GW791343 dihydrochloride是有种属特异性的P2X7变构调节剂,对人P2X7的pIC50为6.9-7.2。
产品描述
GW791343 dihydrochloride is a P2X7 allosteric modulator.
体外活性
GW791343 were non-competitive inhibitors of human P2X(7) receptors.?Receptor protection studies using decavanadate and pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS) showed that neither compound-17 nor GW791343 competitively interacted at the ATP binding site and so were probably negative allosteric modulators of the P2X(7) receptor.?GW791343 prevented the slowly reversible blockade of the human P2X(7) receptor produced by compound-17 and inhibited [(3)H]-compound-17 binding to the P2X(7) receptor suggesting they may bind to similar or interacting sites[1].
Cas No.
1019779-04-4
分子式
C20H26Cl2F2N4O
分子量
447.35
别名
GW791343 (HCl)
储存和溶解度
DMSO:42 mg/mL (93.89 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years