Catalog No.S6618

For research use only.

JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.

JNJ-42153605 Chemical Structure

CAS No. 1254977-87-1

Purity & Quality Control

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Biological Activity

Description JNJ-42153605 is a potent and selective mGlu2 receptor positive allosteric modulator with an EC50 of 17 nM.
mGlu2 receptor [1]
17 nM(EC50)
In vitro

JNJ-42153605 is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM (>50-fold vs mGluR2) and also shows no or negligible affinity or activity at any of the targets in the CEREP panel of receptors (>100-fold selectivity for mGlu2 receptor)[1].

In vivo

In mice, JNJ-42153605 dose-dependently and significantly attenuates the increase in locomotor activity induced by phencyclidine (PCP, 5 mg/kg sc) with an ED50 of 5.4 mg/kg sc. 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. Volume of distribution is slightly higher than total body water, indicating distribution outside the plasma. Bioavailability is low to moderate across the species (35% in rat and 18−33% in dog)[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Ethanol 10 mg/mL
(24.97 mM)
DMSO 4 mg/mL
(9.98 mM)
Water Insoluble

Chemical Information

Molecular Weight 400.44


CAS No. 1254977-87-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1CC2=NN=C3N2C=CC(=C3C(F)(F)F)N4CCC(CC4)C5=CC=CC=C5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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