BX430

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Chemical Structure| 688309-70-8 同义名 : Blocker of P2X4 Compound 3.0
CAS号 : 688309-70-8
货号 : A1226351
分子式 : C15H15Br2N3O
纯度 : 99%+
分子量 : 413.107
MDL号 : MFCD02678819
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -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：
生物活性
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].
实验方案
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
参考文献

[1]Ase AR, Honson NS, Zaghdane H, Pfeifer TA, Séguéla P. Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels. Mol Pharmacol. 2015 Apr;87(4):606-16. doi: 10.1124/mol.114.096222