Description: |
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease. |
Target: |
IC50: 0.54 μM (human P2X4 receptor channels)[1] |
In Vitro: |
BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC50[1]. BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs[1]. Human P2X4-expressing cells treated with thapsigargin plus BX430 shows a significant reduction in the intracellular calcium rise evoked by ATP[1]. BX430 (5 μM) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells[1]. |
References: |
[1]. Ase AR, et al. Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels. Mol Pharmacol. 2015 Apr;87(4):606-16.
[2]. Sophocleous RA, et al. Pharmacological and genetic characterisation of the canine P2X4 receptor. Br J Pharmacol. 2020 Feb 4. |