688309-70-8|1-(2,6-Dibromo-4-isopropylphenyl)-3-(pyridin-3-yl)urea|CsnPharm

CAS No.: 688309-70-8

BX430 Catalog No. CSN25312

Synonyms: Blocker of P2X4 Compound 3.0

BX430 is selective P2X4 allosteric antagonist with IC50 of 0.54 μM.

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实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4207 mL
- 12.1034 mL
- 24.2068 mL
- 5 mM
- 0.4841 mL
- 2.4207 mL
- 4.8414 mL
- 10 mM
- 0.2421 mL
- 1.2103 mL
- 2.4207 mL

技术信息

CAS号

688309-70-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H15Br2N3O

运输

蓝冰

分子量

413.11

别名

Blocker of P2X4 Compound 3.0

溶解度

DMSO	83.0 mg/mL (200.9 mM)
Water	Insoluble
Ethanol	83.0 mg/mL (200.9 mM)

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BX430 Catalog No. CSN25312

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