JNJ-55308942 是 P2X7 功能性的选择性脑渗透拮抗剂，对 hP2X7 和 rP2X7 的 IC50 分别为 10 和 15 nM，Kis 分别为 7.1 和 2.9 nM。

JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.

JNJ-55308942 shows pKis of 8.1and 8.5 for recombinant hP2X7 and rP2X7. JNJ-55308942 attenuates IL-1β release in a concentration-dependent manner in human blood and in mouse blood and microglia[2].

JNJ-55308942 (5 mg/kg; p.o.) shows the F of 81%, Vss of 1.7 L/kg, CL of 1.7 L/kg, Cmax of 3.7 mL min/kg, and AUC of 1747 ng/mL[1]. In male C57/BL6J mice, JNJ-55308942 (30 mg/kg; p.o.) significantly attenuates the effect of LPS on FSC, CD45 surface expression, and CD11b surface expression. In a model of Bacillus Calmette-Guerin-induced depression, JNJ-55308942 (30 mg/kg; orally) reverses the BCG-induced deficits of sucrose preference and social interaction (ED50 = 0.07 mg/kg). The P2X7 antagonist (3 mg/kg, orally) blocks Bz-ATP-induced brain IL-1β release in conscious rats[2].

2166558-11-6

C17H12F5N7O

425.32

DMSO:90mg/mL (211.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years