JNJ-47965567
产品说明书
 |
同义名 : | - |
| CAS号 : | 1428327-31-4 | |
| 货号 : | A720722 | |
| 分子式 : | C28H32N4O2S | |
| 纯度 : | 99%+ | |
| 分子量 : | 488.64 | |
| MDL号 : | MFCD28334214 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The purinergic receptor P2X, ligand-gated ion channel, 7 (P2X7) is an ATP-gated ion channel that plays an essential role in neuropsychiatry, neurodegeneration, and chronic pain. JNJ 47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist with high affinity binding at both the human (pKi=7.9±0.07) and rat (pKi=8.7±0.07) P2X7 ion channel. The potency (pIC50) of JNJ 47965567 to attenuate Bz-ATP-induced calcium flux at human, macaque, dog, rat, and mouse P2X7 was 8.3±0.08, 8.6±0.1, 8.5±0.2, 7.2±0.08, and 7.5±0.1, respectively. JNJ 47965567 reduced LPS primed BZ-ATP-induced IL-1β release with a pIC50 of 6.7±0.07 in human whole blood and a pIC50 of 7.5±0.07 in freshly isolated human monocytes from the blood. JNJ 47965567 also inhibited IL-18 release with a pIC50 value of 7.3 ± 0.1. JNJ-47965567 at a concentration of 100nM rapidly inhibited Bz-ATP-evoked currents in 1321N1 cells expressing hP2X7 (93.9% inhibition). Subcutaneous dosing of JNJ 47965567 at 100mg/kg significantly attenuated IL-1β release in rats challenged with Bz-ATP, a P2X7 agonist. In a rat model of neuropathic pain, subcutaneous administration of JNJ 47965567 at a dose of 30mg/kg resulted in a significant increase in tactile thresholds lasting from 30–60min post-administration[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.05mL 0.41mL 0.20mL |
10.23mL 2.05mL 1.02mL |
20.46mL 4.09mL 2.05mL |
| 参考文献 |
|---|