JNJ-42153605

For research use only.

Catalog No.S6618

JNJ-42153605 Chemical Structure

Molecular Weight(MW): 400.44

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

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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.
Targets
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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 400.44
Formula

C22H23F3N4

CAS No. 1254977-87-1
Storage powder
in solvent
Synonyms N/A
Smiles FC(F)(F)C1=C(C=C[N]2C(=NN=C12)CC3CC3)N4CCC(CC4)C5=CC=CC=C5

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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.

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GluR Signaling Pathway Map

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