GW791343 3HCl

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 HCl是GW791343的HCl盐形式，GW791343是人P2X7受体抑制剂的非竞争性变构调节剂，pIC50为7。

GW791343 HCl is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.

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.GW791343 trihydrochloride (3, 10, 30 μM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor.GW791343 trihydrochloride (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 extracellular ATP accumulation to 144 of control levels.

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Neuroscience

GluR

P2X7

Neurological Disease

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309712-55-8

483.81

C20H24F2N4O·3HCl

>98% (HPLC)

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CC1=C(C=C(C=C1)CN2CCNCC2)NC(=O)CNC3=CC(=C(C=C3)F)F.Cl.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years