GW791343 (HCl)

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GW791343 是一种 P2X7 变构调节剂。

GW791343 is a P2X7 allosteric modulator.?

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 AssayCell 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 extracellular ATP accumulation to 144 of control levels.

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Neuroscience

P2 Receptor

P2X7

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1019779-04-4

483.8

C20H27Cl3F2N4O

>98% (HPLC)

DMSO:42 mg/mL?(93.89 mM)

Cc1ccc(CN2CCNCC2)cc1NC(=O)CNc1ccc(F)c(F)c1.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years