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.
IC50&Target
IC50: 0.54 μM (human P2X4 receptor channels)
体外研究
BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC50.
BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs.
Human P2X4-expressing cells treated with thapsigargin plus BX430 shows a significant reduction in the intracellular calcium rise evoked by ATP.
BX430 (5 μM) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells.
分子式
C15H15N3OBr2
分子量
413.11
CAS号
688309-70-8
运输条件
Room temperature in continental US; may vary elsewhere.