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• 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：
  

  	1mg	5mg	10mg
  1 mM	2.235 ml	11.177 ml	22.354 ml
  5 mM	0.447 ml	2.235 ml	4.471 ml
  10 mM	0.224 ml	1.118 ml	2.235 ml
  50 mM	0.045 ml	0.224 ml	0.447 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *