Seltorexant
Based on 3 publication(s) in Google Scholar
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 1293281-49-8
- Formel: C21H22FN7O
- Molecular Weight:407.44
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Seltorexant
MoreAlle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
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human OX2R 8.0 (pKi) |
rat OX2R 8.1 (pKi) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 34, JNJ-42847922
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Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cells
Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cells
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[PMID: 26087021] |
The sleep-promoting effects of Seltorexant (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (350-450 g)[1]
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Dosage:30 mg/kg
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Administration:p.o.; per day for 7 days
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Result:The reduced sleep onset (non–rapid eye movement (NREM) latency) and the increased NREM sleep duration were maintained upon 7-day repeated dosing with JNJ-42847922. The prolongation of NREM sleep time was due to a significant increase in NREM bout duration throughout the treatment period assessed on D1 and D7. Rapid eye movement (REM) sleep was only marginally affected on D4 of treatment, resulting in a small but significant reduction in REM sleep latency and an increase in REM sleep duration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1293281-49-8
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Appearance Solid
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Molecular Weight 407.44
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Formel C21H22FN7O
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Color White to yellow
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SMILES
O=C(N1CC(CN(C2=NC(C)=CC(C)=N2)C3)C3C1)C4=C(N5N=CC=N5)C=CC=C4F
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Synonyms
JNJ-42847922
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Bioorg Chem
Synthesis and characterization of a new Positron emission tomography probe for orexin 2 receptors neuroimaging. [Abstract]2022 Jun;123:105779. PMID: 35397430 -
Int J Neuropsychopharmacol
2025 Aug 1;28(8):pyaf047. PMID: 40613271 -
bioRxiv
Prioritizing Neuroactive Ligands Using Motif-Guided Virtual Discovery and Zebrafish Profiling. [Abstract]2026 Jan 16:2026.01.15.699747. PMID: 41648545
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (61.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4543 mL | 12.2717 mL | 24.5435 mL | 61.3587 mL |
| 5 mM | 0.4909 mL | 2.4543 mL | 4.9087 mL | 12.2717 mL | |
| 10 mM | 0.2454 mL | 1.2272 mL | 2.4543 mL | 6.1359 mL | |
| 15 mM | 0.1636 mL | 0.8181 mL | 1.6362 mL | 4.0906 mL | |
| 20 mM | 0.1227 mL | 0.6136 mL | 1.2272 mL | 3.0679 mL | |
| 25 mM | 0.0982 mL | 0.4909 mL | 0.9817 mL | 2.4543 mL | |
| 30 mM | 0.0818 mL | 0.4091 mL | 0.8181 mL | 2.0453 mL | |
| 40 mM | 0.0614 mL | 0.3068 mL | 0.6136 mL | 1.5340 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4909 mL | 1.2272 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4091 mL | 1.0226 mL |
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