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JNJ-42153605 GluR modulator

Cat.No.S6618

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

Chemical Structure

Molecular Weight: 400.44

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Quality Control

Batch: S661801 Ethanol]10 mg/mL]false]DMSO]4 mg/mL]false]Water]Insoluble]false Purity: 99.46%
99.46

Solubility

In vitro
Batch:

Ethanol : 10 mg/mL

DMSO : 4 mg/mL (9.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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

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Chemical Information, Storage & Stability

Molecular Weight 400.44 Formula

C22H23F3N4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1254977-87-1 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CC1CC2=NN=C3N2C=CC(=C3C(F)(F)F)N4CCC(CC4)C5=CC=CC=C5

Mechanism of Action

Targets/IC50/Ki
mGlu2 receptor
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 this compound 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).
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. This compound 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).
References

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