JNJ-42153605


CAS No. : 1254977-87-1

1254977-87-1
Price and Availability of CAS No. : 1254977-87-1
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5mg $150 In-stock
10mg $220 In-stock
50mg $590 In-stock
100mg $840 In-stock
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Cat. No. : HY-18162
M.Wt: 400.44
Formula: C22H23F3N4
Purity: >98 %
Solubility: DMSO : 16.67 mg/mL (41.63 mM; Need ultrasonic)
Introduction of 1254977-87-1 :

JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM. IC50 & Target: EC50: 17 nM (mGlu2 PAM)[1] 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]. 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[1].

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