For research use only. Not for therapeutic Use.
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.
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].
| Catalog Number | I011238 |
| CAS Number | 688309-70-8 |
| Synonyms | 1-(2,6-dibromo-4-propan-2-ylphenyl)-3-pyridin-3-ylurea |
| Molecular Formula | C15H15Br2N3O |
| Purity | ≥95% |
| InChI | InChI=1S/C15H15Br2N3O/c1-9(2)10-6-12(16)14(13(17)7-10)20-15(21)19-11-4-3-5-18-8-11/h3-9H,1-2H3,(H2,19,20,21) |
| InChIKey | JFNKIJKRXKPQCC-UHFFFAOYSA-N |
| SMILES | CC(C)C1=CC(=C(C(=C1)Br)NC(=O)NC2=CN=CC=C2)Br |
| Reference | [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. |
