| 名称 | JNJ-47965567 |
| 描述 | JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively). |
| 动物实验 | The authors used a combination of in vitro assays (calcium flux, radioligand binding, electrophysiology, IL-1β release) in both recombinant and native systems.?Target engagement of JNJ-47965567 was demonstrated by ex vivo receptor binding autoradiography and in vivo blockade of Bz-ATP induced IL-1β release in the rat brain.?Finally, the efficacy of JNJ-47965567 was tested in standard models of depression, mania and neuropathic pain |
| 体外活性 | JNJ-47965567 is potent high affinity (pKi 7.9 0.07), selective human P2X7 antagonist, with no significant observed speciation.?In native systems, the potency of the compound to attenuate IL-1β release was 6.7 0.07 (human blood), 7.5 0.07 (human monocytes) and 7.1 0.1 (rat microglia).?JNJ-47965567 exhibited target engagement in rat brain, with a brain EC50 of 78 19 ng·mL(-1) (P2X7 receptor autoradiography) and functional block of Bz-ATP induced IL-1β release.?JNJ-47965567 (30 mg·kg(-1) ) attenuated amphetamine-induced hyperactivity and exhibited modest, yet significant efficacy in the rat model of neuropathic pain.?No efficacy was observed in forced swim test. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 200 mg/mL (409.30 mM), Sonication is recommended.
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| 关键字 | Inhibitor | P2X7 | JNJ479655 | JNJ 47965567 | pain | P2X Receptor | JNJ47965567 | inhibit | JNJ-47965567 | JNJ 479655 | neuropathic | P2XRs |
| 相关产品 | Opiranserin hydrochloride | Aurintricarboxylic acid | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | JNJ-55308942 | JNJ-42253432 | Ivermectin | Lappaconitine | CTP disodium dihydrate | Brilliant blue G-250 |
| 相关库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 | 共价抑制剂库 | 离子通道库 | 抗癌化合物库 |
United States
