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Home - Products - Membrane Transporter/Ion Channel - P2X Receptor - JNJ-42253432

JNJ-42253432

CAS No. 1428327-35-8

JNJ-42253432( —— )

Catalog No. M34298 CAS No. 1428327-35-8

JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    JNJ-42253432
  • Note
    Research use only, not for human use.
  • Brief Description
    JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.
  • Description
    JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
  • In Vitro
    ——
  • In Vivo
    When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED50 of 10 mg/kg for SERT occupancy.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    P2X Receptor
  • Recptor
    P2X Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1428327-35-8
  • Formula Weight
    446.63
  • Molecular Formula
    C28H38N4O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (223.90 mM; Ultrasonic )
  • SMILES
    CN1CCc2c(C1)cccc2C(=O)NCC1(CCCCC1)N1CCN(CC1)c1ccccc1
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.?
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