1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. JNJ-42153605

JNJ-42153605 

Cat. No.: HY-18162 Purity: 99.00%
Handling Instructions

JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.

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

JNJ-42153605 Chemical Structure

JNJ-42153605 Chemical Structure

CAS No. : 1254977-87-1

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
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100 mg USD 1140 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

JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.

IC50 & Target[1]

mGluR2

17 nM (EC50)

In Vitro

JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux[1].

In Vivo

JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog[1].

Molecular Weight

400.44

Formula

C₂₂H₂₃F₃N₄

CAS No.

1254977-87-1

SMILES

FC(C1=C(N2CCC(C3=CC=CC=C3)CC2)C=CN4C1=NN=C4CC5CC5)(F)F

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 : 16.67 mg/mL (41.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4973 mL 12.4863 mL 24.9725 mL
5 mM 0.4995 mL 2.4973 mL 4.9945 mL
10 mM 0.2497 mL 1.2486 mL 2.4973 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: 1.67 mg/mL (4.17 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 1.67 mg/mL (4.17 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.67 mg/mL (4.17 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats: The effects of the tested molecule and vehicle on sleep−wake distribution during the lights-on period are investigated in 16 rats. Two EEG recording sessions are performed: the first recording session starts at 13:30 h and lasts 20 h following oral administration of saline. The second recording session is performed during the same consecutive circadian time and for the same duration following administration of either vehicle (20% CD+2H2T) or JNJ-42153605[1].

Mice: Male NMRI mice are treated with vehicle, or JNJ-42153605, and immediately challenged with either PCP (5.0 mg/kg, sc) or vehicle and individually placed into open-fields for a 30 min period. The distance traveled by animals is measured using video tracking and computerized analysis systems[1].

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

References
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Keywords:

JNJ-42153605JNJ42153605JNJ 42153605mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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Product Name:
JNJ-42153605
Cat. No.:
HY-18162
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