JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
性状
Solid
体内研究(In Vivo)
When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED 50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED 50 of 10 mg/kg for SERT occupancy. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.
溶解度数据
In Vitro: DMSO : 100 mg/mL (223.90 mM; Need ultrasonic)配制储备液