JNJ-42847922 manufacturers
- Seltorexant
-
-
2026-08-13
- CAS:1293281-49-8
- Min. Order: 1g
- Purity: 98%
- Supply Ability: 100 g
- Seltorexant
-
- $31.00
-
2026-06-02
- CAS:1293281-49-8
- Purity: 99.90%
- Supply Ability: 10g
- Seltorexant
-
- $31.00
-
2026-06-02
- CAS:1293281-49-8
- Purity: 99.90%
- Supply Ability: 10g
|
| | JNJ-42847922 Basic information |
| Product Name: | JNJ-42847922 | | Synonyms: | [2-(4,6-DIMETHYLPYRIMIDIN-2-YL)-1,3,3A,4,6,6A-HEXAHYDROPYRROLO[3,4-C]PYRROL-5-YL]-[2-FLUORO-6-(TRIAZOL-2-YL)PHENYL]METHANONE;JNJ-42847922;JNJ-42847922,Cid 67116280;[5-(4,6-dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone;Methanone, [5-(4,6-dimethyl-2-pyrimidinyl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl][2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl]-;Hypocretin Receptor,JNJ42847922,HCRT Receptor,Orexin Receptor (OX Receptor),Seltorexant,movement,barrier,insomnia,somnolence,eye,blood-brain,inhibit,rapid,selective,sleep,JNJ 42847922,Inhibitor;(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;Seltorexant, 10 mM in DMSO | | CAS: | 1293281-49-8 | | MF: | C21H22FN7O | | MW: | 407.44 | | EINECS: | | | Product Categories: | API | | Mol File: | 1293281-49-8.mol |  |
| | JNJ-42847922 Chemical Properties |
| Boiling point | 667.7±65.0 °C(Predicted) | | density | 1.46±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 250 mg/mL (613.59 mM) | | pka | 6.50±0.50(Predicted) | | form | Solid | | color | White to yellow |
| | JNJ-42847922 Usage And Synthesis |
| Description | Seltorexant, also known as JNJ-42847922 and MIN-202, is a potent OX2R antagonist that has been shown to promote sleep in various species. JNJ-42847922 had an approximate 2-log selectivity ratio versus the human orexin-1 receptor. Ex vivo receptor binding studies demonstrated that JNJ-42847922 quickly occupied OX2R binding sites in the rat brain after oral administration and rapidly cleared from the brain. Seltorexant shows antidepressant and sleep-promoting effects in patients with major depressive disorder. JNJ-42847922 induces somnolence in healthy subjects without residual central effects. | | Uses | 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[1]. | | in vivo | Seltorexant (JNJ-42847922) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats[1]. 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]. | Animal Model: | Male Sprague-Dawley rats (350-450 g)[1] | | Dosage: | 30 mg/kg | | Administration: | p.o.; per day for 7 days | | 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. |
| | IC 50 | human OX2R: 8.0 (pKi); rat OX2R: 8.1 (pKi) | | 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. DOI:10.1124/jpet.115.225466 |
| | JNJ-42847922 Preparation Products And Raw materials |
| Raw materials | Benzoyl chloride, 2-fluoro-6-(2H-1,2,3-triazol-2-yl)--->Pyrrolo[3,4-c]pyrrole, 2-(4,6-dimethyl-2-pyrimidinyl)octahydro--->5-Benzyl-2-Boc-hexahydro-pyrrolo[3,4-C]pyrrole-->2-Fluoro-6-(2H-1,2,3-triazol-2-yl)benzoic acid-->3-Benzyl-3,7-diazabicyclo[3.3.0]octane-->2-BOC-HEXAHYDRO-PYRROLO[3,4-C]PYRROLE-->2-FLUORO-6-IODOBENZOIC ACID |
|