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A 438079 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A 438079 hydrochloride图片
CAS NO:899431-18-6
规格:98%
分子量:342.61
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
P2X7 receptor antagonist,competitive and selective
CAS:899431-18-6
分子式:C13H10Cl3N5
分子量:342.61
纯度:98%
存储:Store at -20°C

Background:

A 438079 hydrochloride is a selective antagonist of P2X7 receptor with IC50 values of 100 and 300 nM in rat and human, respectively [1].


A 438079 is a derivative of the origin compound tetrazole 5 selected out as a novel P2X7 receptor antagonist. In human 1321N1 astrocytoma cells with expressing recombinant human P2X7, A 438079 treatment suppressed the Ca2+flux with pIC50 value of 6.9. In the pore formation assay, A 438079 blocked the pore formation of human THP-1 cells and prevented the cells from uptaking the diiodide dye YO-PRO. Moreover, in the spinal nerve ligation model, administration of A 438079 reduced the neuropathic pain induced by the application of a von Frey hair. The ED50 value was 76 μM/kg [2].


参考文献:
1. Nelson D W, Gregg R J, Kort M E, et al. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. Journal of medicinal chemistry, 2006, 49(12): 3659-3666.
2. Donnelly-Roberts D L, Jarvis M F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. British journal of pharmacology, 2007, 151(5): 571-579.