonist 3 increases wakefulness in the orexin/ataxin-3 NT1 mouse model and healthy beagle dogs. Orexin 2 Receptor Agonist 3 can be used in the study of narcolepsy.

Ledasorexton is an orally active OX2R agonist (EC₅₀: 0.99 nM). Ledasorexton has awakening effect in mice. Ledasorexton can be used for research of neurological disease.

SHR-1806 is a OX40 agonist and a NF-κB activator, with antitumor activity. SHR-1806 mediates ADCC and CDC effects, enhances the function and expansion of effector T cells, suppresses regulatory T cells, and increases γ-interferon secretion. SHR-1806 exhibits typical pharmacokinetic characteristics and favorable safety profiles. SHR-1806 can be used in studies related to solid tumors and colon cancer.

Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes apoptosis.

YNT-3708 is an orexin receptor (OXR) agonist, with EC₅₀ values of 14.6 nM and 277 nm for OX1R and OX2R, respectively.

OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC₅₀=8.29 nM) over OX2 (187 nM).

Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX₂R.

Orexin B, human is an endogenous agonist at Orexin receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

OX2R agonist 3 (compound 63c) is an agonist for orexin receptor type 2 (OX2R) with EC₅₀ of 339 nM. OX2R agonist 3 is able to cross the blood-brain barrier and exhibits no cytotoxicity in cells

OX2R agonist 1 is an OX2R antagonist with an EC₅₀ of less than 100 nM. OX2R agonist 1 can be used in research related to excessive daytime sleepiness or narcolepsy.