GW791343 dihydrochloride 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 dihydrochloride 能增强昼夜交替的 ATP 释放。GW791343 dihydrochloride 可用于神经系统疾病的研究。
| 生物活性 | GW791343 dihydrochloride 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 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study ofneurological disease[1][2]. |
| IC50& Target | P2X7 Receptor 6.9-7.2 (pIC50) |
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体外研究
(In Vitro) | 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[1].
GW791343 dihydrochloride (3, 10, 30 μM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor[1].
GW791343 dihydrochloride (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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(223.54 mM;Need ultrasonic) DMSO : 20 mg/mL(44.71 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2354 mL | 11.1769 mL | 22.3539 mL | | 5 mM | 0.4471 mL | 2.2354 mL | 4.4708 mL | | 10 mM | 0.2235 mL | 1.1177 mL | 2.2354 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 50 mg/mL (111.77 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.47 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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