| Bioactivity | PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4. | ||||||||||||
| Target | IC50: 1.38 μM (human P2X4), 92.8 nM (rat P2X4), 1.76 μM (mouse P2X4) | ||||||||||||
| Invitro | PSB-12062 shows similar potency in human, rat, and mouse species. PSB-12062 shows to be allosteric in nature with a 35-fold selectivity toward P2X4 versus P2X1, P2X2, P2X3, and P2X7. However, PSB-12062 is unable to completely block ATP-induced P2X4-mediated calcium influx even when used at high concentrations (>30 μM)[1]. | ||||||||||||
| Name | PSB-12062 | ||||||||||||
| CAS | 55476-47-6 | ||||||||||||
| Formula | C19H15NO3S | ||||||||||||
| Molar Mass | 337.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Hernandez-Olmos V, et al. N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists. J Med Chem. 2012 Nov 26;55(22):9576-88. [2]. Stokes L, et al. P2X4 Receptor Function in the Nervous System and Current Breakthroughs in Pharmacology.Front Pharmacol. 2017 May 23;8:291. |