For research use only. Not for therapeutic Use.
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders[1][2].
JNJ-5471779 (30 mg/kg; p.o.; 6 hours) significantly reduces the latency for rapid eye movement (REM) sleep and prolongs the time spent in REM sleep[2].
JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses[2].
JNJ-5471779 (5mg/kg; p.o.) shows low clearance[1].
| Catalog Number | I029836 |
| CAS Number | 1628843-99-1 |
| Synonyms | (3-fluoro-2-pyrimidin-2-ylphenyl)-[(2R)-2-[[5-(trifluoromethyl)pyrazin-2-yl]amino]-7-azabicyclo[2.2.1]heptan-7-yl]methanone |
| Molecular Formula | C22H18F4N6O |
| Purity | ≥95% |
| InChI | InChI=1S/C22H18F4N6O/c23-14-4-1-3-13(19(14)20-27-7-2-8-28-20)21(33)32-12-5-6-16(32)15(9-12)31-18-11-29-17(10-30-18)22(24,25)26/h1-4,7-8,10-12,15-16H,5-6,9H2,(H,30,31)/t12?,15-,16?/m1/s1 |
| InChIKey | NWUAUSABGZEYEW-DSSZZKGTSA-N |
| SMILES | C1CC2C(CC1N2C(=O)C3=C(C(=CC=C3)F)C4=NC=CC=N4)NC5=NC=C(N=C5)C(F)(F)F |
| Reference | [1]. Préville C, et al. Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793. ACS Med Chem Lett. 2020;11(10):2002-2009. Published 2020 Apr 27. [2]. Bonaventure P, et al. Evaluation of JNJ-54717793 a Novel Brain Penetrant Selective Orexin 1 Receptor Antagonist in Two Rat Models of Panic Attack Provocation. Front Pharmacol. 2017;8:357. Published 2017 Jun 9. |
