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JNJ-42153605
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Catalog No. T3451Cas No. 1254977-87-1
JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
JNJ-42153605
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Purity: 98.57%
Catalog No. T3451Cas No. 1254977-87-1
JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $31 | In Stock | In Stock | |
| 5 mg | $52 | In Stock | In Stock | |
| 10 mg | $75 | In Stock | In Stock | |
| 25 mg | $133 | In Stock | In Stock | |
| 50 mg | $205 | In Stock | In Stock | |
| 100 mg | $292 | In Stock | In Stock | |
| 200 mg | $410 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | 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:98.57%
Color:White
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Product Introduction
Bioactivity
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 |
| Smiles | FC(F)(F)c1c(ccn2c(CC3CC3)nnc12)N1CCC(CC1)c1ccccc1 |
| Relative Density. | 1.38 g/cm3 (Predicted) |
| 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: Slightly soluble  |
Calculator
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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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
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