Seltorexant (Synonyms: JNJ-42847922) |
Katalog-Nr.GC37623
One-Click Copy Product Info
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Seltorexant (JNJ-42847922) ist ein oral aktiver, hochaffiner und selektiver Orexin-2-Rezeptor (OX2R)-Antagonist (pKi-Werte von 8,0 und 8,1 fÜr Human- und Ratten-OX2R).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1293281-49-8
Sample solution is provided at 25 µL, 10mM.
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Seltorexant is an orally active, high-affinity, and selective OX2R antagonist with a pKi value of 8.1 for rat OX2R [1]. Seltorexant can cross the blood-brain barrier (BBB) and bind to OX2R, which selectively block OX2R to initiate and prolong sleep [2]. Seltorexant has been widely used to shorten the latency of rapid eye movement (REM) sleep in rats and to prolong the duration of REM sleep [3].
In vivo, Seltorexant treatment via a single subcutaneous injection at a dose of 10mg/kg for 30 minutes acutely reduced responding for sucrose under both sleep deprivation and sleep recovery conditions[4]. Intraperitoneal injection of a 10mg/kg/day dose of Seltorexant for 5 days can increase the anxiety-like behavior in male mice[5].
References:
[1] Bonaventure P, Shelton J, Yun S, et al. Characterization of JNJ-42847922, a selective orexin-2 receptor antagonist, as a clinical candidate for the treatment of insomnia[J]. The Journal of Pharmacology and Experimental Therapeutics, 2015, 354(3): 471-482.
[2] Ziemichód W, Kurowska A, Grabowska K, et al. Characteristics of seltorexant—innovative agent targeting orexin system for the treatment of depression and anxiety[J]. Molecules, 2023, 28(8): 3575.
[3] Mesens S, Krystal A D, Melkote R, et al. Efficacy and safety of seltorexant in insomnia disorder: a randomized clinical trial[J]. JAMA psychiatry, 2025, 82(10): 967-976.
[4] Forbes C, Zeak J, Shelton M, et al. Acute Sleep Deprivation in Adolescence Produces Transcriptional Changes in the Orexin System and Regulates Motivation for Reward[J]. Biological Psychiatry Global Open Science, 2026: 100746.
[5] Chen L, Tian R, Wei S, et al. Activation of orexin receptor 2 plays anxiolytic effect in male mice[J]. Brain Research, 2025, 1859: 149646.
| Animal experiment [1]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats (350-450g) were maintained in a controlled environment at 22±3°C and 60% relative humidity under a 12h light/dark cycle, and were given free access to standard rodent nutrition and water. Rats were chronically implanted with telemetric devices for the recording of sleep parameters. Administer 30mg/kg of Seltorexant orally every day for 7 consecutive days, and then analyze the sleep parameters of the rats. |
Dosage form | 30mg/kg/day for 7 days; p.o. |
Applications | Seltorexant treatment maintained the reduced sleep onset and increased sleep duration in rats. |
References: | |
| Cas No. | 1293281-49-8 | SDF | |
| Überlieferungen | JNJ-42847922 | ||
| Canonical SMILES | O=C(N1CC(CN(C2=NC(C)=CC(C)=N2)C3)C3C1)C4=C(N5N=CC=N5)C=CC=C4F | ||
| Formula | C21H22FN7O | M.Wt | 407.44 |
| Löslichkeit | DMSO: 250 mg/mL (613.59 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4543 mL | 12.2717 mL | 24.5435 mL |
| 5 mM | 490.9 μL | 2.4543 mL | 4.9087 mL |
| 10 mM | 245.4 μL | 1.2272 mL | 2.4543 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)