2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. GW791343 trihydrochloride

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。

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GW791343 trihydrochloride Chemical Structure

GW791343 trihydrochloride Chemical Structure

CAS No. : 309712-55-8

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GW791343 trihydrochloride 的其他形式现货产品:

Other Forms of GW791343 trihydrochloride:

GW791343 trihydrochloride 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

GW791343 trihydrochloride 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 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GW791343 trihydrochloride 相关抗体:

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

483.81

Formula

C20H27Cl3F2N4O
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.
纯度 & 产品资料
参考文献

GW791343 trihydrochloride 相关分类

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Keywords:

GW791343 trihydrochloride309712-55-8P2X ReceptorP2XRsneurological diseasedepressive disorderSCN cellsATPInhibitorinhibitorinhibit

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