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BX430

Catalog No. T14844 CAS 688309-70-8

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.

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BX430, CAS 688309-70-8

Pack Size	Availability	Price/USD
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

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Purity: 99.95%

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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.
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (72.62 mM)

References and Literature

1. Ase AR, et al. Identification and characterization of a selective allosteric antagonist of human P2X4 receptor channels. Mol Pharmacol. 2015 Apr;87(4):606-16. 2. Sophocleous RA, et al. Pharmacological and genetic characterisation of the canine P2X4 receptor. Br J Pharmacol. 2020 Feb 4.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Metabolism Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Anti-Hypertension Compound Library Bioactive Compounds Library Max Calcium Channel Compound Library Bioactive Compound Library Anti-Cardiovascular Disease Compound Library

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Keywords

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

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