| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
| S81689-5mg | 94% | ￥990.00 | 货期：2-3天 | - | - | - |
|
| S81689-10mg | 94% | ￥1400.00 | 货期：2-3天 | - | - | - |
|
| S81689-50mg | 94% | ￥5500.00 | 货期：2-3天 | - | - | - |
|
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease
| 产品描述： | GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | P2X7 Receptor:6.9-7.2 (pIC50);P2XReceptor | ||||||||||||||||||||
| 体外研究： | GW791343 dihydrochloride (0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM; 40 min) shows a non-competitive antagonistic activity to the human P2X7 receptor. GW791343 dihydrochloride (3, 10, 30 µM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor. GW791343 dihydrochloride (5 µM; 24-48 h; ATP measured every 4 h) enhances ATP rhythm in SCN cells. Cell Viability Assay Cell Line: HEK293 cells (expressing human recombinant P2X7 receptors) Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM Incubation Time: 40 min (pre-incubate for 10 min and incubate with other P2X7 receptor antagonists for another 30 min) Result: Inhibited agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer.Reduced maximal responses toATP and BzATP in sucrose buffer. Cell Viability Assay Cell Line: HEK293 cells (expressing human recombinant P2X7 receptors) Concentration: 3, 10, 30 µM Incubation Time: 40 min (pre-incubate for 10 min and incubate with other P2X7 receptor antagonists for another 30 min) Result: Showed slow reversal effects at the human P2X7 receptor (after 45 min had reversed sufficiently), and had a rapid dissociation rate. Cell Viability Assay Cell Line: SCN cells (from 16-to 21- day-old Wistar rats, which are kept under a controlled 12-12 h light-dark cycle from birth) Concentration: 5 µM (replace the medium with fresh drug-containing culture medium every 4 h). Incubation Time: 24-48 h (ATP measured every 4 h) Result: Enhanced the amplitude of ATP release rhythm and | ||||||||||||||||||||
| 参考文献： | 1. Michel AD, et al. Negative and positive allosteric modulators of the P2X(7) receptor. Br J Pharmacol. 2008 Feb;153(4):737-50. 2. Svobodova I, et al. Circadian ATP Release in Organotypic Cultures of the Rat Suprachiasmatic Nucleus Is Dependent on P2X7 and P2Y Receptors. Front Pharmacol. 2018 Mar 6;9:192. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、H2O | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 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
沪公网安备 31011702002021号
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