| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 30 mg/mL (72.62 mM)
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| Keywords | P2X Receptor | Ca channels | chronic | channels | species | BX-430 | P2XRs | BX430 | Inhibitor | disease | Ca2+ channels | cardiovascular | P2X4 | receptor | specificity | inhibit | Calcium Channel | BX 430 | human | pain |
| Inhibitors Related | Nisoldipine | Nimodipine | 2,5-Di-tert-butylhydroquinone | Diltiazem hydrochloride | Levetiracetam | L-Ascorbic acid | Lanthanum(III) chloride heptahydrate | Butamben | Ethyl cinnamate | 1-Octanol | 1,2,4-Trihydroxybenzene | Otilonium bromide |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Calcium Channel Compound Library | Neuroprotective Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Ion Channel Targeted Library |
United States
