BX430

SKU: orb1308509

Description

BX430 is a potent, selective, and species-specific noncompetitive allosteric antagonist of human P2X4 receptor channels (IC₅₀ = 0.54 µM). It serves as a valuable research tool for investigating the role of P2X4 in pathologies such as chronic pain and cardiovascular disease, with utility in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	688309-70-8
MW	413.11
Purity	99.95%
Formula	C₁₅H₁₅Br₂N₃O
SMILES	CC(C)c1cc(Br)c(NC(=O)Nc2cccnc2)c(Br)c1
Target	Calcium Channel,P2X Receptor
Solubility	DMSO:30 mg/mL (72.62 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.84 mM)

Bioactivity

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Target 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.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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P2X Receptor, P2X4, P2XReceptor, P2XRs, receptor, specificity, species, Inhibitor, human P2X4 receptor channels, human, pain, inhibit, Ca channels, BX 430, BX430, BX-430, cardiovascular, Calcium Channel, Ca2+ channels, channels, CalciumChannel, chronic, disease

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Compound Identifiers

PubChem CID

2810999 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	688309-70-8
MW:	413.11
Formula:	C₁₅H₁₅Br₂N₃O

BX430

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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