BX430

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BX430 用于治疗慢性疼痛和心血管疾病，它是一种有效的、选择性的非竞争性变构人 P2X4 受体通道拮抗剂，IC50 为 0.54 μM。 BX430具有物种特异性。

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.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.

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Neuroscience

P2 Receptor

human P2X4 receptor channels

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688309-70-8

413.11

C15H15Br2N3O

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (201.71 mM)

CC(C)c1cc(Br)c(NC(=O)Nc2cccnc2)c(Br)c1

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(-20℃)

With Ice Pack

≥ 2 years