Seltorexant

Seltorexant (JNJ-42847922) Research Standard

Seltorexant (JNJ-42847922, MIN-202) is a potent, orally active, and highly selective Orexin-2 Receptor (OX2R) antagonist. By selectively modulating the orexin signaling pathway, which is integral to arousal and the regulation of the sleep–wake cycle, Seltorexant has emerged as a significant reference compound in neurobiological and pharmacological research. In laboratory and analytical settings, it is utilized to probe the kinetics of the Orexin-2 receptor, map receptor-ligand binding interactions, and investigate the physiological implications of OX2R antagonism in experimental models.Technical Specifications

Mechanism of Action & Research Context

Seltorexant is engineered for high-affinity binding to the Orexin-2 receptor. Its structural features—including the specific fluorine atom positioning and the triazole ring system—are critical for its pharmacological profile.

• OX2R Selectivity: The compound exhibits high selectivity for the Orexin-2 receptor over the Orexin-1 receptor (OX1R). Researchers use this selectivity to isolate the effects of OX2R antagonism in cell-based assays and radioligand competition studies.

• Binding Pocket Interaction: The molecule’s three-dimensional shape enables a precise fit within the OX2R binding pocket. This makes it an ideal probe for studying receptor-ligand kinetics and displacement dynamics using labeled tracers.

• Signaling Modulation: By acting as an antagonist, Seltorexant inhibits the downstream signaling pathways associated with orexin-induced arousal, providing a mechanism to study the reduction of wake-promoting neurochemical activity in controlled in vitro models.

Research Applications

Seltorexant is a specialized reagent essential for modern neuropharmacology and receptor research.

Primary fields of in vitro and analytical laboratory investigation include:

• Binding Affinity Assays: Measuring $K_i$ values and binding kinetics to establish potency and selectivity profiles against OX2R versus OX1R.

• Competition Binding Studies: Utilizing radioligand displacement assays to map the binding footprint within the Orexin-2 receptor.

• Protein Binding Analysis: Evaluating the free fraction of the compound in plasma solutions to support pharmacokinetic modeling.

• Receptor Mapping: Employing the compound as a structural probe to examine how specific ligand modifications influence receptor affinity.

Storage & Handling Guidelines

To maintain the chemical stability and experimental reliability of the compound:

• Storage Environment: Store in a cool, dry place. Keep containers tightly closed when not in active use.

• Environmental Control: Protect strictly from light; store in dark or opaque vials to prevent photodegradation.

• Moisture Management: The compound should be kept away from humidity to ensure the integrity of the powder or solution.

• Aseptic Technique: Use sterile, non-reactive laboratory tools to handle samples. Maintain a clean, dedicated workspace to prevent cross-contamination, particularly when preparing sensitive assay solutions.

Research Use Disclaimer

Research Use Only Disclaimer: This product is developed and distributed strictly as a Research Use Only (RUO) laboratory reference chemical intended exclusively for non-clinical analytical and scientific investigation. It is not an FDA-approved drug, medical treatment, dietary supplement, or food ingredient, and is strictly prohibited for human or animal consumption. Kimera Chems supplies this high-purity research material solely to qualified institutions and professional investigators for authorized laboratory research.