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 pIC 50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.
性状
Solid
IC50 & Target[1][2]
P2X7 Receptor 6.9-7.2 (pIC50)
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.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. has not independently confirmed the accuracy of these methods. They are for reference only.
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)
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.
溶解度数据
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]. 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.