Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 313 | 现货 | ||
2 mg | ¥ 449 | 现货 | ||
5 mg | ¥ 739 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 2,220 | 现货 | ||
50 mg | ¥ 3,320 | 现货 | ||
100 mg | ¥ 4,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 868 | 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 (human):7.9(pKis), P2X7 (rat):8.7(pKis) |
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. |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (409.30 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0465 mL | 10.2325 mL | 20.465 mL | 51.1624 mL |
5 mM | 0.4093 mL | 2.0465 mL | 4.093 mL | 10.2325 mL | |
10 mM | 0.2046 mL | 1.0232 mL | 2.0465 mL | 5.1162 mL | |
20 mM | 0.1023 mL | 0.5116 mL | 1.0232 mL | 2.5581 mL | |
50 mM | 0.0409 mL | 0.2046 mL | 0.4093 mL | 1.0232 mL | |
100 mM | 0.0205 mL | 0.1023 mL | 0.2046 mL | 0.5116 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
JNJ-47965567 1428327-31-4 Membrane transporter/Ion channel Neuroscience P2X Receptor Inhibitor P2X7 JNJ479655 JNJ 47965567 pain JNJ47965567 JNJ-479655 inhibit JNJ 479655 neuropathic P2XRs inhibitor