JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC 50 s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Action Type
ANTAGONIST
Mechanism of action
P2X purinoceptor 7 antagonist
Product Description
JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC 50 s 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 pIC 50 s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC 50 , 7.8, 7.9 and 8.1, respectively). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
JNJ-54175446 shows dose-dependent occupancy with the ED 50 of 0.46 mg/kg, corresponding to plasma EC 50 of 105 ng/mL . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
