| 产品描述： | A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta |
| 靶点： |
IC50: of 20 nM (human P2X7 receptor), 42 nM (rat P2X7 receptor), 150 nM (mouse P2X7 receptor);P2XReceptor;CalciumChannel |
| 体外研究： |
A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models. A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes. RT-PCR Cell Line: Optic nerve astrocyte cells Concentration: 50 nM Incubation Time: 1 hour(pre-treatment) Result: Prevented the IL-1β priming in astrocyte cells |
| 体内研究： |
A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats. A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice. A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals. Animal Model: Male Sprague-Dawley, BALB/c mice and IL-1(−/−) mice for CFA-induced chronic inflammatory Dosage: 30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice) Administration: Injection; pre-injected 30mins Result: Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1(−/−) mice. |
| 参考文献： |
1. Honore P, et al. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81. 2. Albalawi F et.al, The P2X7 Receptor Primes IL-1β and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain. Front Cell Neurosci. 2017 Aug 8;11:227 3. Falk S et al.P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience. 2015 Apr 16; 291:93-105. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.42 ml |
12.099 ml |
24.198 ml |
| 5 mM |
0.484 ml |
2.42 ml |
4.84 ml |
| 10 mM |
0.242 ml |
1.21 ml |
2.42 ml |
| 50 mM |
0.048 ml |
0.242 ml |
0.484 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京