Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 39.00 | |
5 mg | In stock | $ 64.00 | |
10 mg | In stock | $ 113.00 | |
25 mg | In stock | $ 240.00 | |
50 mg | In stock | $ 383.00 | |
100 mg | In stock | $ 569.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 70.00 |
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. |
Targets&IC50 | P2X4 receptor (human):0.54 μM |
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]. |
Molecular Weight | 413.11 |
Formula | 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)
You can also refer to dose conversion for different animals. More
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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