
JNJ-42153605
CAS No. 1254977-87-1
JNJ-42153605( JNJ-42153605 | JNJ 42153605 | JNJ42153605 )
Catalog No. M17222 CAS No. 1254977-87-1
JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
Purity : >98% (HPLC)






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10MG | 194 | In Stock |
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25MG | 353 | In Stock |
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50MG | 530 | In Stock |
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100MG | 759 | In Stock |
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Biological Information
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Product NameJNJ-42153605
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NoteResearch use only, not for human use.
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Brief DescriptionJNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
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DescriptionJNJ-42153605 is a potent and selective mGlu2 receptor PAM with an acceptable pharmacokinetic profile in rodent and nonrodent species. JNJ-42153605 showed centrally mediated in vivo effectivity in models sensitive to mGlu2 receptor modulation such as sleep?wake electroencephalogram (sw-EEG) in rats,34 showing suppressed REM sleep during the first 4 h after oral administration of a 3 mg/kg dose.
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In VitroJNJ-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 VivoJNJ-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.
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SynonymsJNJ-42153605 | JNJ 42153605 | JNJ42153605
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PathwayChromatin/Epigenetic
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TargetCOX
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RecptormGluR2 PAM
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Research Area——
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Indication——
Chemical Information
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CAS Number1254977-87-1
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Formula Weight400.45
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Molecular FormulaC22H23F3N4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 16.67 mg/mL (41.63 mM)
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SMILESc12c(c(ccn1c(nn2)CC1CC1)N1CCC(CC1)c1ccccc1)C(F)(F)F
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Chemical Name3-(Cyclopropylmethyl)-7-(4-phenyl-1-piperidinyl)-8-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyridine
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Cid JM, et al. J Med Chem. 2012 Oct 25;55(20):8770-89.
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