BX430 是一种有效且选择性的非竞争性的人 P2X4 受体通道变构拮抗剂，IC₅₀ 为 0.54 μM。 BX430 具有物种特异性。BX430 用于慢性疼痛和心血管疾病。

BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC 50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.

Solid

IC50: 0.54 μM (human P2X4 receptor channels)

BX430 has virtually no functional impact on all other P2X subtypes, namely, P2X1-P2X3, P2X5, and P2X7, at 10-100 times its IC50.
BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs.
Human P2X4-expressing cells treated with thapsigargin plus BX430 shows a significant reduction in the intracellular calcium rise evoked by ATP.
BX430 (5 μM) markedly reduces the amplitude of ATP-evoked intracellular calcium responses in THP-1 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 83.33 mg/mL (201.71 mM; Need ultrasonic)配制储备液