货号:A1226351 同义名: Blocker of P2X4 Compound 3.0
BX430 is selective P2X4 allosteric antagonist with IC50 of 0.54 μM.
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描述 | The P2X4 receptor channel is an ATP-gated nonselective cation channel widely expressed in central neurons. BX430 is a potent antagonist of P2X4 with an IC50 of 0.54μM. It is highly selective towards P2X4, showing no functional impact other P2X subtypes (i.e. P2X1–P2X3, P2X5, and P2X7) at 10 – 100 times its IC50. BX430 at a concentration of 5μM significantly reduced both peak (–29%) and total (–75%) current of the P2X4 channel response when co-applied with ATP. The application of 5μM extracellular BX430 during the desensitizing phase of the P2X4 current evoked an immediate acceleration of the relaxation. Treatment with 10μM BX430 significantly blocked ivermectin (3μM)-potentiated P2X4 current response (67%). P2X4-mediated YO-PRO1 uptake was also significantly inhibited by 5μM BX430[1]. |
作用机制 | BX430 is a highly selective, noncompetitive P2X4 antagonist that binds to an allosteric site on the P2X4 receptor channel. It acts on the P2X4 channel from the extracellular side[1]. |
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存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.42mL 0.48mL 0.24mL |
12.10mL 2.42mL 1.21mL |
24.21mL 4.84mL 2.42mL |
CAS号 | 688309-70-8 |
分子式 | C15H15Br2N3O |
分子量 | 413.107 |
别名 | Blocker of P2X4 Compound 3.0 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 85 mg/mL(205.76 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |