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JNJ-42153605

Cat. No. M7565
JNJ-42153605 Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 260 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux.

In vivo: JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative of antipsychotic activity. JNJ-42153605 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.

Protocol
Cell Experiment
Cell lines Chinese Hamster Ovary (CHO) cells
Preparation method Final assay mixtures contained 7 (human mGluR2) or 10 (rat mGluR2) μg of membrane protein were pre-incubated with JNJ-42153605 alone (determination of agonist effects) or together with an EC20 concentration (4 μM) of glutamate (determination of PAM effects) for 30 min at 30°C. [35S]GTPγS was added at a concentration of 0.1 nM and Filter-bound radioactivity according to an earlier protocol.
Concentrations 30 mM
Incubation time 30 min
Animal Experiment
Animal models Sprague Dawley rats
Formulation
Dosages 3, 10 and 30 mg/kg
Administration Oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 400.44
Formula C22H23F3N4
CAS Number 1254977-87-1
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

Efficacy of mGlu2 -positive allosteric modulators alone and in combination with levetiracetam in the mouse 6 Hz model of psychomotor seizures.
Metcalf CS, et al. Epilepsia. 2017 Mar;58(3):484-493. PMID: 28166368.

mGlu2 Receptor Agonism, but Not Positive Allosteric Modulation, Elicits Rapid Tolerance towards Their Primary Efficacy on Sleep Measures in Rats.
Ahnaou A, et al. PLoS One. 2015 Dec 11;10(12):e0144017. PMID: 26658273.

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  Catalog
Abmole Inhibitor Catalog 2017




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