<Suppliers Price>

BX 430

Names

[ CAS No. ]:
688309-70-8

[ Name ]:
BX 430

[Synonym ]:
1-(2,6-Dibromo-4-isopropylphenyl)-3-(3-pyridinyl)urea
N-(2,6-dibromo-4-isopropylphenyl)-N'-(3-pyridinyl)urea
Urea, N-[2,6-dibromo-4-(1-methylethyl)phenyl]-N'-3-pyridinyl-

Biological Activity

[Description]:

BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Cardiovascular Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

[Target]

IC50: 0.54 μM (human P2X4 receptor channels)[1]


[In Vitro]

BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC50[1]. BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs[1]. Human P2X4-expressing cells treated with thapsigargin plus BX430 shows a significant reduction in the intracellular calcium rise evoked by ATP[1]. BX430 (5 μM) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells[1].

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
395.4±42.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H15Br2N3O

[ Molecular Weight ]:
413.107

[ Flash Point ]:
192.9±27.9 °C

[ Exact Mass ]:
410.958160

[ LogP ]:
4.56

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.679

Safety Information

[ Hazard Codes ]:
Xn

Related Compounds