1628843-99-1
1628843-99-1 structure
- Name: JNJ-54717793
- Chemical Name: JNJ-54717793
- CAS Number: 1628843-99-1
- Molecular Formula: C22H18F4N6O
- Molecular Weight: 458.41
- Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
- Create Date: 2021-09-06 10:57:04
- Modify Date: 2024-01-14 16:53:21
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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].
| Name | JNJ-54717793 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
human OX1R:16 nM (Ki) human OX2R:700 nM (Ki) OX1 Receptor:85 ng/mL (EC50) |
| In Vivo | 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]. Animal Model: OX2R KO mice[2] Dosage: 30 mg/kg Administration: P.o. Result: Significantly reduced the latency for rapid eye movement (REM) sleep and prolonged the time spent in REM sleep. Animal Model: Rat[2] Dosage: 3~30 mg/kg Administration: P.o. Result: Attenuated bradycardia responses. Animal Model: Mouse[1] Dosage: 5.0 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Clearance was found to be low. |
| References |
| Molecular Formula | C22H18F4N6O |
|---|---|
| Molecular Weight | 458.41 |