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JNJ-42153605

Catalog No. T3451 CAS 1254977-87-1

JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).

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JNJ-42153605, CAS 1254977-87-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 58.00
2 mg	In stock	$ 82.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 216.00
25 mg	In stock	$ 392.00
50 mg	In stock	$ 589.00
100 mg	In stock	$ 843.00

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Purity: 99.13%

Purity: 97.25%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
Targets&IC50	mGlu2:17 nM(EC50)
In vitro	JNJ-42153605 has been evaluated for its specificity to the mGlu2 receptor, demonstrating no agonist or antagonist effects on other mGlu receptor subtypes at concentrations up to 30 μM. Additionally, it shows high permeability without evidence of P-glycoprotein efflux.
In vivo	JNJ-42153605 demonstrates significant in vivo efficacy by suppressing REM sleep at a 3 mg/kg oral dose in rats, as observed in the sleep-wake EEG paradigm—a result attributed to mGlu2 mediation. Additionally, it mitigates PCP-induced hyperlocomotion in mice, indicating antipsychotic properties, with an effective dose (ED50) of 5.4 mg/kg subcutaneously. The compound is rapidly absorbed in the gastrointestinal tract, peaking at 0.5 hours post-administration. It exhibits moderate to high clearance rates in both rats and dogs (35 and 29 mL/min/kg, respectively), with relatively short elimination half-lives of 2.7 hours in rats and between 0.8 to 1.1 hours in dogs[1].

Molecular Weight	400.44
Formula	C22H23F3N4
CAS No.	1254977-87-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Slightly soluble

References and Literature

1. Cid JM, et al. Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor. J Med Chem. 2012 Oct 25;55(20):8770-89.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library NO PAINS Compound Library Bioactive Compound Library Bioactive Compounds Library Max Fluorochemical Library Neurotransmitter Receptor Compound Library Glutamine Metabolism Compound Library

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Keywords

JNJ-42153605 1254977-87-1 Neuroscience GluR Inhibitor Metabotropic glutamate receptors JNJ 42153605 inhibit JNJ42153605 mGluR inhibitor

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