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Home - Products - Membrane Transporter/Ion Channel - P2X Receptor - JNJ-54175446

JNJ-54175446

CAS No. 1627902-21-9

JNJ-54175446( —— )

Catalog No. M33391 CAS No. 1627902-21-9

JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β/IL-18 from microglia, and may be used in the study of depression.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    JNJ-54175446
  • Note
    Research use only, not for human use.
  • Brief Description
    JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β/IL-18 from microglia, and may be used in the study of depression.
  • Description
    JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.
  • In Vitro
    JNJ-54175446 (Compound 14) is a potent and selective brain penetrant P2X7 antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC50, 7.8, 7.9 and 8.1, respectively).
  • In Vivo
    JNJ-54175446 shows dose-dependent occupancy with the ED50 of 0.46 mg/kg, corresponding to plasma EC50 of 105 ng/mL.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    P2X Receptor
  • Recptor
    P2X Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1627902-21-9
  • Formula Weight
    440.78
  • Molecular Formula
    C18H13ClF4N6O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 62.5 mg/mL (141.79 mM; Ultrasonic )
  • SMILES
    C[C@H]1N(CCc2c1nnn2-c1ncc(F)cn1)C(=O)c1cccc(c1Cl)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Letavic MA, et al. 4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. Send to?
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