| Name | BX430 |
| Description | 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. |
| In vitro | 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 30 mg/mL (72.62 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.84 mM), Sonication is recommended.
|
| Keywords | specificity | species | receptor | pain | P2XRs | P2XReceptor | P2X4 | P2X Receptor | Inhibitor | inhibit | human P2X4 receptor channels | human | disease | chronic | channels | cardiovascular | CalciumChannel | Calcium Channel | Ca2+ channels | Ca channels | BX-430 | BX430 | BX 430 |
| Inhibitors Related | Quadrol | Tricaine methanesulfonate | Nisoldipine | 2,4,6-Tri-tert-butylphenol | Chlorocresol | L-Ascorbic acid | L-Phenylalanine | ATP disodium salt | L-Ascorbic acid sodium salt | 2-Nitrobenzoic acid | Magnesium Chloride Hexahydrate | Magnesium sulfate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Calcium Channel Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Neuroprotective Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
