GW791343 trihydrochloride 是一种有效的人P2X7受体负变构调节剂 (有种属特异性)，对人P2X7受体产生非竞争性拮抗作用，其pIC50值为 6.9-7.2。GW791343 trihydrochloride 能增强昼夜交替的 ATP 释放。GW791343 trihydrochloride 可用于神经系统疾病的研究。
| 生物活性 | GW791343 trihydrochloride is a potent humanP2X7receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on humanP2X7receptor, with apIC50of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study ofneurological disease[1][2]. |
| IC50& Target | P2X7 Receptor 6.9-7.2 (pIC50) |
|
体外研究
(In Vitro) | GW791343 trihydrochloride (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[1].
GW791343 trihydrochloride (3, 10, 30 μM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor[1].
GW791343 trihydrochloride (5 μM; 24-48 h; ATP measured every 4 h) enhances ATP rhythm in SCN cells[2].
Cell Viability Assay[1] | 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[1] | 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[2] | 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 extracellular ATP accumulation to 144 of control levels. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com