JNJ-54175446
Names
[ CAS No. ]:
1627902-21-9
[ Name ]:
JNJ-54175446
Biological Activity
[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]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C18H13ClF4N6O
[ Molecular Weight ]:
440.78