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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 74 In Stock
5MG 132 In Stock
10MG 194 In Stock
25MG 353 In Stock
50MG 530 In Stock
100MG 759 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    JNJ-42153605
  • Note
    Research use only, not for human use.
  • Brief Description
    JNJ-42153605 is a mGlu2 receptor positive allosteric modulator (EC50: 17 nM).
  • Description
    JNJ-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.
  • 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.
  • Synonyms
    JNJ-42153605 | JNJ 42153605 | JNJ42153605
  • Pathway
    Chromatin/Epigenetic
  • Target
    COX
  • Recptor
    mGluR2 PAM
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1254977-87-1
  • Formula Weight
    400.45
  • Molecular Formula
    C22H23F3N4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 16.67 mg/mL (41.63 mM)
  • SMILES
    c12c(c(ccn1c(nn2)CC1CC1)N1CCC(CC1)c1ccccc1)C(F)(F)F
  • Chemical Name
    3-(Cyclopropylmethyl)-7-(4-phenyl-1-piperidinyl)-8-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyridine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Cid JM, et al. J Med Chem. 2012 Oct 25;55(20):8770-89.
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