Name | BX 430 |
Synonyms | BX 430 1-(2,6-Dibromo-4-isopropylphenyl)-3-(pyridin-3-yl)urea N-[2,6-Dibromo-4-(1-methylethyl)phenyl]-N'-(3-pyridinyl)urea Urea, N-[2,6-dibromo-4-(1-methylethyl)phenyl]-N'-3-pyridinyl- |
CAS | 688309-70-8 |
Molecular Formula | C15H15Br2N3O |
Molar Mass | 413.11 |
Melting Point | 164-168°C |
Solubility | DMSO : 83.33 mg/mL (201.71 mM; Need ultrasonic) |
Appearance | Solid |
Color | White |
Storage Condition | 2-8°C |
Use | BX430 is a potent and selective non-competitive human P2X4 receptor channel allosteric antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease. |
Target | human P2X4 receptor channels |
In vitro study | BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC 50 . 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.421 ml | 12.103 ml | 24.207 ml |
5 mM | 0.484 ml | 2.421 ml | 4.841 ml |
10 mM | 0.242 ml | 1.21 ml | 2.421 ml |
5 mM | 0.048 ml | 0.242 ml | 0.484 ml |
biological activity | BX430 is an effective, selective, non-competitive human P2X4 receptor channel allosteric antagonist, IC50 value is 0.54 μM. BX430 is an effective antagonist against zebrafish P2X4, but has no effect on rat and mouse P2X4 orthologs. BX430 can be used for chronic pain and cardiovascular diseases. |
target | TargetValue hP2X4 (Cell-free say) 0.54 μM |
Target | Value |
HP2X4 (Cell-free assay) | 0.54 μM |
in vitro study | BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC 50 . 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 μ M) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells. |