JNJ-54166060 is a potent P2X7 antagonist. Bioactivity data of JNJ- rP2X7 IC50=4 nM; rP2X7 IC50=115nM; HLM/RLM = 0.35/0.64, ED50 = 2.3 mg/kg in rats. JNJ-54166060 shows high orally bioavailable bioavailability and low-moderate clearance in preclinical species, acceptable safety margins in rats, and a predicted human dose of 120 mg of QD. Additionally, JNJ-54166060 possesses a unique CYP profile and was found to be a regioselective inhibitor of midazolam CYP3A metabolism. References:

纯度：≥98%

CAS：1627900-42-8