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JNJ-42153605
Catalog No. T3451Cas No. 1254977-87-1
JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
JNJ-42153605
Catalog No. T3451Cas No. 1254977-87-1
JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $29 | In Stock | |
| 2 mg | $44 | In Stock | |
| 5 mg | $74 | In Stock | |
| 10 mg | $107 | In Stock | |
| 25 mg | $190 | In Stock | |
| 50 mg | $293 | In Stock | |
| 100 mg | $417 | In Stock | |
| 200 mg | $585 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $76 | In Stock |
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Purity:98.57%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO: Slightly soluble  |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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