Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BX430 是一种有效的选择性非竞争性变构人 P2X4 受体通道拮抗剂,IC50 为 0.54 μM。它具有物种特异性,可用于治疗慢性疼痛和心血管疾病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 298 | 现货 | ||
2 mg | ¥ 428 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 1,220 | 现货 | ||
25 mg | ¥ 2,320 | 现货 | ||
50 mg | ¥ 3,710 | 现货 | ||
100 mg | ¥ 5,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 778 | 现货 |
产品描述 | BX430 is used for chronic pain and cardiovascular disease and it is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. |
靶点活性 | P2X4 receptor (human):0.54 μM |
体外活性 | BX430, with submicromolar potency (IC50 = 0.54 M). BX430 is highly selective, having virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC50.?Unexpected species differences were noticed, as BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs.?The concentration-response curve for ATP on human P2X4 in the presence of BX430 shows an insurmountable blockade, indicating a noncompetitive allosteric mechanism of action.?Using a fluorescent dye uptake assay, we observed that BX430 also effectively suppresses ATP-evoked and ivermectin-potentiated membrane permeabilization induced by P2X4 pore dilation.?Finally, in single-cell calcium imaging, we validated its selective inhibitory effects on native P2X4 channels at the surface of human THP-1 cells that were differentiated into macrophages.?In summary, this ligand provides a novel molecular probe to assess the specific role of P2X4 in inflammatory and neuropathic conditions, where ATP signaling has been shown to be dysfunctional[1]. |
分子量 | 413.11 |
分子式 | C15H15Br2N3O |
CAS No. | 688309-70-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (72.62 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4207 mL | 12.1033 mL | 24.2066 mL | 60.5166 mL |
5 mM | 0.4841 mL | 2.4207 mL | 4.8413 mL | 12.1033 mL | |
10 mM | 0.2421 mL | 1.2103 mL | 2.4207 mL | 6.0517 mL | |
20 mM | 0.121 mL | 0.6052 mL | 1.2103 mL | 3.0258 mL | |
50 mM | 0.0484 mL | 0.2421 mL | 0.4841 mL | 1.2103 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BX430 688309-70-8 Membrane transporter/Ion channel Metabolism Neuroscience P2X Receptor Calcium Channel Ca channels chronic channels species BX-430 P2XRs Inhibitor disease Ca2+ channels cardiovascular P2X4 receptor specificity inhibit BX 430 human pain inhibitor