[CAS NO. 1254977-87-1] JNJ-42153605
PRODUCTS SPECIFICATIONS [1254977-87-1]
DESCRIPTION [1254977-87-1]
Overview
| MDL | MFCD22199231 |
|---|---|
| Molecular Weight | 400.44 |
| Molecular Formula | C22H23F3N4 |
| SMILES | FC(C1=C(N2CCC(C3=CC=CC=C3)CC2)C=CN4C1=NN=C4CC5CC5)(F)F |
Summary
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 ( mGlu2 ) receptor with an EC 50 of 17 nM.
IC50 & Target
|
mGluR2 17 nM (EC 50 ) |
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 ED 50 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 16.67 mg/mL ( 41.63 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4973 mL | 12.4863 mL | 24.9725 mL |
| 5 mM | 0.4995 mL | 2.4973 mL | 4.9945 mL |
| 10 mM | 0.2497 mL | 1.2486 mL | 2.4973 mL |