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JNJ-40411813

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Catalog No. TQ0094Cas No. 1127498-03-6

Alias ADX-71149

JNJ-40411813 (ADX-71149) (ADX-71149) is a new positive allosteric modulator of the metabotropic glutamate 2 receptor (mGlu2R, EC50: 147 nM).

JNJ-40411813

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Purity: 99.74%

Catalog No. TQ0094Alias ADX-71149Cas No. 1127498-03-6

JNJ-40411813 (ADX-71149) (ADX-71149) is a new positive allosteric modulator of the metabotropic glutamate 2 receptor (mGlu2R, EC50: 147 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$50	In Stock	In Stock
5 mg	$119	In Stock	In Stock
10 mg	$193	In Stock	In Stock
25 mg	$323	In Stock	In Stock
50 mg	$461	In Stock	In Stock
100 mg	$592	-	In Stock
200 mg	$783	-	In Stock
1 mL x 10 mM (in DMSO)	$133	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.74%

Appearance:Solid

Color:White

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Product Introduction

JNJ-40411813 AI Summary

JNJ-40411813 acts as a positive allosteric modulator of the human mGlu2 receptor, with an EC50 of 147.0 nM and Emax of 273.0% for the wild-type receptor. It shows selectivity for the mGlu2 receptor over other receptors, including 5HT receptors, although it does exhibit antagonism at the 5HT2A receptor and inhibits the human ERG channel. It demonstrates moderate to high metabolic stability in liver microsomes, high plasma protein binding across multiple species, and moderate oral bioavailability and apparent permeability in Caco2 cells. The compound has a high log P value of 4.6, indicating significant lipophilicity, and displays bioactivity in rat sleep-wake EEG paradigms, affecting the sleep-wake cycle. It also exhibits weak to moderate antiviral activity, inhibiting SARS-CoV-2 induced cytotoxicity of VERO-6 and Caco-2 cells at a concentration of 10 µM, albeit with low efficacy. Additionally, JNJ-40411813 shows inhibitory activity against human HDAC6, with around 59.91% inhibition in enzymatic assays. Collectively, the therapeutic indices suggest a favorable balance between efficacy and safety in various models, making it a compound of interest for further pharmacological studies..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	JNJ-40411813 (ADX-71149) (ADX-71149) is a new positive allosteric modulator of the metabotropic glutamate 2 receptor (mGlu2R, EC50: 147 nM).
Targets&IC50	mGluR2:147 nM (EC50)
Synonyms	ADX-71149

Chemical Properties

Molecular Weight	344.88
Formula	C₂₀H₂₅ClN₂O
Cas No.	1127498-03-6
Smiles	CCCCn1ccc(N2CCC(CC2)c2ccccc2)c(Cl)c1=O
Relative Density.	1.18 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 24 mg/mL (69.59 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8996 mL	14.4978 mL	28.9956 mL	144.9780 mL
5 mM	0.5799 mL	2.8996 mL	5.7991 mL	28.9956 mL
10 mM	0.2900 mL	1.4498 mL	2.8996 mL	14.4978 mL
20 mM	0.1450 mL	0.7249 mL	1.4498 mL	7.2489 mL
50 mM	0.0580 mL	0.2900 mL	0.5799 mL	2.8996 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc