A 438079 hydrochloride |
| Catalog No.GC13733 |
An antagonist of the nucleotide receptor P2X7
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 899431-18-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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 Ca 2+ 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].
References:
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.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *