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BX430

CAT: 0013-GTR19157790-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19157790-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.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.
CAS Number
688309-70-8
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 83.33 mg/mL (201.71 mM)
Smiles
CC (C) c1cc (Br) c (NC (=O) Nc2cccnc2) c (Br) c1
Molecular Formula
C15H15Br2N3O
Molecular Weight
413.11
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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CatalogName
BA6575-50BX430

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