1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. Seltorexant hydrochloride

Seltorexant hydrochloride (Synonyms: JNJ-42847922 hydrochloride)

Cat. No.: HY-109012A
Handling Instructions

Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.

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

Seltorexant hydrochloride Chemical Structure

Seltorexant hydrochloride Chemical Structure

CAS No. : 1293284-49-7

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Description

Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain[1].

IC50 & Target

human OX2R

8.0 (pKi)

rat OX2R

8.1 (pKi)

In Vivo

Seltorexant hydrochloride (JNJ-42847922 hydrochloride) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats[1].
The sleep-promoting effects of Seltorexant hydrochloride (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.
Clinical Trial
Molecular Weight

443.91

Formula

C₂₁H₂₃ClFN₇O

CAS No.

1293284-49-7

SMILES

O=C(N1CC(CN(C2=NC(C)=CC(C)=N2)C3)C3C1)C4=C(N5N=CC=N5)C=CC=C4F.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

SeltorexantJNJ-42847922JNJ42847922JNJ 42847922Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT Receptorselectiveinsomniasleeprapideyemovementblood-brainbarriersomnolenceInhibitorinhibitorinhibit

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Product name:
Seltorexant hydrochloride
Cat. No.:
HY-109012A
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