| Bioactivity | 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) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | BX430 | ||||||||||||
| CAS | 688309-70-8 | ||||||||||||
| Formula | C15H15Br2N3O | ||||||||||||
| Molar Mass | 413.11 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |