PSB-12062 (N-(p-Methylphenylsulfonyl)phenoxazine) (Synonyms: N-(p-Methylphenylsulfonyl)phenoxazine) |
Catalog No.GC30805 |
PSB-12062 (N-(p-metilfenilsulfonil)fenoxazina) es un antagonista potente y selectivo de P2X4 con una IC50 de 1,38 μM para P2X4 humano.
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Cas No.: 55476-47-6
Sample solution is provided at 25 µL, 10mM.
PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
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].
[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.
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