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1627902-21-9

1627902-21-9 structure
1627902-21-9 structure
  • Name: JNJ-54175446
  • Chemical Name: JNJ-54175446
  • CAS Number: 1627902-21-9
  • Molecular Formula: C18H13ClF4N6O
  • Molecular Weight: 440.78
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
  • Create Date: 2019-02-09 15:55:20
  • Modify Date: 2024-01-05 15:32:08
  • 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.

Name JNJ-54175446
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.
Related Catalog
Target

pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor)[1]

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)[1].
In Vivo JNJ-54175446 shows dose-dependent occupancy with the ED50 of 0.46 mg/kg, corresponding to plasma EC50 of 105 ng/mL[1].
References

[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

Molecular Formula C18H13ClF4N6O
Molecular Weight 440.78