JNJ-47965567 是一种中央渗透性、高亲和力、选择性 P2X7 拮抗剂,对人和大鼠 P2X7 的 pKis 分别为 7.9 和 8.7。
Cas No. |
1428327-31-4 |
Canonical SMILES |
O=C(C1=CC=CN=C1SC2=CC=CC=C2)NCC3(CCOCC3)N(CC4)CCN4C5=CC=CC=C5 |
分子式 |
C28H32N4O2S |
分子量 |
488.6 |
溶解度 |
DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL,Ethanol: 12.5 mg/mL |
储存条件 |
Store at -20°C |
General tips |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition |
Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
半岛bd体育手机客户端 描述 |
JNJ-47965567 is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux, which is reduced by JNJ-47965567 in 1321N1 cells transfected with recombinant P2X7 human, macaque, dog, rat, or mouse protein with pIC50s of 8.3, 8.6, 8.5, 7.2, or 7.5, respectively. JNJ-47965567 suppresses neonatal hypoxia-induced seizures in mice and has some anticonvulsant properties in rats. It also reduces spontaneous seizures in epileptic mice even after treatment is stopped. |