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JNJ-47965567 (JNJ-479655) 是中枢通透性、高亲和力、选择性的P2X7拮抗剂,可用于探讨中枢 P2X7 在中枢神经系统病理生理模型中的作用。它对人和大鼠 P2X7 作用的pKi 值分别为 7.9 和 8.7。
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JNJ-47965567 (JNJ-479655) 是中枢通透性、高亲和力、选择性的P2X7拮抗剂,可用于探讨中枢 P2X7 在中枢神经系统病理生理模型中的作用。它对人和大鼠 P2X7 作用的pKi 值分别为 7.9 和 8.7。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 313 | 现货 | |
2 mg | ¥ 429 | 现货 | |
5 mg | ¥ 619 | 现货 | |
10 mg | ¥ 993 | 现货 | |
25 mg | ¥ 1,990 | 现货 | |
50 mg | ¥ 3,180 | 现货 | |
100 mg | ¥ 4,560 | 现货 | |
500 mg | ¥ 9,490 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 667 | 现货 |
产品描述 | 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). |
靶点活性 | P2X7 (rat):8.7(pKis), P2X7 (human):7.9(pKis) |
体外活性 | JNJ-47965567是一种具有高亲和力(pKi 7.9 ± 0.07)和选择性的人类P2X7受体拮抗剂,没有观察到显著的种间差异。在天然系统中,这种化合物减少IL-1β释放的能力分别为:人血液中6.7 ± 0.07、人单核细胞中7.5 ± 0.07、大鼠微胶质细胞中7.1 ± 0.1。JNJ-47965567在大鼠脑中显示出靶向作用,其脑中EC50为78 ± 19 ng·mL(-1)(P2X7受体放射自显影)并且能阻断Bz-ATP诱导的IL-1β释放。以30 mg·kg(-1)剂量,JNJ-47965567减轻了苯丙胺诱导的超活动行为,并在大鼠神经病理疼痛模型中显示出了适度但显著的有效性。在强迫游泳测试中未观察到有效性。 |
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 |
别名 | JNJ-479655 |
分子量 | 488.64 |
分子式 | C28H32N4O2S |
CAS No. | 1428327-31-4 |
Smiles | O=C(NCC1(CCOCC1)N1CCN(CC1)c1ccccc1)c1cccnc1Sc1ccccc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 200 mg/mL (409.30 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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