JNJ-42153605
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
100mg | $900 | Check With Us |
250mg | $1600 | Check With Us |
500mg | $2400 | Check With Us |
Cat #: V2844 CAS #: 1254977-87-1 Purity ≥ 98%
Description: JNJ-42153605 is a potent, selective and allosteric modulator of the mGlu2 (metabotropic glutamate 2) receptor with with an EC50 of 17 nM.
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Molecular Weight (MW) | 400.44 |
---|---|
Molecular Formula | C₂₂H₂₃F₃N₄ |
CAS No. | 1254977-87-1 |
Storage | -20℃ for 3 years in powder formrr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 10 mMrr |
Water: <1 mg/mLrr | |
Ethanol: | |
SMILES Code | FC(C1=C(N2CCC(C3=CC=CC=C3)CC2)C=CN4C1=NN=C4CC5CC5)(F)F |
Synonyms | JNJ-42153605; JNJ 42153605; JNJ42153605 |
Protocol | 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 |
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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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.4973 mL | 12.4863 mL | 24.9725 mL | 49.9451 mL |
5mM | 0.4995 mL | 2.4973 mL | 4.9945 mL | 9.9890 mL |
10mM | 0.2497 mL | 1.2486 mL | 2.4973 mL | 4.9945 mL |
20mM | 0.1249 mL | 0.6243 mL | 1.2486 mL | 2.4973 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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