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Seltorexant (also known as MIN-202 and JNJ-42847922), is a novel, potent and selective orexin-2 receptor antagonist. It can promote sleep in various species and is under development for the treatment of insomnia and major depressive disorder.
| ln Vivo |
At doses up to Sprague-Dawley weight, seltorexant (JNJ-42847922) (3–30 mg/kg; flour) initiates and prolongs sleep [1]. 30 mg/kg seltorexant (wall; daily for 7 days)
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (350-450 g) [1]
Doses: 30 mg/kg Route of Administration: po; in the antenna The sleep-prolonging effect remains stable after 7 days of repeated spraying [1]. Once-daily for 7 days Experimental Results: Reductions in sleep onset time (non-rapid eye movement (NREM) latency) and increases in NREM sleep duration were maintained after repeated dosing of JNJ-42847922 for 7 days. The prolongation of NREM sleep duration was due to a significant increase in NREM episode duration throughout the treatment period assessed on D1 and D7. Rapid eye movement (REM) sleep was only slightly affected on day 4 of treatment, resulting in a small but significant decrease in REM sleep latency and an increase in REM sleep duration. |
| References |
[1]. Bonaventure P, et al. Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia. J Pharmacol Exp Ther. 2015 Sep;354(3):471-82.
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| Molecular Formula |
C21H22FN7O
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| Molecular Weight |
407.4534
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| Exact Mass |
407.187
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| CAS # |
1293281-49-8
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| Related CAS # |
Seltorexant hydrochloride;1293284-49-7
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| SMILES |
FC1C=CC=C(C=1C(N1CC2CN(C3N=C(C)C=C(C)N=3)CC2C1)=O)N1N=CC=N1
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| Chemical Name |
((3aR,6aS)-5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanone
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| Synonyms |
MIN-202 JNJ42847922MIN 202 JNJ-42847922MIN202 JNJ 42847922 Seltorexant
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~61.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4543 mL | 12.2714 mL | 24.5429 mL | |
| 5 mM | 0.4909 mL | 2.4543 mL | 4.9086 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4543 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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