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

Seltorexant (Synonyms: JNJ-42847922)

Cat. No.: HY-109012 Purity: 99.51%
Handling Instructions

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.

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

Seltorexant Chemical Structure

Seltorexant Chemical Structure

CAS No. : 1293281-49-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 165 In-stock
Estimated Time of Arrival: December 31
50 mg USD 455 In-stock
Estimated Time of Arrival: December 31
100 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target[1]

human OX2R

8.0 (pKi)

rat OX2R

8.1 (pKi)

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 JNJ-42847922 (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

407.44

Formula

C₂₁H₂₂FN₇O

CAS No.

1293281-49-8

SMILES

O=C(N1CC(CN(C2=NC(C)=CC(C)=N2)C3)C3C1)C4=C(N5N=CC=N5)C=CC=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (613.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4543 mL 12.2717 mL 24.5435 mL
5 mM 0.4909 mL 2.4543 mL 4.9087 mL
10 mM 0.2454 mL 1.2272 mL 2.4543 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (15.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (15.34 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (15.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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Seltorexant
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HY-109012
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