1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. JNJ-54717793

JNJ-54717793 

Cat. No.: HY-134188
Handling Instructions

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.

For research use only. We do not sell to patients.

JNJ-54717793 Chemical Structure

JNJ-54717793 Chemical Structure

CAS No. : 1628843-99-1

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

458.41

Formula

C₂₂H₁₈F₄N₆O

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
JNJ-54717793
Cat. No.:
HY-134188
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