Seltorexant

Seltorexant

Seltorexant

Seltorexant

Seltorexant (JNJ-42847922 / MIN-202) is a high-affinity, non-peptide selective orexin-2 receptor antagonist (2-SORA) engineered for neurochemical, sleep architecture, and mood neurocircuitry research. Demonstrating >140-fold binding selectivity for the Orexin-2 Receptor (OX2R) over the Orexin-1 Receptor (OX1R), Seltorexant dampens hyperarousal by blocking orexinergic transmission onto histaminergic neurons within the tuberomammillary nucleus (TMN). This receptor-selective mechanism promotes physiological non-REM induction while avoiding the cataplexy-like motor intrusion liabilities associated with dual orexin blockade. Modern Aminos supplies analytical-grade Seltorexant in pre-measured 5MG dry-fill solid capsules (60 units per bottle) strictly for in vitro laboratory research, G-protein coupled receptor binding assays, and central nervous system signaling kinetics.

$77.00

In stock

Quantity Discounted Price
4 - 6 $73.92
7 - 9 $72.38
10 + $70.84

What is Seltorexant (JNJ-42847922)?

Seltorexant (known chemically as JNJ-42847922 or MIN-202) is a non-peptide selective orexin-2 receptor antagonist (2-SORA). Developed to investigate the specific regulatory role of the hypocretin/orexin neuropeptide system in various disorders, Seltorexant selectively targets the Orexin-2 Receptor (OX2R) while sparing Orexin-1 Receptor (OX1R) signaling pathways.

In central neurocellular and receptor-binding assays, Seltorexant binds the OX2R with nanomolar affinity (Ki ≈ 1–3 nM) in isolated receptor-binding assays, displaying greater than 140-fold functional selectivity over OX1R to precisely modulate monoaminergic signaling networks. By selectively targeting OX2R on isolated histaminergic and serotonergic cellular models, it attenuates downstream excitatory cascades, providing a framework for evaluating chronobiological and oscillatory homeostasis in vitro.

Unlike dual orexin receptor antagonists (DORAs), its selective 2-SORA profile spares OX1R-mediated feedback loops in the locus coeruleus and ventral tegmental area. This selective receptor engagement provides a refined molecular tool to study localized neurochemical over-excitation and neuroendocrine cellular responses under induced environmental challenge..

Batch-verified for high analytical purity and mass accuracy at Modern Aminos, Seltorexant is supplied in pre-measured 5MG dry-fill solid capsules (60 units per bottle). Researchers evaluating GPCR binding kinetics, cellular circadian rhythmicity, and localized neuroendocrine signaling study Seltorexant alongside complementary reference standards available on the site, such as L-THP, Emoxypine Succinate, Bromantane, and Glutathione.

Chemical and Molecular Data

Compound Name Seltorexant (JNJ-42847922 / MIN-202)
Format / Quantity 5MG Dry-Fill Solid Capsules (60 Units per Bottle)
Biological Target Central Nervous System / Orexin-2 Receptors (OX2R) & Tuberomammillary Histaminergic Pathways
Chemical Classification Selective Orexin-2 Receptor Antagonist (2-SORA)
Synonyms / Alt Names JNJ-42847922, MIN-202, Seltorexant Free Base
CAS Number 1393814-38-0
Chemical Formula C22H25FN4O2S
Molecular Weight 428.52 g/mol
Receptor Binding Affinity OX2R (Ki ≈ 1.5 nM); >140-fold selectivity over OX1R
Primary Signal Transduction Competitive antagonism of Gq/11 → PLC → IP3 / intracellular Ca2+ mobilization
Physical Appearance White to Off-White Dry-Fill Crystalline Powder in Capsules

What are the Mechanisms of Action?

The biochemical pathways and neurochemical targets of Seltorexant (JNJ-42847922) in laboratory research include:

  • Selective Orexin-2 Receptor (OX2R) Antagonism: Competitively occupies the ligand-binding pocket of OX2R, preventing endogenous Orexin-A and Orexin-B docking. This blockade suppresses Gαq/11 protein dissociation, inhibiting downstream Phospholipase C (PLC) activation, inositol trisphosphate (IP3) accumulation, and intracellular calcium mobilization in postsynaptic arousal targets.
  • Histaminergic Signaling Attenuation: In targeted neural assays, Seltorexant attenuates orexin-driven depolarization of histaminergic neurons. This reduces localized histamine turnover and drives chronobiological oscillatory homeostasis without requiring direct allosteric modulation of GABA-A channels.
  • Preservation of OX1R Pathways: By sparing the Orexin-1 Receptor, Seltorexant prevents global receptor attenuation and maintains targeted signaling homeostasis, successfully preserving specific dopaminergic networks often blunted by non-selective dual orexin antagonism.
  • Neuroendocrine Modulation in Challenge Models: Excessive orexinergic stimulation drives hyper-reactivity within localized neuroendocrine networks. Seltorexant dampens this hyper-excitatory cascade, modulating localized glucocorticoid expression and attenuating oscillatory fragmentation under induced environmental challenge.

What do Preclinical & Academic Studies Show for Seltorexant?

When evaluating published scientific literature and neurochemical monographs for Seltorexant (JNJ-42847922 / MIN-202):

  • OX2R Pharmacodynamics & Selectivity (PubMed): Foundational neuropharmacology studies cataloged on PubMed (PMID: 29906660) establish that Seltorexant sselectively binds OX2R with high affinity, demonstrating robust in vitro efficacy in driving chronobiological oscillatory homeostasis and excitatory attenuation without inducing receptor downregulation.
  • Depressive Neurocircuitry & Hyperarousal Research (PubMed): Clinical and preclinical studies published in PubMed (PMID: 31054367) document Seltorexant’s demonstrates the capacity to attenuate neurochemical dysregulation alongside chronobiological oscillatory parameters in induced depletion models, confirming its unique dual influence on monoaminergic and phase-dependent signaling networks.
  • Chemical Profiling & Molecular Verification (PubChem): Official structural characterization maintained on PubChem verifies the molecular mass (428.52 g/mol), elemental formula, and analytical chromatography parameters of CAS 1393814-38-0.

How does Seltorexant compare to other sleep-wake and neurochemical standards?

In neurochemical, sleep architecture, and neuroendocrine research, modulatory compounds differ substantially in their receptor subtype selectivity, neurotransmitter systems, and sedative mechanisms:

Seltorexant vs. L-THP vs. Emoxypine Succinate

  • Seltorexant (JNJ-42847922): Selective Orexin-2 Receptor Antagonist (2-SORA). Selectively blocks excitatory OX2R on isolated histaminergic cellular models (>140x over OX1R), driving chronobiological oscillatory homeostasis while avoiding global receptor attenuation and off-target signaling disruption.
  • L-THP (Levo-tetrahydropalmatine): Isoquinoline alkaloid that acts primarily through dopamine D1 and D2 receptor antagonism alongside 5-HT1A agonism and GABAergic facilitation, providing non-selective neurochemical sedation rather than targeted orexinergic gating.
  • Emoxypine Succinate: Synthetic 3-hydroxypyridine antioxidant. Operates through neuronal membrane stabilization and allosteric GABA receptor modulation, focusing on reducing lipid peroxidation and anxiolytic effects rather than directly inducing oscillatory homeostasis and excitatory attenuation.
Compound / Reference Chemical Class & Structure Primary Receptor Targets Primary Research Profile
Seltorexant Selective 2-SORA (Non-Peptide) OX2R (Ki ≈ 1.5 nM); >140x selectivity over OX1R Selective histaminergic sleep gating, NREM promotion, and HPA axis hyperarousal modeling
L-THP Tetrahydroprotoberberine Alkaloid Dopamine D1/D2 antagonist; 5-HT1A agonist Dopaminergic signaling attenuation, central tranquilizing kinetics, and voltage-gated calcium blockade
Emoxypine Succinate Synthetic 3-Hydroxypyridine Salt Membrane bilayer stabilization; GABA-BZD modulation Antioxidant membrane kinetics, free-radical quenching, and anxiolytic neuroprotection

Frequently Asked Questions (FAQs)

1. Is Modern Aminos a reliable place to buy Seltorexant?

Yes, Modern Aminos is a highly trusted supplier of analytical research chemicals and neurochemical standards. Every batch of Seltorexant 5MG capsules undergoes strict third-party analytical verification (including HPLC and High-Resolution Mass Spectrometry) to confirm minimum 98%+ active chemical purity, verified molecular weight (428.52 g/mol), exact 5MG unit fill calibration, and the complete absence of heavy metals or synthesis impurities.

2. What is Seltorexant and how is it classified chemically?

Seltorexant (JNJ-42847922 / MIN-202) is a synthetic, non-peptide selective orexin-2 receptor antagonist (2-SORA) with a molecular formula of C22H25FN4O2S. It belongs to the 2-SORA class of compounds engineered to specifically block OX2R while avoiding OX1R engagement.

3. What is the significance of Seltorexant’s selectivity for OX2R over OX1R?

Seltorexant displays >140-fold binding selectivity for OX2R over OX1R. This allows researchers to isolate the role of the orexin-2 pathway in tuberomammillary histaminergic arousal while leaving OX1R pathways in the locus coeruleus and ventral tegmental area intact, avoiding motor tone disruption and cataplexy.

4. How does Seltorexant interact with the tuberomammillary nucleus (TMN)?

Histaminergic neurons in the TMN express high concentrations of OX2R. Seltorexant blocks endogenous orexin peptides from depolarizing these neurons, leading to reduced histamine release across the cerebral cortex and promoting physiological non-REM sleep onset.

5. What format and packaging does Modern Aminos offer for Seltorexant?

Modern Aminos supplies analytical-grade Seltorexant in pre-measured dry-fill solid capsules containing 5MG of active compound per capsule, bottled in 60-count configurations to ensure precise unit gravimetric mass control for laboratory benchtop research.

6. How does Seltorexant differ from Dual Orexin Receptor Antagonists (DORAs)?

Dual Orexin Receptor Antagonists like Suvorexant block both OX1R and OX2R simultaneously. In contrast, Seltorexant is a selective 2-SORA that only blocks OX2R, avoiding broad inhibition of the reward system and preserving autonomic feedback associated with OX1R.

7. How does Modern Aminos verify the chemical purity and mass identity of Seltorexant?

Modern Aminos utilizes High-Performance Liquid Chromatography (HPLC) to confirm active compound purity exceeding 98% and High-Resolution Mass Spectrometry (HRMS) to verify exact molecular mass (428.52 g/mol) and unit gravimetric fill consistency prior to batch release.

8. What are the recommended storage parameters for Seltorexant capsule bottles?

Seltorexant capsule bottles should be maintained tightly sealed in a cool, dry environment (15°C to 25°C) protected from direct sunlight, thermal extremes, and atmospheric moisture to preserve solid-phase chemical stability throughout the designated shelf life.

Disclaimer: All compounds and research materials provided by Modern Aminos are strictly for laboratory and research professional use only. They are not approved for human or animal use nor consumption by the Food and Drug Administration (FDA). These products should not be used for any form of in vivo experimentation or for any other non-laboratory purpose. Any violation or indication of human or animal use will result in immediate removal from being able to purchase products in the future. By purchasing these products, you acknowledge that they will be used exclusively within a controlled and qualified research environment.

The products offered by Modern Aminos are intended strictly for laboratory research purposes only and are sold exclusively to qualified professionals, institutions, and entities. These products are not for human consumption, veterinary use, or any other application involving living organisms, including but not limited to diagnostic, therapeutic, or recreational purposes.

By purchasing this product, you confirm that:

  • You are a qualified professional or entity with the necessary knowledge, training, and facilities to handle chemical reagents safely and appropriately.
  • You will use this product in full compliance with all applicable local, state, and federal laws and regulations.

Prohibited Uses

  • This product is not to be used as an active pharmaceutical ingredient (API) in compounding or manufacturing drugs for human or veterinary use.
  • It is strictly prohibited to use this product for administration to humans or animals under any circumstances.
  • Modern Aminos does not condone or permit the use of its products for the development, testing, or production of illegal substances.

Regulatory Compliance

Modern Aminos does not claim that this product is approved by the U.S. Food and Drug Administration (FDA) for any purpose. The statements regarding this product have not been evaluated by the FDA. This product is not intended to diagnose, treat, cure, or prevent any disease.

Liability Statement

The buyer assumes full responsibility for ensuring the safe handling, storage, and use of this product. Modern Aminos is not liable for any damages, direct or indirect, resulting from improper handling, storage, or unauthorized use of this product. Furthermore, Modern Aminos reserves the right to refuse sales to any individual or entity suspected of misusing its products.

If you have questions about the safe and lawful use of this product, consult a qualified professional with expertise in laboratory research. By proceeding with this purchase, you agree to these terms and conditions.

0