JNJ-54175446

SKU: orb1707157

Description

JNJ-54175446 is a brain-penetrant, selective P2X7 receptor antagonist that inhibits microglial release of pro-inflammatory cytokines IL-1β and IL-18. It is a valuable research tool for investigating neuroinflammation in depression models, with applications in both in vitro cellular assays and in vivo behavioral studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1627902-21-9
• MW: 440.78
• Purity: 99.79%
• Formula: C₁₈H₁₃ClF₄N₆O
• SMILES: C[C@H]1N(CCc2c1nnn2-c1ncc(F)cn1)C(=O)c1cccc(c1Cl)C(F)(F)F
• Target: P2X Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.54 mM);DMSO:50 mg/mL (113.44 mM)

Bioactivity

• Target IC50:
  P2X7 receptor (rat):8.81(pic50)|P2X7 receptor (rat):8.81 (pIC50)|P2X7 receptor (human):(pic50)8.46 |P2X7 receptor (human):8.46 (pIC50)
• In Vivo:
  JNJ-54175446 (30 mg/kg, intraperitoneal) administered once daily significantly reduces spontaneous recurrent seizures in mice, persisting for several days after the end of treatment.
• In Vitro:
  JNJ-54175446 is a selective purinergic P2X7 receptor (P2X7R) antagonist that attenuates the release of IL-1β/IL-18 from microglial cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

hP2X7 receptor, P2X Receptor, P2X7, P2XReceptor, JNJ54175446, JNJ-54175446, JNJ-5446, JNJ 54175446, rP2X7 receptor

Compound Identifiers

PubChem CID

90409366